anilides

Summary

Top Publications

  1. pmc Switch from antagonist to agonist of the androgen receptor bicalutamide is associated with prostate tumour progression in a new model system
    Z Culig
    Department of Urology, University of Innsbruck, Austria
    Br J Cancer 81:242-51. 1999
  2. ncbi Inhibition of the hedgehog pathway in advanced basal-cell carcinoma
    Daniel D Von Hoff
    Translational Genomics Research Institute and Scottsdale Healthcare, Scottsdale, AZ, USA
    N Engl J Med 361:1164-72. 2009
  3. ncbi Smoothened mutation confers resistance to a Hedgehog pathway inhibitor in medulloblastoma
    Robert L Yauch
    Genentech, South San Francisco, CA 94080, USA
    Science 326:572-4. 2009
  4. ncbi Efficacy and safety of vismodegib in advanced basal-cell carcinoma
    Aleksandar Sekulic
    Mayo Clinic, Scottsdale, AZ 85259, USA
    N Engl J Med 366:2171-9. 2012
  5. ncbi Phase I trial of hedgehog pathway inhibitor vismodegib (GDC-0449) in patients with refractory, locally advanced or metastatic solid tumors
    Patricia M LoRusso
    Karmanos Cancer Institute, Detroit, Michigan Johns Hopkins University, Baltimore, Maryland, USA
    Clin Cancer Res 17:2502-11. 2011
  6. pmc VEGF and c-Met blockade amplify angiogenesis inhibition in pancreatic islet cancer
    Weon Kyoo You
    Cardiovascular Research Institute, Comprehensive Cancer Center, and Department of Anatomy, University of California, San Francisco, CA 94143, USA
    Cancer Res 71:4758-68. 2011
  7. ncbi Coregulator recruitment and histone modifications in transcriptional regulation by the androgen receptor
    Zhigang Kang
    Biomedicum Helsinki, Institute of Biomedicine, University of Helsinki, FI 00014, Finland
    Mol Endocrinol 18:2633-48. 2004
  8. ncbi Androgen receptor or estrogen receptor-beta blockade alters DHEA-, DHT-, and E(2)-induced proliferation and PSA production in human prostate cancer cells
    Julia T Arnold
    Endocrine Section, Laboratory of Clinical Investigation, Division of Intramural Research, National Center for Complementary and Alternative Medicine, National Institutes of Health, Bethesda, Maryland 20892 0933, USA
    Prostate 67:1152-62. 2007
  9. ncbi Inhibition of tumor cell growth, invasion, and metastasis by EXEL-2880 (XL880, GSK1363089), a novel inhibitor of HGF and VEGF receptor tyrosine kinases
    Fawn Qian
    Exelixis, Inc, South San Francisco, California 94083, USA
    Cancer Res 69:8009-16. 2009
  10. ncbi A phase I study of foretinib, a multi-targeted inhibitor of c-Met and vascular endothelial growth factor receptor 2
    Joseph Paul Eder
    Early Drug Development Center, Department of Medical Oncology, Dana Farber Cancer Institute and Department of Medicine, Brigham and Women s Hospital and Harvard Medical School, Boston, Massachusetts, USA
    Clin Cancer Res 16:3507-16. 2010

Research Grants

  1. ADAM: Androgen Deprivation vs. Antiandrogen Monotherapy
    Matthew Smith; Fiscal Year: 2004
  2. ACETYLCHOLINESTERASE-CATALYZED HYDROLYSIS
    Daniel Quinn; Fiscal Year: 1991
  3. LIPID CONJUGATES OF XENOBIOTICS
    GHULAM ANSARI; Fiscal Year: 2004
  4. TOTAL SYNTHESIS OF AZADIRACHTIN
    K Nicolaou; Fiscal Year: 2008
  5. SYNTHESIS OF ANTICANCER AGENTS
    K C Nicolaou; Fiscal Year: 2010
  6. Enabling Technologies for Combinatorial Chemistry
    K Nicolaou; Fiscal Year: 2005
  7. TOTAL SYNTHESIS OF APOPTOLIDIN
    K Nicolaou; Fiscal Year: 2004
  8. TOTAL SYNTHESIS OF NATURAL PRODUCTS
    K Nicolaou; Fiscal Year: 2002
  9. A pharmacogenetic and pharmacodynamic study of erlotinib
    CHARLES RUDIN; Fiscal Year: 2004
  10. DEVELOPMENT OF LIGAND ASSISTED ASYMMETRIC SYNTHESES
    Arun Ghosh; Fiscal Year: 2001

Detail Information

Publications245 found, 100 shown here

  1. pmc Switch from antagonist to agonist of the androgen receptor bicalutamide is associated with prostate tumour progression in a new model system
    Z Culig
    Department of Urology, University of Innsbruck, Austria
    Br J Cancer 81:242-51. 1999
    ..These findings may have repercussions on the natural course of prostate cancer with androgen deprivation and on strategies of therapeutic intervention...
  2. ncbi Inhibition of the hedgehog pathway in advanced basal-cell carcinoma
    Daniel D Von Hoff
    Translational Genomics Research Institute and Scottsdale Healthcare, Scottsdale, AZ, USA
    N Engl J Med 361:1164-72. 2009
    ..In a phase 1 clinical trial, we assessed the safety and pharmacokinetics of GDC-0449, a small-molecule inhibitor of SMO, and responses of metastatic or locally advanced basal-cell carcinoma to the drug...
  3. ncbi Smoothened mutation confers resistance to a Hedgehog pathway inhibitor in medulloblastoma
    Robert L Yauch
    Genentech, South San Francisco, CA 94080, USA
    Science 326:572-4. 2009
    ..These findings show that acquired mutations in a serpentine receptor with features of a G protein-coupled receptor can serve as a mechanism of drug resistance in human cancer...
  4. ncbi Efficacy and safety of vismodegib in advanced basal-cell carcinoma
    Aleksandar Sekulic
    Mayo Clinic, Scottsdale, AZ 85259, USA
    N Engl J Med 366:2171-9. 2012
    ..A phase 1 study of vismodegib (GDC-0449), a first-in-class, small-molecule inhibitor of the hedgehog pathway, showed a 58% response rate among patients with advanced basal-cell carcinoma...
  5. ncbi Phase I trial of hedgehog pathway inhibitor vismodegib (GDC-0449) in patients with refractory, locally advanced or metastatic solid tumors
    Patricia M LoRusso
    Karmanos Cancer Institute, Detroit, Michigan Johns Hopkins University, Baltimore, Maryland, USA
    Clin Cancer Res 17:2502-11. 2011
    ..This phase I trial assessed GDC-0449 treatment in patients with solid tumors refractory to current therapies or for which no standard therapy existed...
  6. pmc VEGF and c-Met blockade amplify angiogenesis inhibition in pancreatic islet cancer
    Weon Kyoo You
    Cardiovascular Research Institute, Comprehensive Cancer Center, and Department of Anatomy, University of California, San Francisco, CA 94143, USA
    Cancer Res 71:4758-68. 2011
    ....
