sulfonamides

Summary

Summary: A group of compounds that contain the structure SO2NH2. Members of this group, also known as sulfa drugs, are derivatives of sulfanilamide, which competitively inhibit folic acid synthesis in microorganisms, and are bacteriostatic. They have been largely supplanted by more effective and less toxic antibiotics. (From Dorland, 28th ed)

Top Publications

  1. ncbi Effect of very high-intensity statin therapy on regression of coronary atherosclerosis: the ASTEROID trial
    Steven E Nissen
    Department of Cardiovascular Medicine, Cleveland Clinic Lerner School of Medicine, Cleveland, Ohio 44195, USA
    JAMA 295:1556-65. 2006
  2. pmc Inhibition of mutated, activated BRAF in metastatic melanoma
    Keith T Flaherty
    Abramson Cancer Center of the University of Pennsylvania, Philadelphia, USA
    N Engl J Med 363:809-19. 2010
  3. pmc Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation
    Ramin Nazarian
    Division of Dermatology Department of Medicine, UCLA s Jonsson Comprehensive Cancer Center, 52 121 CHS, Los Angeles, California 90095 1750, USA
    Nature 468:973-7. 2010
  4. ncbi Rosuvastatin to prevent vascular events in men and women with elevated C-reactive protein
    Paul M Ridker
    Center for Cardiovascular Disease Prevention, Brigham and Women s Hospital, Harvard Medical School, Boston, MA 02215, USA
    N Engl J Med 359:2195-207. 2008
  5. ncbi An inhibitor of Bcl-2 family proteins induces regression of solid tumours
    Tilman Oltersdorf
    Idun Pharmaceuticals, 9380 Judicial Drive, San Diego, California 92121, USA
    Nature 435:677-81. 2005
  6. pmc RAF inhibitor resistance is mediated by dimerization of aberrantly spliced BRAF(V600E)
    Poulikos I Poulikakos
    Department of Molecular Pharmacology and Chemistry, Memorial Sloan Kettering Cancer Center, New York, New York 10065, USA
    Nature 480:387-90. 2011
  7. ncbi Pazopanib in locally advanced or metastatic renal cell carcinoma: results of a randomized phase III trial
    Cora N Sternberg
    FACP, Department of Medical Oncology, San Camillo Forlanini Hospital, Circonvallazione Gianicolense 87, Rome, Italy 00152
    J Clin Oncol 28:1061-8. 2010
  8. pmc COT drives resistance to RAF inhibition through MAP kinase pathway reactivation
    Cory M Johannessen
    Broad Institute of Harvard and Massachusetts Institute of Technology, 7 Cambridge Center, Cambridge, Massachusetts 02142, USA
    Nature 468:968-72. 2010
  9. ncbi ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor
    Christin Tse
    Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064 6101, USA
    Cancer Res 68:3421-8. 2008
  10. pmc The BH3 mimetic ABT-737 targets selective Bcl-2 proteins and efficiently induces apoptosis via Bak/Bax if Mcl-1 is neutralized
    Mark F van Delft
    The Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, Victoria 3050, Australia
    Cancer Cell 10:389-99. 2006

Detail Information

Publications325 found, 100 shown here

  1. ncbi Effect of very high-intensity statin therapy on regression of coronary atherosclerosis: the ASTEROID trial
    Steven E Nissen
    Department of Cardiovascular Medicine, Cleveland Clinic Lerner School of Medicine, Cleveland, Ohio 44195, USA
    JAMA 295:1556-65. 2006
    ....
  2. pmc Inhibition of mutated, activated BRAF in metastatic melanoma
    Keith T Flaherty
    Abramson Cancer Center of the University of Pennsylvania, Philadelphia, USA
    N Engl J Med 363:809-19. 2010
    ..The identification of somatic mutations in the gene encoding the serine-threonine protein kinase B-RAF (BRAF) in the majority of melanomas offers an opportunity to test oncogene-targeted therapy for this disease...
  3. pmc Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation
    Ramin Nazarian
    Division of Dermatology Department of Medicine, UCLA s Jonsson Comprehensive Cancer Center, 52 121 CHS, Los Angeles, California 90095 1750, USA
    Nature 468:973-7. 2010
    ....
  4. ncbi Rosuvastatin to prevent vascular events in men and women with elevated C-reactive protein
    Paul M Ridker
    Center for Cardiovascular Disease Prevention, Brigham and Women s Hospital, Harvard Medical School, Boston, MA 02215, USA
    N Engl J Med 359:2195-207. 2008
    ....
  5. ncbi An inhibitor of Bcl-2 family proteins induces regression of solid tumours
    Tilman Oltersdorf
    Idun Pharmaceuticals, 9380 Judicial Drive, San Diego, California 92121, USA
    Nature 435:677-81. 2005
    ....
  6. pmc RAF inhibitor resistance is mediated by dimerization of aberrantly spliced BRAF(V600E)
    Poulikos I Poulikakos
    Department of Molecular Pharmacology and Chemistry, Memorial Sloan Kettering Cancer Center, New York, New York 10065, USA
    Nature 480:387-90. 2011
    ....
  7. ncbi Pazopanib in locally advanced or metastatic renal cell carcinoma: results of a randomized phase III trial
    Cora N Sternberg
    FACP, Department of Medical Oncology, San Camillo Forlanini Hospital, Circonvallazione Gianicolense 87, Rome, Italy 00152
    J Clin Oncol 28:1061-8. 2010
    ..CONCLUSION Pazopanib demonstrated significant improvement in PFS and tumor response compared with placebo in treatment-naive and cytokine-pretreated patients with advanced and/or metastatic RCC...
  8. pmc COT drives resistance to RAF inhibition through MAP kinase pathway reactivation
    Cory M Johannessen
    Broad Institute of Harvard and Massachusetts Institute of Technology, 7 Cambridge Center, Cambridge, Massachusetts 02142, USA
    Nature 468:968-72. 2010
    ....
  9. ncbi ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor
    Christin Tse
    Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064 6101, USA
    Cancer Res 68:3421-8. 2008
    ..The oral efficacy of ABT-263 should provide dosing flexibility to maximize clinical utility both as a single agent and in combination regimens...
  10. pmc The BH3 mimetic ABT-737 targets selective Bcl-2 proteins and efficiently induces apoptosis via Bak/Bax if Mcl-1 is neutralized
    Mark F van Delft
    The Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, Victoria 3050, Australia
    Cancer Cell 10:389-99. 2006
    ..Hence, ABT-737 should prove efficacious in tumors with low Mcl-1 levels, or when combined with agents that inactivate Mcl-1, even to treat those tumors that overexpress Bcl-2...
  11. pmc RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF
    Poulikos I Poulikakos
    Program in Molecular Pharmacology and Chemistry and Department of Medicine, Memorial Sloan Kettering Cancer Center, New York, New York 10065, USA
    Nature 464:427-30. 2010
    ..In agreement with this prediction, RAF inhibitors do not inhibit ERK signalling in cells that coexpress BRAF(V600E) and mutant RAS...
  12. ncbi Mitochondria primed by death signals determine cellular addiction to antiapoptotic BCL-2 family members
    Michael Certo
    Department of Medical Oncology, Dana Farber Cancer Institute, 44 Binney Street, Boston, Massachusetts 02115, USA
    Cancer Cell 9:351-65. 2006
    ..Our data allow us to distinguish a cellular state we call "primed for death," which can be determined by BH3 profiling and which correlates with dependence on antiapoptotic family members for survival...
  13. ncbi RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth
    Georgia Hatzivassiliou
    Genentech, South San Francisco, California 94080, USA
    Nature 464:431-5. 2010
    ..Furthermore, this work provides new insights into the therapeutic use of ATP-competitive RAF inhibitors...
  14. pmc Dissecting therapeutic resistance to RAF inhibition in melanoma by tumor genomic profiling
    Nikhil Wagle
    Department of Medical Oncology, Dana Farber Cancer Institute, 44 Binney St, D1542, Boston, MA, USA
    J Clin Oncol 29:3085-96. 2011
    ..These results provide an instructive framework for assessing mechanisms of acquired resistance to kinase inhibition and illustrate the use of emerging technologies in a manner that may accelerate personalized cancer medicine...