  7. ncbi Coregulator recruitment and histone modifications in transcriptional regulation by the androgen receptor
    Zhigang Kang
    Biomedicum Helsinki, Institute of Biomedicine, University of Helsinki, FI 00014, Finland
    Mol Endocrinol 18:2633-48. 2004
    ....
  8. ncbi Androgen receptor or estrogen receptor-beta blockade alters DHEA-, DHT-, and E(2)-induced proliferation and PSA production in human prostate cancer cells
    Julia T Arnold
    Endocrine Section, Laboratory of Clinical Investigation, Division of Intramural Research, National Center for Complementary and Alternative Medicine, National Institutes of Health, Bethesda, Maryland 20892 0933, USA
    Prostate 67:1152-62. 2007
    ..LNCaP and LAPC-4 prostate cancer cells were used to determine whether DHEA-modulated proliferation and prostate specific antigen (PSA) production were mediated via the androgen receptor (AR) and/or ERbeta...
  9. ncbi Inhibition of tumor cell growth, invasion, and metastasis by EXEL-2880 (XL880, GSK1363089), a novel inhibitor of HGF and VEGF receptor tyrosine kinases
    Fawn Qian
    Exelixis, Inc, South San Francisco, California 94083, USA
    Cancer Res 69:8009-16. 2009
    ..Collectively, these data indicate that EXEL-2880 may prevent tumor growth through a direct effect on tumor cell proliferation and by inhibition of invasion and angiogenesis mediated by HGF and VEGF receptors...
  10. ncbi A phase I study of foretinib, a multi-targeted inhibitor of c-Met and vascular endothelial growth factor receptor 2
    Joseph Paul Eder
    Early Drug Development Center, Department of Medical Oncology, Dana Farber Cancer Institute and Department of Medicine, Brigham and Women s Hospital and Harvard Medical School, Boston, Massachusetts, USA
    Clin Cancer Res 16:3507-16. 2010
    ..Secondary objectives included evaluation of plasma pharmacokinetics, long-term safety after repeated administration, preliminary antitumor activity, and pharmacodynamic activity...
  11. ncbi Androgen receptor regulates Cdc6 in synchronized LNCaP cells progressing from G1 to S phase
    V Uma Bai
    Vattikuti Urology Institute, Henry Ford Health Sciences Center, Detroit, Michigan, USA
    J Cell Physiol 204:381-7. 2005
    ..AR may play an important role in the onset of DNA synthesis in prostate cancer cells by regulating the expression and stability of Cdc6, which is critically required for the assembly of the pre-replication complex(pre-RC)...
  12. ncbi Mechanisms underlying pioglitazone-mediated relaxation in isolated blood vessel
    Hidemi Nomura
    Department of Veterinary Pharmacology, School of Veterinary Medicine, Kitasato University, Aomori, Japan
    J Pharmacol Sci 108:258-65. 2008
    ..While endothelium-dependent relaxation is mediated via nitric oxide, the endothelium-independent one is responsible for smooth muscle K+ (K(V), K(IR))-channel opening...
  13. ncbi Combined androgen blockade for prostate cancer: review of efficacy, safety and cost-effectiveness
    Hideyuki Akaza
    Research Center for Advanced Science and Technology, The University of Tokyo, Tokyo, Japan
    Cancer Sci 102:51-6. 2011
    ....
  14. ncbi GDC-0449-a potent inhibitor of the hedgehog pathway
    Kirk D Robarge
    Genentech, Small Molecule Drug Discovery 1 DNA Way, South San Francisco, CA 94080, United States
    Bioorg Med Chem Lett 19:5576-81. 2009
    ..5mg/kg BID in a medulloblastoma allograft mouse model that is wholly dependent on the Hh pathway for growth and is currently in human clinical trials, where it is initially being evaluated for the treatment of BCC...
  15. ncbi Small-molecule modulators of the Sonic Hedgehog signaling pathway
    Benjamin Z Stanton
    Department of Chemistry and Chemical Biology, Harvard University, 12 Oxford Street, Cambridge, MA 02138, USA
    Mol Biosyst 6:44-54. 2010
    ..Several Shh inhibitors have not succeeded in the clinic for unknown reasons, but clinical trials in BCC and pancreatic cancer with the promising Smo antagonists GDC-0449 and IPI-926 are currently underway...
  16. ncbi Attenuation of early liver fibrosis by pharmacological inhibition of smoothened receptor signaling
    Akshay Pratap
    Division of Solid Organ Transplantation, Methodist University Hospital, Memphis, TN, USA
    J Drug Target 20:770-82. 2012
    ..Thus, GDC has the potential to serve as a new therapeutic agent for treating early liver fibrosis...
  17. pmc Itraconazole and arsenic trioxide inhibit Hedgehog pathway activation and tumor growth associated with acquired resistance to smoothened antagonists
    James Kim
    Institute for Stem Cell Biology and Regenerative Medicine, Stanford University, Stanford, CA 94305, USA
    Cancer Cell 23:23-34. 2013
    ..Itraconazole and arsenic trioxide, alone or in combination, inhibit the growth of medulloblastoma and basal cell carcinoma in vivo, and prolong survival of mice with intracranial drug-resistant SMO(D477G) medulloblastoma...
  18. pmc Rosiglitazone treatment prevents mitochondrial dysfunction in mutant huntingtin-expressing cells: possible role of peroxisome proliferator-activated receptor-gamma (PPARgamma) in the pathogenesis of Huntington disease
    Rodrigo A Quintanilla
    Department of Anesthesiology, University of Rochester, University Medical Center, 601 Elmwood Avenue, Rochester, NY 14642, USA
    J Biol Chem 283:25628-37. 2008
    ....
  19. pmc PPARgamma agonist rosiglitazone is neuroprotective after traumatic brain injury via anti-inflammatory and anti-oxidative mechanisms
    Jae Hyuk Yi
    Department of Neurological Surgery, University of Wisconsin, K4 8 Mail code CSC 8660, 600 Highland Avenue, Madison, WI 53792, USA
    Brain Res 1244:164-72. 2008
    ..Treatment with GW9662 (a specific PPARgamma antagonist) prevented all the above PPARgamma-mediated actions. Thus, PPARgamma activation confers neuroprotection after TBI by anti-inflammatory, anti-apoptotic and anti-oxidative mechanisms...
  20. ncbi Androgens up-regulate the insulin-like growth factor-I receptor in prostate cancer cells
    Giuseppe Pandini
    Dipartimento di Medicina Interna e di Medicina Specialistica, Cattedra di Endocrinologia, University of Catania, Ospedale Garibaldi, Catania, Italy
    Cancer Res 65:1849-57. 2005
    ..Anti-androgen therapy may be only partially effective, or almost ineffective, in blocking important biological effects of androgens, such as activation of the IGF system...
  21. pmc Hedgehog signaling antagonist promotes regression of both liver fibrosis and hepatocellular carcinoma in a murine model of primary liver cancer
    George M Philips
    Division of Gastroenterology, Department of Medicine, Duke University Medical Center, Durham, North Carolina, United States of America
    PLoS ONE 6:e23943. 2011
    ..We used Mdr2(-/-) mice to investigate the hypothesis that activation of the hedgehog (Hh) signaling pathway promotes development of both liver fibrosis and HCC...
  22. ncbi Activation of TRPV1 contributes to morphine tolerance: involvement of the mitogen-activated protein kinase signaling pathway
    Yong Chen
    Department of Neurology, University of Wurzburg, 97080 Wurzburg, Germany
    J Neurosci 28:5836-45. 2008
    ..Thus, blocking TRPV1 might be a way to reduce morphine tolerance...
  23. ncbi Small molecule inhibition of GDC-0449 refractory smoothened mutants and downstream mechanisms of drug resistance
    Gerrit J P Dijkgraaf
    Department of Molecular Biology, Genentech Inc, South San Francisco, California 94080, USA
    Cancer Res 71:435-44. 2011
    ..Importantly, these HPI resistant MB allografts retained their sensitivity to PI3K inhibition, presenting additional opportunities for the treatment of such tumors...
  24. ncbi Role of androgen receptor in the progression of human prostate tumor cells to androgen independence and insensitivity
    John M Kokontis
    Ben May Institute for Cancer Research and the Department of Biochemistry and Molecular Biology, The University of Chicago, Chicago, Illinois 60637, USA
    Prostate 65:287-98. 2005
    ..Various studies have implicated the androgen receptor (AR) in the progression of androgen-dependent human prostate cancer cells to androgen-independent and androgen-insensitive phenotypes, but the exact role of AR in progression is unclear...
  25. ncbi Antagonism of peroxisome proliferator-activated receptor gamma prevents high-fat diet-induced obesity in vivo
    Ryosuke Nakano
    Pharmacology Research Laboratories, Drug Discovery Research, Astellas Pharma Inc, 5 2 3 Toukoudai, Tsukuba shi, Ibaraki 300 2698, Japan
    Biochem Pharmacol 72:42-52. 2006
    ..These data indicate that antagonism of PPARgamma using a synthetic ligand suppresses the increased adiposity observed in HF diet-induced obesity, and that a PPARgamma antagonist could possibly be developed as an anti-obesity drug...
  26. ncbi Prolonged treatment with bicalutamide induces androgen receptor overexpression and androgen hypersensitivity
    Hiromitsu Kawata
    Pharmaceutical Research Department 2, Kamakura Research Laboratories, Chugai Pharmaceutical Co, Ltd, Kamakura, Kanagawa, Japan
    Prostate 70:745-54. 2010
    ..However, the mechanism of bicalutamide resistance remains unclear because few cell models have been generated...
  27. pmc Hedgehog pathway inhibition radiosensitizes non-small cell lung cancers
    Jing Zeng
    Department of Radiation Oncology and Molecular Radiation Sciences, The Johns Hopkins University School of Medicine, Baltimore, Maryland 21231 2410, USA
    Int J Radiat Oncol Biol Phys 86:143-9. 2013
    ..Whether Hedgehog inhibition can affect radiation efficacy in vivo has not been reported...
  28. ncbi Bicalutamide functions as an androgen receptor antagonist by assembly of a transcriptionally inactive receptor
    David Masiello
    Cancer Biology Program, Hematology Oncology Division, Department of Medicine, Beth Israel Deaconess Medical Center and Harvard Medical School, Boston, Massachusetts 02215, USA
    J Biol Chem 277:26321-6. 2002
    ..These results demonstrate that bicalutamide stimulates the assembly of a transcriptionally inactive AR on DNA and support altered coactivator (or corepressor) expression as a mechanism of bicalutamide-resistant androgen-independent PCa...
  29. ncbi Bicalutamide as immediate therapy either alone or as adjuvant to standard care of patients with localized or locally advanced prostate cancer: first analysis of the early prostate cancer program
    William A See
    Medical College of Wisconsin, Milwaukee, Wisconsin, USA
    J Urol 168:429-35. 2002
    ..We determine the efficacy and tolerability of bicalutamide as immediate therapy, either alone or as adjuvant to treatment of curative intent, in patients with clinically localized or locally advanced prostate cancer...
  30. ncbi The androgen receptor pathway is by-passed in prostate cancer cells generated after prolonged treatment with bicalutamide
    Alfred Hobisch
    Department of Urology, General Hospital Feldkirch, Feldkirch, Austria
    Prostate 66:413-20. 2006
    ..However, little attention has been paid to the androgen receptor-signaling pathway in the development of therapy resistance in patients who receive chronic treatment with a non-steroidal anti-androgen...
  31. ncbi Hedgehog signaling inhibition by the small molecule smoothened inhibitor GDC-0449 in the bone forming prostate cancer xenograft MDA PCa 118b
    Maria Karlou
    Department of Genitourinary Medical Oncology, The David Koch Center for Applied Research of Genitourinary Cancers, The Stanford Alexander Tissue Derivatives Laboratory, The University of Texas MD Anderson Cancer Center, Houston, Texas 77030 4009, USA
    Prostate 72:1638-47. 2012
    ....
  32. pmc Store-operated Ca(2+) entry (SOCE) contributes to normal skeletal muscle contractility in young but not in aged skeletal muscle
    Angela M Thornton
    Department of Physiology and Biophysics, Robert Wood Johnson Medical School, Piscataway, NJ 08854, USA
    Aging (Albany NY) 3:621-34. 2011
    ....
  33. ncbi Multidimensional chemical genetic analysis of diversity-oriented synthesis-derived deacetylase inhibitors using cell-based assays
    Stephen J Haggarty
    Departments of Molecular and Cellular Biology, Harvard University, 12 Oxford Street, Cambridge, MA 02138, USA
    Chem Biol 10:383-96. 2003
    ..These small molecules will facilitate dissecting the role of acetylation in a variety of cell biological processes...
  34. ncbi Prosaposin upregulates AR and PSA expression and activity in prostate cancer cells (LNCaP)
    Shahriar Koochekpour
    Department of Microbiology and Immunology, Louisiana State University Health Sciences Center, New Orleans, Louisiana 70112, USA
    Prostate 67:178-89. 2007
    ..Here, we explored the possibility for a functional relationship between prosaposin and androgen receptor (AR) in LNCaP cells...
  35. ncbi Structural biasing elements for in-cell histone deacetylase paralog selectivity
    Jason C Wong
    Department of Chemistry and Chemical Biology, Harvard Institute of Chemistry and Cell Biology, and the Howard Hughes Medical Institute, Harvard University, 12 Oxford Street, Cambridge, Massachusetts 02138, USA
    J Am Chem Soc 125:5586-7. 2003
    ..We also show that suberoylanilide hydroxamic acid (SAHA) alone is a nonparalog-selective HDAC inhibitor and that the 1,3-dioxane diversity appended to SAHA is essential for HDAC6 paralog selectivity...