  15. pmc PTEN loss confers BRAF inhibitor resistance to melanoma cells through the suppression of BIM expression
    Kim H T Paraiso
    Department of Molecular Oncology, The Moffitt Cancer Center and Research Institute, University of South Florida College of Medicine, Tampa, Florida, USA
    Cancer Res 71:2750-60. 2011
    ..In conclusion, we have shown for the first time that loss of PTEN contributes to intrinsic BRAF inhibitor resistance via the suppression of BIM-mediated apoptosis...
  16. pmc Melanoma whole-exome sequencing identifies (V600E)B-RAF amplification-mediated acquired B-RAF inhibitor resistance
    Hubing Shi
    Division of Dermatology, Department of Medicine, University of California, Los Angeles, 52 121 CHS, 10833 Le Conte Avenue, California 90095 1750, USA
    Nat Commun 3:724. 2012
    ..Thus, alternative clinical strategies may potentially overcome distinct modes of extracellular signal-regulated kinase reactivation underlying acquired B-RAF inhibitor resistance in melanoma...
  17. ncbi Pazopanib for metastatic soft-tissue sarcoma (PALETTE): a randomised, double-blind, placebo-controlled phase 3 trial
    Winette T A van der Graaf
    Radboud University Medical Centre, Department of Medical Oncology, Nijmegen, Netherlands
    Lancet 379:1879-86. 2012
    ..We investigated the effect of pazopanib on progression-free survival in patients with metastatic non-adipocytic soft-tissue sarcoma after failure of standard chemotherapy...
  18. pmc Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity
    James Tsai
    Plexxikon, Inc, 91 Bolivar Drive, Berkeley, CA 94710, USA
    Proc Natl Acad Sci U S A 105:3041-6. 2008
    ....
  19. pmc Bcl-2 inhibitors: targeting mitochondrial apoptotic pathways in cancer therapy
    Min H Kang
    Cancer Center and the Department of Cell Biology and Biochemistry, School of Medicine, Texas Tech University Health Sciences Center, Lubbock, Texas 79430, USA
    Clin Cancer Res 15:1126-32. 2009
    ..Here, we review the role of the Bcl-2 family in apoptotic pathways and those agents that are known and/or designed to inhibit the anti-apoptotic Bcl-2 family of proteins...
  20. pmc EGFR-mediated re-activation of MAPK signaling contributes to insensitivity of BRAF mutant colorectal cancers to RAF inhibition with vemurafenib
    Ryan B Corcoran
    Massachusetts General Hospital Cancer Center, Boston, MA 02129, USA
    Cancer Discov 2:227-35. 2012
    ..These findings support evaluation of combined RAF and EGFR inhibition in BRAF mutant CRC patients...
  21. pmc RAS mutations are associated with the development of cutaneous squamous cell tumors in patients treated with RAF inhibitors
    Patrick A Oberholzer
    Broad Institute of Massachusetts Institute of Technology, Cambridge, USA
    J Clin Oncol 30:316-21. 2012
    ..The potential of these agents to promote secondary malignancies is concerning. We analyzed cSCC and KA lesions for genetic mutations in an attempt to identify an underlying mechanism for their formation...
  22. ncbi Bosentan therapy for pulmonary arterial hypertension
    Lewis J Rubin
    Division of Pulmonary and Critical Care Medicine, University of California at San Diego, La Jolla 92037 1330, USA
    N Engl J Med 346:896-903. 2002
    ..The present trial investigated the effect of bosentan on exercise capacity in a larger number of patients and compared two doses...
  23. ncbi Rosuvastatin in older patients with systolic heart failure
    John Kjekshus
    Department of Cardiology, University of Oslo, Rikshospitalet University Hospital, Oslo, Norway
    N Engl J Med 357:2248-61. 2007
    ..Patients with systolic heart failure have generally been excluded from statin trials. Acute coronary events are uncommon in this population, and statins have theoretical risks in these patients...
  24. ncbi Functional expression and mutations of c-Met and its therapeutic inhibition with SU11274 and small interfering RNA in non-small cell lung cancer
    Patrick C Ma
    Section of Hematology Oncology, Department of Medicine, University of Chicago Medical Center, Pritzker School of Medicine, Chicago, Illinois, USA
    Cancer Res 65:1479-88. 2005
    ..These results indicate that c-Met inhibition will be an important therapeutic strategy against NSCLC to improve its clinical outcome...
  25. pmc The RAF inhibitor PLX4032 inhibits ERK signaling and tumor cell proliferation in a V600E BRAF-selective manner
    Eric W Joseph
    Weill Cornell Graduate School of Medical Sciences, New York, NY 10065, USA
    Proc Natl Acad Sci U S A 107:14903-8. 2010
    ..This selectivity may lead to a broader therapeutic index and help explain the greater antitumor activity observed with this drug than with MEK inhibitors...
  26. pmc Recovery of phospho-ERK activity allows melanoma cells to escape from BRAF inhibitor therapy
    K H T Paraiso
    Department of Molecular Oncology, The Moffitt Cancer Center and Research Institute, 12902 Magnolia Drive, Tampa, FL 33612, USA
    Br J Cancer 102:1724-30. 2010
    ..Resistance to BRAF inhibitors is an emerging problem in the melanoma field. Strategies to prevent and overcome resistance are urgently required...
  27. ncbi Programmed anuclear cell death delimits platelet life span
    Kylie D Mason
    Molecular Genetics of Cancer Division, The Walter and Eliza Hall Institute of Medical Research, Parkville, Victoria 3050, Australia
    Cell 128:1173-86. 2007
    ....
  28. ncbi Activity of vincristine, L-ASP, and dexamethasone against acute lymphoblastic leukemia is enhanced by the BH3-mimetic ABT-737 in vitro and in vivo
    Min H Kang
    Developmental Therapeutics Program, Childrens Hospital Los Angeles and University of Southern California Institute for Pediatric Clinical Research, Los Angeles, CA 90027, USA
    Blood 110:2057-66. 2007
    ..Combining VXL with a BH3-mimetic warrants clinical investigation in ALL at relapse and potentially in chemotherapy-resistant ALL subgroups...
  29. pmc Navitoclax, a targeted high-affinity inhibitor of BCL-2, in lymphoid malignancies: a phase 1 dose-escalation study of safety, pharmacokinetics, pharmacodynamics, and antitumour activity
    Wyndham H Wilson
    National Cancer Institute, National Institutes of Health, Bethesda, MD, USA
    Lancet Oncol 11:1149-59. 2010
    ..We aimed to assess the safety and antitumour activity of navitoclax in patients with lymphoid tumours, and establish the drug's pharmacokinetic and pharmacodynamic profiles...
  30. ncbi Stimulation of lipogenesis by pharmacological activation of the liver X receptor leads to production of large, triglyceride-rich very low density lipoprotein particles
    Aldo Grefhorst
    Laboratory of Pediatrics, Center for Liver, Digestive and Metabolic Diseases, University Hospital Groningen, Hanzeplein 1, 9713 RB Groningen, The Netherlands
    J Biol Chem 277:34182-90. 2002
    ..We conclude that, in addition to raising high density lipoprotein cholesterol concentrations, pharmacological LXR activation in mice leads to development of hepatic steatosis and secretion of atherogenic, large TG-rich VLDL particles...
  31. pmc The HSP90 inhibitor XL888 overcomes BRAF inhibitor resistance mediated through diverse mechanisms
    Kim H T Paraiso
    The Department of Molecular Oncology, The Moffitt Cancer Center and Research Institute, Tampa, Florida, USA
    Clin Cancer Res 18:2502-14. 2012
    ..The clinical use of BRAF inhibitors is being hampered by the acquisition of drug resistance. This study shows the potential therapeutic use of the HSP90 inhibitor (XL888) in six different models of vemurafenib resistance...
  32. pmc Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma
    Gideon Bollag
    Plexxikon Inc, 91 Bolivar Drive, Berkeley, California 94710, USA
    Nature 467:596-9. 2010
    ..These data demonstrate that BRAF-mutant melanomas are highly dependent on B-RAF kinase activity...