  36. ncbi c-Met is a marker of pancreatic cancer stem cells and therapeutic target
    Chenwei Li
    Department of Surgery, University of Michigan, Ann Arbor, Michigan, USA
    Gastroenterology 141:2218-2227.e5. 2011
    ..c-Met is a marker of normal mouse pancreatic stem and progenitor cells; we investigated whether it is also a marker of human pancreatic CSCs that might be developed as a therapeutic target...
  37. ncbi Inhibition of cell proliferation by potential peroxisome proliferator-activated receptor (PPAR) gamma agonists and antagonists
    Michael A Lea
    Department of Biochemistry and Molecular Biology, UMDNJ New Jersey Medical School, Newark, New Jersey 07103, USA
    Anticancer Res 24:2765-71. 2004
    ..We conclude that potential PPAR gamma antagonists may fail to reverse the growth inhibitory effect of PPAR gamma ligands and may themselves act as growth inhibitory agents...
  38. ncbi Additive antitumor effects of the epidermal growth factor receptor tyrosine kinase inhibitor, gefitinib (Iressa), and the nonsteroidal antiandrogen, bicalutamide (Casodex), in prostate cancer cells in vitro
    Claudio Festuccia
    Department of Experimental Medicine, University of L Aquila, L Aquila, Italy
    Int J Cancer 115:630-40. 2005
    ..This causes a significant delay in the onset of EGFR-driven androgen independence...
  39. ncbi Quantifying effects of ligands on androgen receptor nuclear translocation, intranuclear dynamics, and solubility
    Marco Marcelli
    Department of Molecular and Cellular Biology, Baylor College of Medicine, Houston, Texas 77030, USA
    J Cell Biochem 98:770-88. 2006
    ..These results further support the notion that ligand specific interactions rapidly affect receptor and co-factor organization, solubility, and molecular dynamics, and each can be aberrantly affected by mutation and overexpression...
  40. ncbi A 90 kDa fragment of filamin A promotes Casodex-induced growth inhibition in Casodex-resistant androgen receptor positive C4-2 prostate cancer cells
    Y Wang
    Department of Urology, School of Medicine, University of California Davis, Sacramento, CA, USA
    Oncogene 26:6061-70. 2007
    ..Our results demonstrate that expression of nuclear FlnA is necessary for androgen dependence in these cells...
  41. ncbi Histone deacetylase inhibitors reverse gene silencing in Friedreich's ataxia
    David Herman
    Department of Molecular Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    Nat Chem Biol 2:551-8. 2006
    ..This class of HDAC inhibitors may yield therapeutics for Friedreich's ataxia...
  42. ncbi Ca2+-independent phospholipase A2 enhances store-operated Ca2+ entry in dystrophic skeletal muscle fibers
    François Xavier Boittin
    Laboratory of Pharmacology, Geneva Lausanne School of Pharmaceutical Sciences, University of Geneva, University of Lausanne, 1211 Geneva 4, Switzerland
    J Cell Sci 119:3733-42. 2006
    ..The Ca2+-independent phospholipase A2 pathway therefore appears as an attractive target to reduce excessive Ca2+ influx and subsequent degeneration occurring in dystrophic fibers...
  43. ncbi S32826, a nanomolar inhibitor of autotaxin: discovery, synthesis and applications as a pharmacological tool
    Gilles Ferry
    Pharmacologie Moléculaire et Cellulaire, Institut de Recherches Servier, Croissy sur Seine, France
    J Pharmacol Exp Ther 327:809-19. 2008
    ..S32826 is the first reported inhibitor of autotaxin with an IC(50) in the nanomolar range that can be used to validate the role of autotaxin in various pathologies in cellular models...
  44. pmc Hedgehog pathway inhibitor HhAntag691 is a potent inhibitor of ABCG2/BCRP and ABCB1/Pgp
    Yimao Zhang
    Russell H Morgan Department of Radiology and Radiological Sciences, Johns Hopkins Medical Institutions, Baltimore, MD 21231, USA
    Neoplasia 11:96-101. 2009
    ..In addition to its effect on Hh signaling, the ability of HhAntag691 and related compounds to inhibit two key ABC transporters could contribute to their effectiveness in treating malignancies...
  45. ncbi Establishment and characterization of an androgen receptor-dependent, androgen-independent human prostate cancer cell line, LNCaP-CS10
    Nobuyuki Ishikura
    Research Division, Kamakura Research Laboratories, Pharmaceutical Research Department 2, Chugai Pharmaceutical Co Ltd, Kamakura, Kanagawa, Japan
    Prostate 70:457-66. 2010
    ....
  46. ncbi Platensimycin is a selective FabF inhibitor with potent antibiotic properties
    Jun Wang
    Merck Research Laboratories, Rahway, New Jersey 07065, USA
    Nature 441:358-61. 2006
    ..Platensimycin is the most potent inhibitor reported for the FabF/B condensing enzymes, and is the only inhibitor of these targets that shows broad-spectrum activity, in vivo efficacy and no observed toxicity...
  47. ncbi Antiandrogen-induced cell death in LNCaP human prostate cancer cells
    E C Y Lee
    Department of Biological Science, University of Notre Dame, Notre Dame, IN 46556, USA
    Cell Death Differ 10:761-71. 2003
    ....
  48. ncbi Acyl substitution at the ortho position of anilides enhances oral bioavailability of thiophene sulfonamides: TBC3214, an ETA selective endothelin antagonist
    C Wu
    Department of Chemistry, Texas Biotechnology Corporation, 7000 Fannin, Suite 1920, Houston, Texas 77030, USA
    J Med Chem 44:1211-6. 2001
    ..It is very potent (IC(50) for ET(A) = 40 pM) and highly selective for ET(A) vs ET(B) receptors (400 000-fold), with a half-life of >4 h and oral bioavailability of 25% in rats, 42% in cats, and 70% in dogs...
  49. ncbi Synergistic effects of foretinib with HER-targeted agents in MET and HER1- or HER2-coactivated tumor cells
    Li Liu
    GlaxoSmithKline, 17 1356I, 5 Moore Drive, Research Triangle Park, NC 27709 3398, USA
    Mol Cancer Ther 10:518-30. 2011
    ..0225). These data suggest that combination therapy with foretinib and HER-targeted agents should be tested as a treatment option for HER1- or HER2-positive patients with MET-amplified or -overexpressing tumors...
  50. ncbi Pathological changes of high-grade prostatic intraepithelial neoplasia and prostate cancer after monotherapy with bicalutamide 150 mg
    Vincenzo Scattoni
    Department of Urology, University Vita Salute, Scientific Institute H San Raffaele, Milan, Italy
    BJU Int 98:54-8. 2006
    ..To evaluate the morphological changes induced by a 3-month course of neoadjuvant bicalutamide 150 mg/day before radical prostatectomy (RP) on prostatic adenocarcinoma and high-grade prostatic intraepithelial neoplasia (HGPIN)...