  33. pmc Bcl-2, Bcl-x(L), and Bcl-w are not equivalent targets of ABT-737 and navitoclax (ABT-263) in lymphoid and leukemic cells
    Delphine Merino
    The Walter and Eliza Hall Institute of Medical Research, Parkville, Australia
    Blood 119:5807-16. 2012
    ..These results have profound implications for how BH3-mimetics induce apoptosis and how the use of these compounds can be optimized for treating lymphoid malignancies...
  34. pmc Acquired resistance to ABT-737 in lymphoma cells that up-regulate MCL-1 and BFL-1
    Derek Yecies
    Department of Medical Oncology, Dana Farber Cancer Institute, Boston, MA, USA
    Blood 115:3304-13. 2010
    ..This dynamic increase suggests a novel mechanism whereby modulation of antiapoptotic protein function communicates with nuclear transcriptional machinery...
  35. pmc Combinatorial treatments that overcome PDGFRβ-driven resistance of melanoma cells to V600EB-RAF inhibition
    Hubing Shi
    Department of Medicine, David Geffen School of Medicine, University of California, Los Angeles, CA, USA
    Cancer Res 71:5067-74. 2011
    ..Together, our findings offer a rational strategy to guide clinical testing in preidentified subsets of patients who relapse during treatment with (V600E)B-RAF inhibitors...
  36. ncbi BH3 profiling identifies three distinct classes of apoptotic blocks to predict response to ABT-737 and conventional chemotherapeutic agents
    Jing Deng
    Department of Medical Oncology, Dana Farber Cancer Institute, Boston, MA 02115, USA
    Cancer Cell 12:171-85. 2007
    ..BCL-2 dependence correlates with high levels of proapoptotic BIM sequestered by BCL-2. Strikingly, BH3 profiling can also predict sensitivity to conventional chemotherapeutic agents like etoposide, vincristine, and adriamycin...
  37. ncbi Celecoxib for the prevention of colorectal adenomatous polyps
    Nadir Arber
    Integrated Cancer Prevention Center, Tel Aviv Sourasky Medical Center, and Sackler School of Medicine, Tel Aviv University, Tel Aviv, Israel
    N Engl J Med 355:885-95. 2006
    ..Overexpression of cyclooxygenase 2 (COX-2) has been associated with colorectal adenomatous polyps and cancer, prompting researchers to propose its inhibition as a chemopreventive intervention...
  38. ncbi The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer
    Adrian J Folkes
    Piramed Pharma, 957 Buckingham Avenue, Slough, Berks SL1 4NL, United Kingdom
    J Med Chem 51:5522-32. 2008
    ..This work resulted in the discovery of 17, GDC-0941, which is a potent, selective, orally bioavailable inhibitor of PI3K and is currently being evaluated in human clinical trials for the treatment of cancer...
  39. ncbi Mechanisms of apoptosis sensitivity and resistance to the BH3 mimetic ABT-737 in acute myeloid leukemia
    Marina Konopleva
    Section of Molecular Hematology and Therapy, Department of Blood and Marrow Transplantation, The University of Texas M D Anderson Cancer Center, Houston, Texas 77030, USA
    Cancer Cell 10:375-88. 2006
    ..These data suggest that ABT-737 could be a highly effective antileukemia agent when the mechanisms of resistance identified here are considered...
  40. pmc Incidence of the V600K mutation among melanoma patients with BRAF mutations, and potential therapeutic response to the specific BRAF inhibitor PLX4032
    Jill C Rubinstein
    Department of Dermatology, Yale University School of Medicine, New Haven, CT 06520, USA
    J Transl Med 8:67. 2010
    ..Here we present evidence that a patient bearing the BRAF V600K mutation responded remarkably to PLX4032, suggesting that clinical trials should include all patients with activating BRAF V600E/K mutations...
  41. ncbi Combinations of BRAF, MEK, and PI3K/mTOR inhibitors overcome acquired resistance to the BRAF inhibitor GSK2118436 dabrafenib, mediated by NRAS or MEK mutations
    James G Greger
    Oncology R and D Translational Research, GlaxoSmithKline, Collegeville, Pennsylvania, USA
    Mol Cancer Ther 11:909-20. 2012
    ..In addition, these resistant clones respond to the combination of GSK2126458 with GSK2118436 or GSK1120212. Clinical trials are ongoing or planned to test these combinations...
  42. ncbi TAK-242 (resatorvid), a small-molecule inhibitor of Toll-like receptor (TLR) 4 signaling, binds selectively to TLR4 and interferes with interactions between TLR4 and its adaptor molecules
    Naoko Matsunaga
    Pharmacology Research Laboratories, Pharmaceutical Research Division, Takeda Pharmaceutical Company Limited, Osaka, Japan
    Mol Pharmacol 79:34-41. 2011
    ..This work proposes a novel paradigm of a small molecule capable of disrupting protein-protein interactions...
  43. pmc N-myristoyltransferase inhibitors as new leads to treat sleeping sickness
    Julie A Frearson
    Drug Discovery Unit, Division of Biological Chemistry and Drug Discovery, University of Dundee, Dundee DD1 5EH, UK
    Nature 464:728-32. 2010
    ..Our studies validate T. brucei N-myristoyltransferase as a promising therapeutic target for human African trypanosomiasis...
  44. ncbi Celecoxib versus omeprazole and diclofenac in patients with osteoarthritis and rheumatoid arthritis (CONDOR): a randomised trial
    Francis K L Chan
    Chinese University of Hong Kong, Prince of Wales Hospital, Hong Kong SAR, China
    Lancet 376:173-9. 2010
    ..We aimed to compare risk of gastrointestinal events associated with celecoxib versus diclofenac slow release plus omeprazole...
  45. pmc Efficacy of pazopanib in progressive, radioiodine-refractory, metastatic differentiated thyroid cancers: results of a phase 2 consortium study
    Keith C Bible
    Division of Medical Oncology, Mayo Clinic, Rochester, MN, USA
    Lancet Oncol 11:962-72. 2010
    ..We investigated the safety and efficacy of pazopanib...
  46. ncbi Substantial susceptibility of chronic lymphocytic leukemia to BCL2 inhibition: results of a phase I study of navitoclax in patients with relapsed or refractory disease
    Andrew W Roberts
    MBBS, Department of Clinical Haematology and BMT, The Royal Melbourne Hospital, 2 Centre, Grattan St, Parkville 3050, Victoria, Australia
    J Clin Oncol 30:488-96. 2012
    ..A phase I trial in patients with CLL was conducted to evaluate the safety, pharmacokinetics, and biologic activity of oral navitoclax...
  47. ncbi Analytical performance of a real-time PCR-based assay for V600 mutations in the BRAF gene, used as the companion diagnostic test for the novel BRAF inhibitor vemurafenib in metastatic melanoma
    Harkanwal Halait
    Roche Molecular Diagnostics, Pleasanton, CA 94588, USA
    Diagn Mol Pathol 21:1-8. 2012
    ..A simple 1:2 dilution resulted in a valid test result of 76% in such cases. The cobas test is a reproducible assay that detects some non-V600E mutations and is more accurate than direct sequencing in detecting BRAFV600E...
  48. ncbi Phase II proof-of-concept study of pazopanib monotherapy in treatment-naive patients with stage I/II resectable non-small-cell lung cancer
    Nasser Altorki
    Weill Medical College, Cornell University, 525 East 68th St, New York, NY 10021, USA
    J Clin Oncol 28:3131-7. 2010
    ..This proof-of-concept study examined safety and efficacy of short-term, preoperative pazopanib monotherapy in patients with operable stage I/II NSCLC...
  49. ncbi RG7204 (PLX4032), a selective BRAFV600E inhibitor, displays potent antitumor activity in preclinical melanoma models
    Hong Yang
    Discovery Oncology, Hoffmann La Roche, Inc, Nutley, New Jersey, USA
    Cancer Res 70:5518-27. 2010
    ..There was no toxicity observed in any dose group in any of the in vivo models tested. Our findings offer evidence of the potent antitumor activity of RG7204 against melanomas harboring the mutant BRAF(V600E) gene...