  51. ncbi Induction of invasive phenotype by Casodex in hormone-sensitive prostate cancer cells
    Ping Zhan
    Department of Biological Science, University of Notre Dame, Notre Dame, IN 46556, USA
    J Steroid Biochem Mol Biol 83:101-11. 2002
    ..These observations have significant implications in the treatment of prostate cancer, since the appearance of a more aggressive phenotype following treatment is clearly undesirable...
  52. ncbi Transgenic mouse model for rapid pharmacodynamic evaluation of antiandrogens
    Katharine Ellwood-Yen
    Department of Medicine, Jonsson Comprehensive Cancer Center, David Geffen School of Medicine, University of California at Los Angeles, California, USA
    Cancer Res 66:10513-6. 2006
    ..ARR2 Pb-Lux mice provide a novel method for rapid pharmacodynamic evaluation of novel pharmacologic compounds designed to inhibit androgen receptor signaling...
  53. ncbi Rosiglitazone, a peroxisome proliferator-activated receptor-gamma agonist, reduces acute lung injury in endotoxemic rats
    Dong Liu
    Department of Anesthesiology, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, China
    Crit Care Med 33:2309-16. 2005
    ..This study was designated to determine the effects of rosiglitazone on endotoxin-induced acute lung injury in rats...
  54. pmc Vismodegib
    Charles M Rudin
    The Sidney Kimmel Comprehensive Cancer Center, Johns Hopkins University School of Medicine, Baltimore, Maryland 21287, USA
    Clin Cancer Res 18:3218-22. 2012
    ..The mechanism of action, preclinical and clinical data, and potential utility in other disease contexts are reviewed here...
  55. pmc Drug-targeted inhibition of peroxisome proliferator-activated receptor-gamma enhances the chemopreventive effect of anti-estrogen therapy
    Hongyan Yuan
    Department of Oncology, Georgetown University School of Medicine, and Lombardi Comprehensive Cancer Center, Washington, DC, USA
    Oncotarget 3:345-56. 2012
    ..These findings suggest that it may be possible to pharmacologically influence the responsiveness of tumors to anti-estrogen therapy...
  56. ncbi Androgen receptor as a target in androgen-independent prostate cancer
    Steven P Balk
    Cancer Biology Program, Division of Hematology Oncology, Beth Israel Deaconess Medical Center and Harvard Medical School, Boston, Massachusetts 02215, USA
    Urology 60:132-8; discussion 138-9. 2002
    ..Understanding the mechanisms responsible for AR function in androgen-independent prostate cancer should allow the more rational development of antagonists that can enhance the efficacy of androgen ablation therapies...
  57. pmc Ethanol modulates the VR-1 variant amiloride-insensitive salt taste receptor. II. Effect on chorda tympani salt responses
    Vijay Lyall
    Department of Physiology, Division of Nephrology, Virginia Commonwealth University, Richmond, VA 23298, USA
    J Gen Physiol 125:587-600. 2005
    ..VR-1 KO mice demonstrated no Bz-insensitive CT response to NaCl and no sensitivity to ethanol. We conclude that ethanol increases salt taste sensitivity by its direct action on the Bz-insensitive VR-1 variant salt taste receptor...
  58. pmc Differential androgen deprivation therapies with anti-androgens casodex/bicalutamide or MDV3100/Enzalutamide versus anti-androgen receptor ASC-J9(R) Lead to promotion versus suppression of prostate cancer metastasis
    Tzu Hua Lin
    George Whipple Laboratory for Cancer Research, Department of Pathology, Wilmot Cancer Center, University of Rochester Medical Center, Rochester, New York 14642, USA
    J Biol Chem 288:19359-69. 2013
    ..These findings suggest the potential risks of using anti-androgens and provide a potential new therapy using ASC-J9® to battle PCa metastasis at the castration-resistant stage. ..
  59. ncbi Selection for androgen receptor mutations in prostate cancers treated with androgen antagonist
    M E Taplin
    University of Massachusetts Cancer Center, Worcester 01655, USA
    Cancer Res 59:2511-5. 1999
    ..These findings demonstrate that AR mutations occur in response to strong selective pressure from flutamide treatment...
  60. ncbi Estrogen improves vascular function via peroxisome-proliferator-activated-receptor-γ
    Vedat Tiyerili
    Medizinische Klinik und Poliklinik II, Innere Medizin, Universitatsklinikum Bonn, Sigmund Freud Str 25, 53105 Bonn, Germany
    J Mol Cell Cardiol 53:268-76. 2012
    ....
  61. ncbi Apoptosis induced in HepG2 cells by the synthetic cannabinoid WIN: involvement of the transcription factor PPARgamma
    Michela Giuliano
    Dipartimento di Scienze Biochimiche, Universita di Palermo, Via del Vespro 129, 90127 Palermo, Italy
    Biochimie 91:457-65. 2009
    ..Altogether, the results seem to indicate a potential therapeutic role of WIN in hepatic cancer treatment...
  62. ncbi PPARgamma agonists inhibit TGF-beta induced pulmonary myofibroblast differentiation and collagen production: implications for therapy of lung fibrosis
    Heather A Burgess
    Department of Environmental Medicine, Univ of Rochester School of Medicine, 601 Elmwood Ave, Rochester, NY 14642, USA
    Am J Physiol Lung Cell Mol Physiol 288:L1146-53. 2005
    ..Thus PPARgamma agonists have novel and potent antifibrotic effects in human lung fibroblasts and may have potential for therapy of fibrotic diseases in the lung and other tissues...
  63. ncbi Antagonistic interaction between bicalutamide (Casodex) and radiation in androgen-positive prostate cancer LNCaP cells
    Laurent Quero
    Institut Curie, Bât 110 112, Centre Universitaire, Orsay, France
    Prostate 70:401-11. 2010
    ..However, biological data for the interaction between bicalutamide and ionizing radiation in concomitant association are lacking...
  64. ncbi Novel mechanism of lapatinib resistance in HER2-positive breast tumor cells: activation of AXL
    Li Liu
    Department of Translational Research, GlaxoSmithKline, King of Prussia, Pennsylvania, USA
    Cancer Res 69:6871-8. 2009
    ....
  65. pmc Telmisartan ameliorates insulin sensitivity by activating the AMPK/SIRT1 pathway in skeletal muscle of obese db/db mice
    Asuka Shiota
    Department of Cardio Diabetes Medicine, University of Tokushima Graduate School of Health Biosciences, 3 18 15 Kuramoto, Tokushima 770 8503, Japan
    Cardiovasc Diabetol 11:139. 2012
    ..Here, we investigated the pathways through which telmisartan acts on skeletal muscle, in vitro as well as in vivo...
  66. ncbi Capsaicin, a component of red peppers, induces expression of androgen receptor via PI3K and MAPK pathways in prostate LNCaP cells
    Sophie Malagarie-Cazenave
    Department of Biochemistry and Molecular Biology, School of Medicine, University of Alcala, Madrid, Spain
    FEBS Lett 583:141-7. 2009
    ..AR silencing by the use of siRNA, as well as blocking the AR receptor with bicalutamide, inhibited the proliferative effect of capsaicin...
  67. ncbi Functional consequences of cysteine modification in the ligand binding sites of peroxisome proliferator activated receptors by GW9662
    Lisa M Leesnitzer
    Systems Research, GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709, USA
    Biochemistry 41:6640-50. 2002
    ....
  68. ncbi Sulfonamide anilides, a novel class of histone deacetylase inhibitors, are antiproliferative against human tumors
    Marielle Fournel
    MethylGene, Inc, St Laurent, Quebec, H4S 2A1 Canada
    Cancer Res 62:4325-30. 2002
    ..We have designed and synthesized novel nonhydroxamate sulfonamide anilides that can inhibit human HDAC enzymes and can induce hyperacetylation of histones in human cancer cells...
  69. ncbi Non-steroidal antiandrogens act as AF-1 agonists under conditions of high androgen-receptor expression
    Hiroaki Fuse
    Pharmacological Research Department, ASKA Pharmaceutical Co Ltd, Takatsu ku, Kawasaki, Kanagawa, Japan
    Prostate 67:630-7. 2007
    ....
  70. ncbi The novel histone deacetylase inhibitor BML-210 exerts growth inhibitory, proapoptotic and differentiation stimulating effects on the human leukemia cell lines
    Jurate Savickiene
    Department of Developmental Biology, Institute of Biochemistry, LT 08662 Vilnius, Lithuania
    Eur J Pharmacol 549:9-18. 2006
    ..These findings suggest that BML-210 could be a promising antileukemic agent to induce apoptosis and to modulate differentiation through the modulation of histone acetylation and gene expression...
  71. pmc Androgen receptor interacts with telomeric proteins in prostate cancer cells
    Sahn Ho Kim
    Vattikuti Urology Institute, Henry Ford Hospital, Detroit, Michigan 48202, USA
    J Biol Chem 285:10472-6. 2010
    ..Together, these observations suggest an allosteric role of AR in telomere complex stability in prostate cancer cells and suggest that AR-antagonist Casodex-mediated cell death may be due to telomere complex disruption...
  72. pmc Domain-selective small-molecule inhibitor of histone deacetylase 6 (HDAC6)-mediated tubulin deacetylation
    Stephen J Haggarty
    Department of Molecular and Cellular Biology, and Harvard Institute of Chemistry and Cell Biology, Harvard University, 12 Oxford Street, Cambridge, MA 02138, USA
    Proc Natl Acad Sci U S A 100:4389-94. 2003
    ..They also suggest that small molecules that selectively inhibit HDAC6-mediated alpha-tubulin deacetylation, a first example of which is tubacin, might have therapeutic applications as antimetastatic and antiangiogenic agents...
  73. ncbi Activation of the androgen receptor N-terminal domain by interleukin-6 via MAPK and STAT3 signal transduction pathways
    Takeshi Ueda
    Department of Cancer Endocrinology, British Columbia Cancer Agency, 600 West 10th Avenue, Vancouver, British Columbia V5Z 4E6, Canada
    J Biol Chem 277:7076-85. 2002
    ..These results demonstrate that activation of the human AR NTD by IL-6 was mediated through MAPK and STAT3 signal transduction pathways in LNCaP prostate cancer cells...
  74. ncbi Neuroprotection against focal ischemic brain injury by the peroxisome proliferator-activated receptor-gamma agonist rosiglitazone
    Yumin Luo
    Department of Neurology, University of Pittsburgh School of Medicine, PA 15213, USA
    J Neurochem 97:435-48. 2006
    ..These results suggest that the PPAR-gamma agonist rosiglitazone has neuroprotective properties that are at least partially mediated via anti-inflammatory actions, and is thus a potential novel therapeutic agent for stroke...
  75. ncbi The role of antiandrogen monotherapy in the treatment of prostate cancer
    J Anderson
    Department of Urology, The Royal Hallamshire Hospital, Sheffield, UK
    BJU Int 91:455-61. 2003
    ..Bicalutamide has a more favourable side-effect profile than the other antiandrogens and is more likely to promote compliance...
  76. ncbi Antagonist of peroxisome proliferator-activated receptor gamma induces cerebellar amyloid-beta levels and motor dysfunction in APP/PS1 transgenic mice
    Jing Du
    Protein Science Key Laboratory of the Ministry of Education, Department of Biological Sciences and Biotechnology, School of Medicine, Tsinghua University, Beijing 100084, PR China
    Biochem Biophys Res Commun 384:357-61. 2009
    ..Since cerebellum is spared from significant Abeta accumulation and neurotoxicity in AD patients and animal models, these findings suggest a crucial role of PPARgamma steady-state activity in protection of cerebellum against AD pathology...
  77. ncbi Highly favorable antiviral activity and resistance profile of the novel thiocarboxanilide pentenyloxy ether derivatives UC-781 and UC-82 as inhibitors of human immunodeficiency virus type 1 replication
    J Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Mol Pharmacol 50:394-401. 1996
    ....
  78. ncbi Peroxisome proliferator-activated receptor-gamma antagonists exhibit potent antiproliferative effects versus many hematopoietic and epithelial cancer cell lines
    Jack D Burton
    Center for Molecular Medicine and Immunology, Belleville, New Jersey 07109, USA
    Anticancer Drugs 18:525-34. 2007
    ..These findings support further translational studies to explore the mechanism of action and therapeutic potential of this class of agents...
  79. ncbi Novel mutations of androgen receptor: a possible mechanism of bicalutamide withdrawal syndrome
    Takahito Hara
    Pharmaceutical Research Laboratories, Takeda Chemical Industries, Ltd, Osaka 532 8686, Japan
    Cancer Res 63:149-53. 2003
    ..Our data strongly support the hypothesis that AR mutation is one possible mechanism of the AWS and suggest that flutamide might be effective as a second-line therapy for refractory PC previously treated with bicalutamide...
  80. pmc A novel androgen receptor-binding element modulates Cdc6 transcription in prostate cancer cells during cell-cycle progression
    Feng Jin
    Department of Physiology and Biophysics, Robert Wood Johnson Medical School, UMDNJ, Piscataway, NJ 08854, USA
    Nucleic Acids Res 37:4826-38. 2009
    ..Collectively, our results suggest that Cdc6 is a key regulatory target for AR and provide new insights into the mechanisms of prostate cancer cell proliferation...
  81. pmc Development of a comprehensive human immunodeficiency virus type 1 screening algorithm for discovery and preclinical testing of topical microbicides
    Carol Lackman-Smith
    Southern Research Institute, 431 Aviation Way, Frederick, Maryland 21701, USA
    Antimicrob Agents Chemother 52:1768-81. 2008
    ....