  50. ncbi Efficacy of TG101348, a selective JAK2 inhibitor, in treatment of a murine model of JAK2V617F-induced polycythemia vera
    Gerlinde Wernig
    Division of Hematology, Department of Medicine, Brigham and Women s Hospital, Harvard Medical School, Boston, MA 02115, USA
    Cancer Cell 13:311-20. 2008
    ....
  51. pmc Bcl-xL regulates metabolic efficiency of neurons through interaction with the mitochondrial F1FO ATP synthase
    Kambiz N Alavian
    Department of Internal Medicine, Yale University, New Haven, Connecticut 06520, USA
    Nat Cell Biol 13:1224-33. 2011
    ..Our findings indicate that increased mitochondrial efficiency contributes to the enhanced synaptic efficacy found in Bcl-x(L)-expressing neurons...
  52. ncbi MEK-independent survival of B-RAFV600E melanoma cells selected for resistance to apoptosis induced by the RAF inhibitor PLX4720
    Chen Chen Jiang
    Immunology and Oncology Unit, Newcastle, New South Wales, Australia
    Clin Cancer Res 17:721-30. 2011
    ..To examine mechanisms that determine long-term responses of B-RAF(V600E) melanoma cells to B-RAF inhibitors...
  53. ncbi Bcl-2 inhibitors: small molecules with a big impact on cancer therapy
    M Vogler
    MRC Toxicology Unit, Hodgkin Building, University of Leicester, PO Box 138, Lancaster Road, Leicester LE1 9HN, UK
    Cell Death Differ 16:360-7. 2009
    ..In in vitro studies, primary cells from patients with various B-cell malignancies are exquisitely sensitive to ABT-737, exhibiting novel morphological features of apoptosis including marked outer mitochondrial membrane rupture...
  54. ncbi Different forms of cell death induced by putative BCL2 inhibitors
    M Vogler
    MRC Toxicology Unit, Hodgkin Building, University of Leicester, Leicestershire, UK
    Cell Death Differ 16:1030-9. 2009
    ....
  55. pmc Mechanisms of resistance to RAF inhibitors in melanoma
    Andrew E Aplin
    Department of Cancer Biology, Thomas Jefferson University, Philadelphia, Pennsylvania 19107, USA
    J Invest Dermatol 131:1817-20. 2011
    ..Bi-directional translational efforts are now essential to determine the mechanisms underlying acquired/secondary and intrinsic resistance to RAF inhibitors...
  56. pmc An antiapoptotic BCL-2 family expression index predicts the response of chronic lymphocytic leukemia to ABT-737
    Sayer Al-Harbi
    Department of Cancer Biology, Lerner Research Institute, Cleveland Clinic, Cleveland, OH, USA
    Blood 118:3579-90. 2011
    ..Changes after ABT-737 treatment included increased expression of BFL-1 and BCL-B that may contribute to treatment resistance. This study defines a highly significant BCL-2 expression index for predicting the response of CLL to ABT-737...
  57. pmc Mimicking the BH3 domain to kill cancer cells
    T Ní Chonghaile
    Department of Medical Oncology, Dana Farber Cancer Institute, Boston, MA 02115, USA
    Oncogene 27:S149-57. 2008
    ..Thus, the BH3 mimetics are a new class of cancer drugs that specifically target a mechanism of cancer cell survival to selectively kill cancer cells...
  58. ncbi The potential of celecoxib-loaded hydroxyapatite-chitosan nanocomposite for the treatment of colon cancer
    P Venkatesan
    School of Medical Science and Technology, Indian Institute of Technology, Kharagpur 721302, India
    Biomaterials 32:3794-806. 2011
    ..The present study indicates a promising, effective and safe means of using celecoxib, and potentially other therapeutic agents for colon cancer therapy...
  59. ncbi Comparison of the efficacy and safety of rosuvastatin versus atorvastatin, simvastatin, and pravastatin across doses (STELLAR* Trial)
    Peter H Jones
    Baylor College of Medicine, 6565 Fannin Avenue, A 601, Houston, TX 77030, USA
    Am J Cardiol 92:152-60. 2003
    ..0 mmol/L was achieved by 79% to 92% in rosuvastatin groups compared with 52% to 81% in atorvastatin groups. Drug tolerability was similar across treatments...
  60. pmc Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941
    Florence I Raynaud
    Cancer Research UK Centre for Cancer Therapeutics, The Institute of Cancer Research, Sutton, Surrey, UK
    Mol Cancer Ther 8:1725-38. 2009
    ..Together, these data support the development of GDC-0941 as a potent, orally bioavailable inhibitor of phosphatidylinositide 3-kinase. GDC-0941 has recently entered phase I clinical trials...
  61. pmc Therapeutic efficacy of ABT-737, a selective inhibitor of BCL-2, in small cell lung cancer
    Christine L Hann
    Sidney Kimmel Comprehensive Cancer Center, Johns Hopkins University, Baltimore, MD 21231, USA
    Cancer Res 68:2321-8. 2008
    ..Taken together, these data have specific implications for the clinical development of Bcl-2 inhibitors for SCLC and broader implications for the testing of novel anticancer strategies in relevant preclinical models...
  62. pmc PLX4032, a selective BRAF(V600E) kinase inhibitor, activates the ERK pathway and enhances cell migration and proliferation of BRAF melanoma cells
    Ruth Halaban
    Department of Dermatology, Yale University School of Medicine, New Haven, CT, USA
    Pigment Cell Melanoma Res 23:190-200. 2010
    ..The results suggest that the drug can confer an advantage to BRAF(WT) primary and metastatic tumor cells in vivo and provide markers for monitoring clinical responses...
  63. pmc Chronic lymphocytic leukemia requires BCL2 to sequester prodeath BIM, explaining sensitivity to BCL2 antagonist ABT-737
    Victoria Del Gaizo Moore
    Department of Medical Oncology, Dana Farber Cancer Institute, Boston, Massachusetts 02115, USA
    J Clin Invest 117:112-21. 2007
    ..Indeed, activator BH3-only occupation of BCL2 may prime cancer cells for death, offering a potential explanation for the marked chemosensitivity of certain cancers that express abundant BCL2, such as CLL and follicular lymphoma...
  64. ncbi Alterations in the Noxa/Mcl-1 axis determine sensitivity of small cell lung cancer to the BH3 mimetic ABT-737
    Paula Hauck
    Department of Medicine, Virginia Commonwealth Universityh and McGuire Veterans Affairs Medical Center 111K, 1201 Broad Rock Boulevard, Richmond, VA 23249, USA
    Mol Cancer Ther 8:883-92. 2009
    ..These results indicate that Noxa expression is the critical determinant of ABT-737 sensitivity and loss of Noxa-mediated regulation of Mcl-1 expression may be an important feature of small cell lung cancer biology...
  65. ncbi Cyclooxygenase-2 inhibition by celecoxib reduces proliferation and induces apoptosis in angiogenic endothelial cells in vivo
    Kathleen M Leahy
    Pharmacia, Mail Zone AA4C, 700 Chesterfield Parkway, Chesterfield, Missouri 63017, USA
    Cancer Res 62:625-31. 2002
    ..2-3.0-fold) in response to celecoxib. Thus, the antitumor activity of celecoxib may be attributable, at least in part, to a direct effect on host stromal elements, such as the angiogenic vasculature...
  66. pmc Akt3-mediated resistance to apoptosis in B-RAF-targeted melanoma cells
    Yongping Shao
    Department of Cancer Biology and Kimmel Cancer Center, Thomas Jefferson University, Philadelphia, Pennsylvania 19107, USA
    Cancer Res 70:6670-81. 2010
    ..These findings delineate how mutant B-RAF protects melanoma cells from apoptosis and provide insight into possible resistance mechanisms to B-RAF inhibitors...
  67. ncbi The endothelin antagonist bosentan inhibits the canalicular bile salt export pump: a potential mechanism for hepatic adverse reactions
    K Fattinger
    Division of Clinical Pharmacology and Toxicology, Department of Medicine, University Hospital, Zurich, Switzerland
    Clin Pharmacol Ther 69:223-31. 2001
    ..In this study we investigated whether inhibition of the hepatocanalicular bile salt export pump (rodents, Bsep; humans, BSEP ABCB11) could account for bosentan-induced liver injury...