  82. pmc Acceptability of UC781 gel as a rectal microbicide among HIV-uninfected women and men
    Ana Ventuneac
    HIV Center for Clinical and Behavioral Studies, New York State Psychiatric Institute and Columbia University, 1051 Riverside Drive, Unit 15, New York, NY 10032, USA
    AIDS Behav 14:618-28. 2010
    ..Acceptability research is essential in early phases of microbicide development to identify potential problems, understand user preferences, and introduce changes if needed...
  83. ncbi Pronociceptive response elicited by TRPA1 receptor activation in mice
    E L Andrade
    Department of Pharmacology, Federal University of Santa Catarina, CCB, Campus Universitario Trindade, 88049 900, Florianopolis, SC, Brazil
    Neuroscience 152:511-20. 2008
    ..Thus, the TRPA1 receptor has an apparently relevant role in nociceptive processes and the selective TRPA1 antagonist might possess a potential antinociceptive property...
  84. pmc Peroxisome proliferator-activated receptor gamma is a target of progesterone regulation in the preovulatory follicles and controls ovulation in mice
    Jaeyeon Kim
    University of Illinois, MC 114, 534 Burrill Hall, 407 S Goodwin, Urbana, IL 61801, USA
    Mol Cell Biol 28:1770-82. 2008
    ..Collectively, these studies revealed that PPARgamma is a key mediator of the biological actions of PR in the granulosa cells and activation of its downstream pathways critically controls ovulation...
  85. ncbi Androgen receptor mediates non-genomic activation of phosphatidylinositol 3-OH kinase in androgen-sensitive epithelial cells
    Silvère Baron
    Génétique des Eucaryotes et Endocrinologie Moléculaire, UMR 6547 CNRS Université Blaise Pascal, Campus Universitaire des Cezeaux, 24 avenue des Landais, 63177 Aubiere Cedex, France
    J Biol Chem 279:14579-86. 2004
    ..Together, these novel findings point out an important and physiologically relevant link between androgens and the PI3-K/AKT signaling pathway in governing cell survival...
  86. pmc Inhibition of a Golgi complex lysophospholipid acyltransferase induces membrane tubule formation and retrograde trafficking
    Daniel Drecktrah
    Department of Molecular Biology and Genetics, Cornell University, Ithaca, New York 14853, USA
    Mol Biol Cell 14:3459-69. 2003
    ..These two opposing enzyme activities may help to coordinately regulate Golgi membrane shape and tubule formation...
  87. ncbi Isolation, structure, and absolute stereochemistry of platensimycin, a broad spectrum antibiotic discovered using an antisense differential sensitivity strategy
    Sheo B Singh
    Merck Research Laboratories, P O Box 2000, Rahway, New Jersey 07065, USA
    J Am Chem Soc 128:11916-20. 2006
    ..However, cyclohexenone ring conformation renders for the stronger binding interaction with the enzyme. The isolation, structure elucidation, derivatization, and biological activity of 6,7-dihydroplatensimycin are described...
  88. ncbi A randomized six-day safety study of an antiretroviral microbicide candidate UC781, a non-nucleoside reverse transcriptase inhibitor
    Jill L Schwartz
    CONRAD, Eastern Virginia Medical School, Arlington, Virginia 22209, USA
    Sex Transm Dis 35:414-9. 2008
    ..This study evaluated the effect of a single dose and 5 additional consecutive daily doses of UC781 gel at concentrations of 0.1%, 0.25%, 1.0%, and 0% on urogenital irritation...
  89. pmc The lysophospholipid acyltransferase antagonist CI-976 inhibits a late step in COPII vesicle budding
    William J Brown
    Department of Molecular Biology and Genetics, Cornell University, Ithaca, NY 14853, USA
    Traffic 9:786-97. 2008
    ..These results identify a small molecule inhibitor of a very late step in COPII vesicle formation, consistent with fission inhibition, and demonstrate that this step is likely facilitated by an ER-associated LPAT...
  90. ncbi PPARgamma inhibitors reduce tubulin protein levels by a PPARgamma, PPARdelta and proteasome-independent mechanism, resulting in cell cycle arrest, apoptosis and reduced metastasis of colorectal carcinoma cells
    Katherine L Schaefer
    Section of Gastroenterology and Hepatology, University of Rochester Medical Center, Rochester, NY 14642, USA
    Int J Cancer 120:702-13. 2007
    ..These results suggest that PPARgamma inhibitors are a novel potential antimicrotubule therapy for CRC that acts by directly reducing microtubule precursors...
  91. ncbi A novel vanilloid receptor-1 (VR-1) variant mammalian salt taste receptor
    Vijay Lyall
    Department of Physiology, Virginia Commonwealth University, Richmond, VA 23298 0551, USA
    Chem Senses 30:i42-3. 2005
  92. pmc Ethanol modulates the VR-1 variant amiloride-insensitive salt taste receptor. I. Effect on TRC volume and Na+ flux
    Vijay Lyall
    Department of Physiology, Division of Nephrology, Virginia Commonwealth University, Richmond, VA 23298, USA
    J Gen Physiol 125:569-85. 2005
    ..We conclude that in the presence of mineral salts, ethanol modulates the Bz-insensitive VR-1 variant salt taste receptor...
  93. pmc GW9662, a potent antagonist of PPARgamma, inhibits growth of breast tumour cells and promotes the anticancer effects of the PPARgamma agonist rosiglitazone, independently of PPARgamma activation
    Jill M Seargent
    Cancer Research Unit, Tom Connor s Cancer Research Centre, University of Bradford, All Saints Road, Bradford BD7 1DP, UK
    Br J Pharmacol 143:933-7. 2004
    ..As such, these data support the existence of PPARgamma-independent pathways and question the central belief that PPARgamma ligands mediate their anticancer effects via activation of PPARgamma...
  94. ncbi Dynamics of intracellular movement and nucleocytoplasmic recycling of the ligand-activated androgen receptor in living cells
    R K Tyagi
    Department of Cellular and Structural Biology, The University of Texas Health Science Center at San Antonio, 78284, USA
    Mol Endocrinol 14:1162-74. 2000
    ....
  95. ncbi A unique lysophospholipid acyltransferase (LPAT) antagonist, CI-976, affects secretory and endocytic membrane trafficking pathways
    Kimberly Chambers
    Department of Molecular Biology and Genetics, Cornell University, Ithaca, NY 14853, USA
    J Cell Sci 118:3061-71. 2005
    ....
  96. ncbi Androgen receptor alterations in prostate cancer relapsed during a combined androgen blockade by orchiectomy and bicalutamide
    K Haapala
    Department of Clinical Genetics, Tampere University Hospital, Tampere, Finland
    Lab Invest 81:1647-51. 2001
    ..These data suggest that different AR variants are developed and selected for during various types of hormonal treatments, and also, that CAB achieved by orchiectomy and bicalutamide does not act as a selective force for AR amplification...