  68. ncbi A Phase II, open-label study evaluating pazopanib in patients with recurrent ovarian cancer
    Michael Friedlander
    Prince of Wales Hospital, Randwick, Sydney, Australia
    Gynecol Oncol 119:32-7. 2010
    ..This phase II, open-label study evaluated oral pazopanib monotherapy in patients with low-volume recurrent ovarian cancer...
  69. ncbi The Bcl-xL inhibitor, ABT-737, efficiently induces apoptosis and suppresses growth of hepatoma cells in combination with sorafenib
    Hayato Hikita
    Department of Gastroenterology and Hepatology, Osaka University Graduate School of Medicine, Suita, Osaka, Japan
    Hepatology 52:1310-21. 2010
    ..Sorafenib, not alone but in combination with ABT-737, efficiently induced apoptosis in hepatoma cells. This combination also led to stronger suppression of xenograft tumors than sorafenib alone...
  70. ncbi Concurrent up-regulation of BCL-XL and BCL2A1 induces approximately 1000-fold resistance to ABT-737 in chronic lymphocytic leukemia
    Meike Vogler
    Medical Research Council Toxicology Unit, University of Leicester, Leicester, United Kingdom
    Blood 113:4403-13. 2009
    ....
  71. ncbi Efficacy of darunavir/ritonavir maintenance monotherapy in patients with HIV-1 viral suppression: a randomized open-label, noninferiority trial, MONOI-ANRS 136
    Christine Katlama
    INSERM UMR S 943 and University Pierre and Marie Curie UPMC Paris VI, Paris, France
    AIDS 24:2365-74. 2010
    ..Darunavir/ritonavir (darunavir/r) maintenance strategy, in patients with suppressed HIV RNA viremia, is a potential long-term strategy to avoid nucleoside analogue toxicities and to reduce costs...
  72. ncbi Upregulation of vascular endothelial growth factor by cobalt chloride-simulated hypoxia is mediated by persistent induction of cyclooxygenase-2 in a metastatic human prostate cancer cell line
    X H Liu
    Department of Medicine, Mount Sinai School of Medicine, New York, NY 10029, USA
    Clin Exp Metastasis 17:687-94. 1999
    ....
  73. pmc Transcriptional activation of the NF-kappaB p65 subunit by mitogen- and stress-activated protein kinase-1 (MSK1)
    Linda Vermeulen
    Department of Molecular Biology, University of Gent VIB, K L Ledeganckstraat 35, B 9000 Gent, Belgium
    EMBO J 22:1313-24. 2003
    ..This effect represents, together with phosphorylation of nucleosome components such as histone H3, an essential step leading to selective transcriptional activation of NF-kappaB-dependent gene expression...
  74. ncbi Celecoxib: a review of its use for symptomatic relief in the treatment of osteoarthritis, rheumatoid arthritis and ankylosing spondylitis
    Paul L McCormack
    Adis, a Wolters Kluwer Business, Auckland, New Zealand
    Drugs 71:2457-89. 2011
    ....
  75. pmc The small molecule Hesperadin reveals a role for Aurora B in correcting kinetochore-microtubule attachment and in maintaining the spindle assembly checkpoint
    Silke Hauf
    Research Institute of Molecular Pathology, Dr Bohr Gasse 7, 1030 Vienna, Austria
    J Cell Biol 161:281-94. 2003
    ..Together, our data suggest that Aurora B is required to generate unattached kinetochores on monooriented chromosomes, which in turn could promote bipolar attachment as well as maintain checkpoint signaling...
  76. ncbi Carbonic anhydrase inhibitors. Inhibition of the transmembrane isozyme XII with sulfonamides-a new target for the design of antitumor and antiglaucoma drugs?
    Daniela Vullo
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino Firenze, Italy
    Bioorg Med Chem Lett 15:963-9. 2005
    ..2.1.1), isozyme XII (hCA XII), has been investigated with a series of sulfonamides, including some clinically used derivatives (acetazolamide, methazolamide, ethoxzolamide, dichlorophenamide, ..
  77. ncbi TAK-242 selectively suppresses Toll-like receptor 4-signaling mediated by the intracellular domain
    Tomohiro Kawamoto
    Pharmaceutical Research Division, Takeda Pharmaceutical Company Limited, Osaka 532 8686, Japan
    Eur J Pharmacol 584:40-8. 2008
    ..TAK-242 is therefore a selective inhibitor of signaling from the intracellular domain of TLR4 and represents a novel therapeutic approach to the treatment of TLR4-mediated diseases...
  78. ncbi Pazopanib, a multikinase angiogenesis inhibitor, in patients with relapsed or refractory advanced soft tissue sarcoma: a phase II study from the European organisation for research and treatment of cancer-soft tissue and bone sarcoma group (EORTC study 620
    Stefan Sleijfer
    Dept of Medical Oncology, Erasmus University Medical Center, Daniel den Hoed Cancer Center, Groene Hilledijk 301, 3075 EA Rotterdam, The Netherlands
    J Clin Oncol 27:3126-32. 2009
    ..7%). CONCLUSION Pazopanib is well tolerated in patients with relapsed, advanced STS and demonstrates interesting activity that warrants additional study in patients with leiomyosarcomas, synovial sarcomas, and other STS types...
  79. ncbi Dual PI3K/AKT/mTOR inhibitor BEZ235 synergistically enhances the activity of JAK2 inhibitor against cultured and primary human myeloproliferative neoplasm cells
    Warren Fiskus
    The University of Kansas Cancer Center, Kansas City, KS, USA
    Mol Cancer Ther 12:577-88. 2013
    ..These findings create a compelling rationale to determine the in vivo activity of dual PI3K/mTOR inhibitors in combination with JAK inhibitors against myelofibrosis HPCs...
  80. ncbi A randomised, controlled trial of bosentan in severe COPD
    D Stolz
    Clinic of Pulmonary Medicine and Respiratory Cell Research, University Hospital Basel, Petersgraben 4, CH 4031 Basel, Switzerland
    Eur Respir J 32:619-28. 2008
    ....
  81. ncbi Imaging of CA IX with fluorescent labelled sulfonamides distinguishes hypoxic and (re)-oxygenated cells in a xenograft tumour model
    Ludwig Dubois
    Maastricht Radiation Oncology MaastRO Lab, GROW School for Oncology and Developmental Biology, University of Maastricht, The Netherlands
    Radiother Oncol 92:423-8. 2009
    Carbonic anhydrase (CA) IX is suggested to be an endogenous marker of hypoxia. Fluorescent sulfonamides with a high affinity for CA IX (CAI) have been developed and shown to bind to cells only when CA IX protein was expressed and while ..
  82. ncbi c-Met is a potentially new therapeutic target for treatment of human melanoma
    Neelu Puri
    Departments of Hematology Oncology and Pathology, University of Chicago Medical Center, Chicago, Illinois 60607, USA
    Clin Cancer Res 13:2246-53. 2007
    ..In this study, we investigated the role of c-Met in melanoma biology using a novel small-molecule tyrosine kinase inhibitor SU11274 and small interfering (si) RNA against the receptor...
  83. ncbi Cardiovascular risk and inhibition of cyclooxygenase: a systematic review of the observational studies of selective and nonselective inhibitors of cyclooxygenase 2
    Patricia McGettigan
    Discipline of Clinical Pharmacology, School of Medicine and Public Health, The University of Newcastle, New South Wales, Australia
    JAMA 296:1633-44. 2006
    ..Regulatory agencies have provided variable advice regarding the cardiovascular risks with older nonselective NSAIDs...
  84. pmc Efficient elimination of cancer cells by deoxyglucose-ABT-263/737 combination therapy
    Ryuji Yamaguchi
    Program of Cell Death and Apoptosis, Sanford Burnham Medical Research Institute, La Jolla, California, United States of America
    PLoS ONE 6:e24102. 2011
    ....
  85. pmc Phase II, randomized, placebo-controlled trial of neoadjuvant celecoxib in men with clinically localized prostate cancer: evaluation of drug-specific biomarkers
    Emmanuel S Antonarakis
    Sidney Kimmel Comprehensive Cancer Center, Johns Hopkins School of Medicine, Baltimore, MD 21231, USA
    J Clin Oncol 27:4986-93. 2009
    ..We conducted a randomized, double-blind trial to examine the effect of celecoxib on drug-specific biomarkers from prostate tissue obtained at prostatectomy...
  86. ncbi Phase I trial of pazopanib in patients with advanced cancer
    Herbert I Hurwitz
    Duke University Medical Center, Durham, North Carolina, USA
    Clin Cancer Res 15:4220-7. 2009
    ....
  87. pmc Rosuvastatin for primary prevention in patients with European systematic coronary risk evaluation risk ≥ 5% or Framingham risk >20%: post hoc analyses of the JUPITER trial requested by European health authorities
    Wolfgang Koenig
    Department of Internal Medicine II Cardiology, University of Ulm Medical Center, Albert Einstein Allee 23, Ulm, Germany
    Eur Heart J 32:75-83. 2011
    ..However, as these are post hoc analyses, data describing these subgroups have not previously been available to the clinical community...
  88. ncbi Pharmacokinetic-pharmacodynamic correlation from mouse to human with pazopanib, a multikinase angiogenesis inhibitor with potent antitumor and antiangiogenic activity
    Rakesh Kumar
    Oncology Biology, GlaxoSmithKline, 1250 South Collegeville Road, UP1450, Collegeville, PA 19426, USA
    Mol Cancer Ther 6:2012-21. 2007
    ..Furthermore, the steady-state concentration of pazopanib determined from preclinical activity showed a strong correlation with the pharmacodynamic effects and antitumor activity in the phase I clinical trial...
  89. ncbi Once-daily darunavir/ritonavir vs. lopinavir/ritonavir in treatment-naive, HIV-1-infected patients: 96-week analysis
    Anthony M Mills
    Private Practice, Los Angeles, USA
    AIDS 23:1679-88. 2009
    ..Present 96-week data from ongoing ARTEMIS (AntiRetroviral Therapy with TMC114 ExaMined In Naive Subjects) trial...
  90. pmc A randomized trial of rosuvastatin in the prevention of venous thromboembolism
    Robert J Glynn
    Division of Preventive Medicine, Brigham and Women s Hospital, Harvard Medical School, Boston, MA 02215, USA
    N Engl J Med 360:1851-61. 2009
    ..Observational studies have yielded variable estimates of the effect of statin therapy on the risk of venous thromboembolism, and evidence from randomized trials is lacking...
  91. ncbi Defining the target specificity of ABT-737 and synergistic antitumor activities in combination with histone deacetylase inhibitors
    Kate F Whitecross
    Cancer Immunology Program, The Peter MacCallum Cancer Centre, Trescowthick Research Laboratories, East Melbourne, Australia
    Blood 113:1982-91. 2009
    ..Our studies provide important preclinical data on the binding specificity of ABT-737 and its usefulness against primary hematologic malignancies when used as a single agent and in combination with HDACi...
  92. pmc The benzenesulfoamide T0901317 [N-(2,2,2-trifluoroethyl)-N-[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]-benzenesulfonamide] is a novel retinoic acid receptor-related orphan receptor-alpha/gamma inverse agonist
    Naresh Kumar
    The Scripps Research Institute, Jupiter, FL 33458, USA
    Mol Pharmacol 77:228-36. 2010
    ..More importantly, our results demonstrate that small molecules can be used to target the RORs for therapeutic intervention in metabolic and immune disorders...
  93. ncbi TG101209, a small molecule JAK2-selective kinase inhibitor potently inhibits myeloproliferative disorder-associated JAK2V617F and MPLW515L/K mutations
    A Pardanani
    Division of Hematology, Mayo Clinic, Rochester, MN 55905, USA
    Leukemia 21:1658-68. 2007
    ..Therapeutic efficacy of TG101209 was demonstrated in a nude mouse model. Furthermore, TG101209 suppressed growth of hematopoietic colonies from primary progenitor cells harboring JAK2V617F or MPL515 mutations...
  94. ncbi Effect of rosuvastatin on coronary atheroma in stable coronary artery disease: multicenter coronary atherosclerosis study measuring effects of rosuvastatin using intravascular ultrasound in Japanese subjects (COSMOS)
    Tadateru Takayama
    Division of Cardiology, Nihon University School of Medicine, Tokyo, Japan
    Circ J 73:2110-7. 2009
    ..The effect of rosuvastatin on plaque volume in patients with stable coronary artery disease (CAD), including those receiving prior lipid-lowering therapy, was examined in the present study...
  95. ncbi Phase II trial of celecoxib in prostate-specific antigen recurrent prostate cancer after definitive radiation therapy or radical prostatectomy
    Raj S Pruthi
    Division of Urologic Surgery, Department of Biostatistics, and Lineberger Comprehensive Cancer Center, The University of North Carolina at Chapel Hill, Chapel Hill, North Carolina, USA
    Clin Cancer Res 12:2172-7. 2006
    ..However, human trials are absent. This study evaluated the efficacy of the COX-2 inhibitor celecoxib in prostate-specific antigen (PSA) recurrent prostate cancer after radiation therapy (X-ray therapy or XRT) or radical prostatectomy...
  96. ncbi Apoptosis-based treatment of glioblastomas with ABT-737, a novel small molecule inhibitor of Bcl-2 family proteins
    K E Tagscherer
    Molecular Neuro Oncology, German Cancer Research Center, Heidelberg, Germany
    Oncogene 27:6646-56. 2008
    ..As the resistance of glioma stem cells was associated with high Mcl-1 expression levels, ABT-737 treatment combined with downregulation of Mcl-1 could represent a promising novel approach in glioblastoma treatment...
  97. pmc BCL-2 dependence and ABT-737 sensitivity in acute lymphoblastic leukemia
    Victoria Del Gaizo Moore
    Department of Medical Oncology, Dana Farber Cancer Institute, Boston, MA 02115, USA
    Blood 111:2300-9. 2008
    ..The ALL cells studied exhibit BCL-2 dependence, supporting clinical trials of BCL-2 antagonists in ALL as single agents or combination therapies...
  98. ncbi Maximal COX-2 immunostaining and clinical response to celecoxib and interferon alpha therapy in metastatic renal cell carcinoma
    Brian I Rini
    Department of Hematology and Oncology, Cleveland Clinic, Taussig Cancer Center, Cleveland, Ohio 44195, USA
    Cancer 106:566-75. 2006
    ..Based on potential additive or synergistic antitumor effects, interferon-alpha (IFNalpha) and celecoxib, an oral COX-2 inhibitor, were given to metastatic RCC patients in a Phase II trial...
  99. pmc Differential sensitivity of melanoma cell lines with BRAFV600E mutation to the specific Raf inhibitor PLX4032
    Jonas N Søndergaard
    Department of Medicine, Division of Hematology Oncology, University of California Los Angeles, Los Angeles, CA, USA
    J Transl Med 8:39. 2010
    ..In conclusion, BRAFV600E mutant melanoma cell lines displayed a range of sensitivities to PLX4032 and metabolic imaging using PET probes can be used to assess sensitivity...
  100. pmc Combined Bcl-2/mammalian target of rapamycin inhibition leads to enhanced radiosensitization via induction of apoptosis and autophagy in non-small cell lung tumor xenograft model
    Kwang Woon Kim
    Department of Radiation Oncology, Vanderbilt Ingram Cancer Center, Vanderbilt University School of Medicine, Nashville, Tennessee 37232 5671, USA
    Clin Cancer Res 15:6096-105. 2009
    ..Radiotherapy has a central role in the treatment of non-small cell lung cancer. Effectiveness of this modality, however, is often limited as resistance results from defects in cell death...
  101. ncbi Efficacy and safety of ABT-335 (fenofibric acid) in combination with rosuvastatin in patients with mixed dyslipidemia: a phase 3 study
    Peter H Jones
    Baylor College of Medicine, Houston, TX 77030, USA
    Atherosclerosis 204:208-15. 2009
    ..To evaluate a new formulation of fenofibric acid (ABT-335) co-administered with 2 doses of rosuvastatin in patients with mixed dyslipidemia...

Research Grants64

  1. ELECTRON MONOCHROMATOR TIME-OF-FIGHT MASS SPECTROMETER
    Max Deinzer; Fiscal Year: 2002
    ..Electron attachment to several classes of electrophilic compounds including organophosphates, sulfonamides, dinitro [2,2]para- cyclophane, aliphatic ketones, haloethenes, vinyl chloride and chloroacetaldehyde will be ..
  2. Multigenerational FamIlial and Environmental Risk for Autism (MINERvA) Network
    Abraham Reichenberg; Fiscal Year: 2013
    ..e., sulfonamides and Trimethoprim...
  3. New Strategies and Screening Methods for Metalloproteinase Inhibition
    Seth M Cohen; Fiscal Year: 2010
    ..Chelating sulfonamides will enhance binding to the zinc(II) metalloprotein active site, while sparing other metalloenzymes (e.g...
  4. Development of a novel drug candidate that inhibits hepatitis B virus covalently
    Haitao Guo; Fiscal Year: 2013
    ..library using an innovative cell-based cccDNA high throughput assay, two structurally related disubstituted-sulfonamides (DSS) were discovered that have dramatic inhibition of cccDNA formation by interfering with the ..
  5. TRANSITION STATE ANALYSIS OF ENZYMATIC REACTIONS
    Vern L Schramm; Fiscal Year: 2013
    ..b>Sulfonamides are p- aminobenzoate antagonists of dihydropteroate synthetase, a target for pathogenic bacteria and protozoan ..
  6. LIPOPHILIC ANTIFOLATES AND AIDS OPPORTUNISTIC INFECTIONS
    Andre Rosowsky; Fiscal Year: 2004
    ..toxicity, whereas the relatively low efficacy of TMP and PM as single agents requires them to be used with sulfonamides and other drugs that often cause intolerable side effects...
  7. PURINE BOTTLENECKS FOR THE CHEMOTHERAPY OF TOXOPLASMOSIS
    ELMER PFEFFERKORN; Fiscal Year: 1999
    ..good, prolonged treatment is often difficult because of hypersensitivity to the drugs, particularly to the sulfonamides. Thus, toxoplasmic encephalitis is a significant factor in the morbidity and mortality of AIDS patients...
  8. REACTIONS TO TRIMETHOPRIM-SULFAMETHOXAZOLE IN AIDS
    Manuel Lopez; Fiscal Year: 1990
    ..include evaluation of Type I, II, and III hypersensitivity (measurement of class specific antibodies to several sulfonamides; pyrimidines; the sulfone, dapsone; and combinations of these drugs) and of Type IV cell mediated ..
  9. METABOLIC BASIS OF SULFONAMIDE TOXICITY IN AIDS PATIENTS
    CRAIG SVENSSON; Fiscal Year: 1999
    ..Numerous studies support the hypothesis that bioactivation of sulfonamides is an initial step in the cascade of events which result in adverse drug reactions (ADR)...
  10. Mechanisms of Cutaneous Drug Reactions
    CRAIG SVENSSON; Fiscal Year: 2004
    ..Of particular interest are the delayed-type hypersensitivity reactions that occur with sulfonamides and sulfones...
  11. CARBON DIOXIDE EXCHANGES IN THE LIVER
    SUSANNA DODGSON; Fiscal Year: 1991
    ..We will determine if there are any other effects of the sulfonamides on the mitochondria...
  12. PHARMACOKINETICS OF REVERSIBLE METABOLIC SYSTEMS
    William Jusko; Fiscal Year: 1993
    ..Numerous compounds such as corticosteroids, estrogens, sulfonamides, N- oxides, sulfoxides, some acylglucuronide and disulfide conjugates, HMG- CoA reductase inhibitors, and many ..
  13. SULFONYL ANALOGUES OF SULFATES AND PHOSPHATES
    THEODORE WIDLANSKI; Fiscal Year: 1993
    ..This proposal details the synthesis of stable non-ionic oligonucleotides using sulfonates, sulfones and sulfonamides in the place of phosphate diesters...
  14. Arylation of weakly acidic sp3 hybridized C-H's
    Patrick J Walsh; Fiscal Year: 2013
    ..be applied to DCCP's of unactivated diarylmethanes, allylbenzenes, N,N-dialkylbenzylamines, sulfoxides, sulfonamides, and sulfones to generate novel arylated products...
  15. COMPARATIVE POTENCY OF NEW INHIBITORS OF ZINC HYDROLASES
    MICHAEL MATTA; Fiscal Year: 1990
    ..The inhibitor classes are the phosphonamidates I, the thionophosphonamidates II, and the sulfonamides IIII, where R1 - CH3 and NMR2 is derived from the common L amino acids...
  16. MECHANISMS OF SULFONAMIDE RESISTANCE IN E. COLI
    Brian Nichols; Fiscal Year: 1990
    ..the altered enzyme product is a sulfonamide resistant form that discriminates more effectively between PABA and sulfonamides than does the wild type enzyme...
  17. ESA, a Novel Anti-inflammation Agent
    Lurong Zhang; Fiscal Year: 2005
    ..Our preliminary studies indicate that EsA should not predispose patients to vascular events. While the leading COX2 inhibitor, Celebrex(r), has allergic cross-reactivity to sulfonamides, EsA should not.
  18. THROMBOTIC, INFLAMMATORY & GENE MARKERS OF CVD IN WOMEN
    Paul Ridker; Fiscal Year: 2002
    ....
  19. SECONDARY PREVENTION TRIAL OF VENOUS THROMBOSIS
    Paul Ridker; Fiscal Year: 2002
    ....
  20. Minimally Invasive Surgical Therapies Treatment Consort*
    Claus Roehrborn; Fiscal Year: 2005
    ..The MIST Study Group will be a blueprint for a technology assessment group applicable to other areas of urology and other medical or surgical subspecialties. ..
  21. DEVELOPMENT OF LIGAND ASSISTED ASYMMETRIC SYNTHESES
    Arun Ghosh; Fiscal Year: 2001
    ..Besides the broad range of scope and generality, this line of research will provide excellent opportunities to teach and train graduate and undergraduate students in the laboratory. ..
  22. DESIGN AND SYNTHESIS OF NONPEPTIDE PROTEASE INHIBITORS
    Arun K Ghosh; Fiscal Year: 2010
    ..This research integrates organic synthesis, protein-ligand x-ray crystallography, molecular modeling and in-depth virus and cell-biological studies to design the next generation of HIV-1 protease inhibitors. ..
  23. Overcoming DC defects in cancer patients by VEGF trap
    Jeffrey Sosman; Fiscal Year: 2005
    ..Thereby, the correlative studies described here may lead to the establishment of VEGF inhibition, VEGF Trap, specifically, as an approach to combine with and enhance cancer immunotherapy. ..
  24. Inhibition of nf-kb signaling in melanoma therapy
    Jeffrey Sosman; Fiscal Year: 2005
    ..Abstract Not Provided ..
  25. Phase I/II Study of MS-275 and 5-Azacytidine in Patients with Advanced Non-Small
    CHARLES RUDIN; Fiscal Year: 2008
    ..If successful, this approach could alter the poor prognosis of individuals with this disease. [unreadable] [unreadable] [unreadable]..
  26. MAC 1/LFA 1/P150 95 AND PMN LEUKOCYTE FUNCTION
    Christie Ballantyne; Fiscal Year: 2002
    ..3. Characterize the contribution of each CD11 integrin on the host response to common bacterial and fungal pathogens in vitro and in vivo. ..
  27. Obesity, Inflammation and Thrombosis: LOOK AHEAD
    Christie M Ballantyne; Fiscal Year: 2010
    ....
  28. Nitogen reduction and xenobiotic response
    Lauren A Trepanier; Fiscal Year: 2010
    ..The ultimate goal of these studies is to find better ways to prevent these adverse reactions. ..
  29. A pharmacogenetic and pharmacodynamic study of erlotinib
    CHARLES RUDIN; Fiscal Year: 2004
    ..Defining the basis of this toxicity could also promote the development of EGFR-directed agents that may avoid such toxicity or that may be effective in a broader spectrum of cancer patients. ..
  30. A Cell Based HTS Approach for the Discovery of New Inhibitors of RSV
    William Severson; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  31. Genetic Determinants of C-Reactive Protein
    JACQUELINE DANIK; Fiscal Year: 2008
    ..At the end of the proposed research program, Dr. Suk will have attained advanced skills in genetics and epidemiology which can then be applied to independent research in genetic epidemiology and cardiovascular disease. ..
  32. Severe Asthma From Respiratory Infections
    William W Busse; Fiscal Year: 2010
    ..These studies will provide new insights into the mechanisms of asthma, particularly severe disease, and possibilities of new approaches to treatment. ..
  33. Improving Contraceptive Effectiveness in Obese Women
    Alison B Edelman; Fiscal Year: 2010
    ..abstract_text> ..
  34. A Cell Based HTS Approach for the Discovery of New Inhibitors of the H5N1 Virus
    William Severson; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  35. Strengthening Botanical CAM Research: A Collaboration between CUNY and Columbia
    Edward Kennelly; Fiscal Year: 2007
    ..We anticipate that within a year after the end of the project period, several R21 or R01 botanically-related CAM applications will be submitted to NIH. ..
  36. PHASE I TRIALS OF ANTICANCER AGENTS
    Martin Edelman; Fiscal Year: 2002
    ....
  37. Distribution of PCB Atropisomers
    Hans Joachim Lehmler; Fiscal Year: 2008
    ..The long term career goal is to establish Dr. Lehmler as an investigator with independent research status and funding. ..
  38. Mechanisms Underlying the Cognitive Function of Sleep
    Subimal Datta; Fiscal Year: 2009
    ....
  39. Antitumor Antimitotics That Reverse Tumor Resistance
    Aleem Gangjee; Fiscal Year: 2010
    ..The study will also further define the mechanism of action of the novel series and could afford agents for clinical use. ..
  40. Selective Inhibitors of SRC Family Kinases in Neoplasia
    THOMAS SMITHGALL; Fiscal Year: 2002
    ..Combined with the in vitro assays, we hope to identify novel inhibitory activities that target specific Src kinase isoforms and oncogenic signaling pathways. ..
  41. Src Family Kinases as Molecular Targets for HIV/Nef
    THOMAS EDWARD SMITHGALL; Fiscal Year: 2010
    ..Our work is focused on the interaction of Nef with protein kinases in infected cells. Completion of these experiments will validate these Nef-kinase complexes as targets for the discovery of new anti-HIV therapeutics. ..
  42. Inhibition of Tubercular Mycothiol Pathways
    Spencer Knapp; Fiscal Year: 2004
    ..The most active compounds will be taken as leads for further analogue development and for increasing the potency, specificity, bioavailability, and metabolic stability in M. tuberculosis itself. ..
  43. RECURRENT HEPATITIS B AFTER LIVER TRANSPLANTATION
    Anna Lok; Fiscal Year: 2007
    ..abstract_text> ..
  44. Effects of Microengineered Interactions on Liver-Specific Gene Expression
    Alexander Revzin; Fiscal Year: 2007
    ..In the future, proposed microfabricated devices will be used to induce differentiation of human ESC toward hepatic lineage. [unreadable] [unreadable] [unreadable]..
  45. Syntheses of Amino Acids and Amino Phosphonic Acids
    FRANKLIN DAVIS; Fiscal Year: 2005
    ..Targets include cyclic, unsaturated, and, beta substituted derivatives (beta amino, beta hydroxy, and beta fluoro). ..
  46. Flavopiridol as a Potential Therapy in Multiple Myeloma
    Keith Bible; Fiscal Year: 2005
    ..Results of proposed studies will improve understanding of the effects and mechanism(s) of action of flavopiridol in myeloma cells, thereby potentially contributing to the further clinical development of the drug. ..
  47. REGULATION OF P93 C FES TYROSINE KINASE ACTIVITY
    THOMAS SMITHGALL; Fiscal Year: 2005
    ..These studies will help to elucidate the molecular mechanisms that regulate Fes tyrosine kinase activity and to identify the signal transduction pathways utilized by Fes to transmit signals for differentiation. ..
  48. Perfluorocarbon Materials As Drug Delivery Vehicles
    Hans Joachim Lehmler; Fiscal Year: 2004
    ..abstract_text> ..
  49. SIGNALING BY VASOPRESSIN--ARTERIAL SMOOTH MUSCLE CELLS
    KENNETH BYRON; Fiscal Year: 2002
    ..Finally, the effects of AVP and other hormones on [Ca2+]i and membrane currents will be examined in freshly isolated smooth muscle cells from rat mesenteric arteries. ..
  50. MECHANISMS OF RHINOVIRUS INDUCED ASTHMA
    William Busse; Fiscal Year: 2002
    ..The proposed studies will provide new evidence as the mechanisms by which RV-infected epithelial cells cause granulocytic bronchial inflammation and asthma exacerbations. ..
  51. Third Generation Antiopportunistic Agents
    Aleem Gangjee; Fiscal Year: 2003
    ..Screening against tuberculosis (NIAID) and tumor cells in culture (NCI) is also proposed. ..
  52. IMMUNIZATION AGAINST TUMOR CELL ANTIGENS
    Paul Chapman; Fiscal Year: 2003
    ..This close mentoring relationship reflects our current teaching paradigm. The grant award will provide the PI with more time to conduct the clinical trials and to mentor additional beginning clinical investigators. ..
  53. Interactions of Black Cohosh with Cancer Therapy
    Sara Rockwell; Fiscal Year: 2005
    ..This project will assess these possibilities. The findings will show whether this herb is inactive and harmless, potentially dangerous to breast cancer patients, or of potential value in the treatment of this disease. ..
  54. Urine protein markers of disease in lupus nephritis
    James Oates; Fiscal Year: 2005
    ..Due to the power of proteomic and ANN techniques, novel mediators of disease activity and damage should be identified and thus contribute to the development of more targeted therapies for LN. ..
  55. DNA and Phytochemical Fingerprinting of Actaea Species
    Edward Kennelly; Fiscal Year: 2007
    ..Our long-range goals are to improve the quality of black cohosh dietary supplements and understand the variation in Actaea species. ..
  56. Phase II trial of 17-AAG in melanoma patients
    Paul Chapman; Fiscal Year: 2007
    ..post-treatment specimens, clinically responding tumors vs. non-responding tumors, and mutant BRAF vs. wild-type BRAF tumors. [unreadable] [unreadable] [unreadable]..
  57. Src Family Tyrosine Kinases in Tumor Cell Signaling
    THOMAS SMITHGALL; Fiscal Year: 2007
    ..Successful completion of these studies will provide strong validation of myeloid-specific Src kinases as targets for second-generation anti-CML drug development. ..
  58. Urodynamic and Multiethnic Variability of Men Treated b*
    Steven Kaplan; Fiscal Year: 2005
    ..Baseline urodynamic parameters which may predict improved outcome after MIST 3. The success of various types of MIST in treating BPH in African - American, Hispanic and Caucasian men. ..
  59. HIV PREVENTION TRIALS NETWORK LEADERSHIP GROUP
    Thomas Fleming; Fiscal Year: 2005
    ..abstract_text> ..
  60. ASYMMETRIC SYNTHESIS OF BIOACTIVE PRIMARY AMINES
    FRANKLIN DAVIS; Fiscal Year: 2006
    ....
  61. ALTERED KCa CHANNEL EXPRESSION IN DEVELOPING CEREBELLUM
    ANDREA YOOL; Fiscal Year: 2002
    ..The rat provides a useful model for studying postnatal cerebellar development and neuropathological damage, and may provide insights into methods to manipulate developmental abnormalities in the cerebellum. ..
  62. ESTROGEN BIOTRANSFORMATIONS AND BREAST CANCER ETIOLOGY
    ROBERT BRUEGGEMEIER; Fiscal Year: 2006
    ..3) To measure cellular levels of aromatase expression and cyclooxygenases expression in human breast cancer specimens. ..
  63. Phase I Clinical Trials of Anti-Cancer Agents
    Francis Giles; Fiscal Year: 2007
    ..abstract_text> ..