  97. ncbi Androgen receptor-mediated repression of novel target genes
    Jennifer Prescott
    Department of Preventive Medicine, Norris Cancer Center, Keck School of Medicine, University of Southern California, Los Angeles, California, USA
    Prostate 67:1371-83. 2007
    ....
  98. ncbi Peroxisome proliferator-activated receptor gamma inhibition prevents adhesion to the extracellular matrix and induces anoikis in hepatocellular carcinoma cells
    Katherine L Schaefer
    Section of Gastroenterology, Boston Medical Center, Boston, MA 02118, USA
    Cancer Res 65:2251-9. 2005
    ..Inhibition of PPARgamma function causes HCC cell death by preventing adhesion and inducing anoikis-mediated apoptosis. PPARgamma inhibitors represent a potential novel treatment approach to HCC...
  99. ncbi Anilides of (R)-trifluoro-2-hydroxy-2-methylpropionic acid as inhibitors of pyruvate dehydrogenase kinase
    G R Bebernitz
    Metabolic and Cardiovascular Disease Research, Novartis Institute for Biomedical Research, Summit, New Jersey 07901, USA
    J Med Chem 43:2248-57. 2000
    ..Nevertheless, they are effective at increasing the utilization and disposal of lactate and could be of utility to ameliorate conditions of inappropriate blood lactate elevation...
  100. ncbi Stress kinase signaling regulates androgen receptor phosphorylation, transcription, and localization
    Daniel Gioeli
    Department of Microbiology, P O Box 800734, University of Virginia Health System, Charlottesville, Virginia 22908, USA
    Mol Endocrinol 20:503-15. 2006
    ..Our data suggest that stress kinase signaling and nuclear export regulate AR transcriptional activity...
  101. ncbi Characterization of a novel CI-976-sensitive lysophospholipid acyltransferase that is associated with the Golgi complex
    Kimberly Chambers
    Department of Molecular Biology and Genetics, Cornell University, Ithaca, NY 14853, USA
    Biochem Biophys Res Commun 313:681-6. 2004
    ..0 and 8.0. These studies further define a unique LPC/LPE-specific LPAT from Golgi membranes that likely has a novel function in membrane trafficking...

Research Grants62

  1. ADAM: Androgen Deprivation vs. Antiandrogen Monotherapy
    Matthew Smith; Fiscal Year: 2004
    ..In addition, this project will provide important insights into the relative contributions of testosterone and estrogen in bone metabolism, and maintenance of muscle size and strength in older men. ..
  2. ACETYLCHOLINESTERASE-CATALYZED HYDROLYSIS
    Daniel Quinn; Fiscal Year: 1991
    ..to study reaction dynamics and virtual transition states for BuChE and (especially) AChE catalyzed hydrolyses of anilides, aryl esters and thiocholine esters...
  3. LIPID CONJUGATES OF XENOBIOTICS
    GHULAM ANSARI; Fiscal Year: 2004
    ..in Aim 4, the mechanism of toxicity of FA conjugates of methanol (FA methyl esters) and aniline (fatty acid anilides) will be evaluated in vivo...
  4. TOTAL SYNTHESIS OF AZADIRACHTIN
    K Nicolaou; Fiscal Year: 2008
    ..The proposed work is expected to impact the general areas of pharmaceutical and agricultural research, and infectious diseases in particular, through discoveries in synthetic organic chemistry and chemical biology. ..
  5. SYNTHESIS OF ANTICANCER AGENTS
    K C Nicolaou; Fiscal Year: 2010
    ..abstract_text> ..
  6. Enabling Technologies for Combinatorial Chemistry
    K Nicolaou; Fiscal Year: 2005
    ..abstract_text> ..
  7. TOTAL SYNTHESIS OF APOPTOLIDIN
    K Nicolaou; Fiscal Year: 2004
    ..The proposed work is expected to have significant impact in the area of cancer chemotherapy and should provide enabling technologies and tools for biology and medicine. ..
  8. TOTAL SYNTHESIS OF NATURAL PRODUCTS
    K Nicolaou; Fiscal Year: 2002
    ..3] sigmatropic rearrangement and a radical based ring closure to form the bicyclic skeleton. ..
  9. 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. ..
  10. 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. ..
  11. 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. ..
  12. 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]..
  13. Poly (ADP-Ribose) synthetase in expression of endothelia
    Basilia Zingarelli; Fiscal Year: 2003
    ..abstract_text> ..
  14. METHODOLOGY FOR THE SYNTHESIS OF NITROGEN HETEROCYCLES
    Philip Magnus; Fiscal Year: 2007
    ..The synthetic intermediates, particularly as they more closely resemble the natural products, will be screened to assess biological activity. [unreadable] [unreadable]..
  15. Cannabinoid Regulation of Basal Ganglia Glutamate and GABA
    SCOTT RAWLS; Fiscal Year: 2007
    ..Our outcomes will be a first step in determining whether blocking endocannabinoid inactivation offers any therapeutic advantage over direct activation of cannabinoid receptors with marijuana. [unreadable] [unreadable] [unreadable]..
  16. Regulation of the von Hippel-Lindau Protein
    Paul Corn; Fiscal Year: 2007
    ..abstract_text> ..
  17. Prosaposin, a novel tumor marker for prostate cancer
    Shahriar Koochekpour; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  18. Mechanistic bases for age-related androgen deficiency
    Johannes Veldhuis; Fiscal Year: 2007
    ..Knowing why testosterone falls should help foster new and safer ways to prevent the problem. [unreadable] [unreadable] [unreadable]..
  19. Ensemble Disruption of the GnRH-LH-Testosterone Axis
    Johannes Veldhuis; Fiscal Year: 2007
    ..Expected corollary outcomes are enhanced diagnosis, assessment and management of more subtle pathophysiology of the male gonadal axis in puberty and adulthood. ..
  20. Deciphering Beta-Catenin Contributions in Prostate Cance
    David Mulholland; Fiscal Year: 2008
    ..These cells will be assessed for growth and PSA secretion in tumours carried as xenografts. These novel in vivo tools will allow understanding to the role of Beta-catenin has in Al PrCa. ..
  21. Epitope mapping by H/D exchange mass spectrometry
    Yoshitomo Hamuro; Fiscal Year: 2008
    ..Establishing a fast, cheap and reliable methodology for the epitope mapping should have a direct impact on the monoclonal antibody therapeutic business. [unreadable] [unreadable] [unreadable]..
  22. 2007 AUA/SBUR Summer Research Conference "Clinical Trials and Outcomes Research"
    David Penson; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  23. Learning and Memory in the Melanocortin System
    Sabrina Diano; Fiscal Year: 2008
    ..abstract_text> ..
  24. Improved Macaque Safety Model for Topical Microbicides: Post-coital Assessments
    Dorothy Patton; Fiscal Year: 2008
    ..In addition, we will collect parallel assessments, when mating has occurred with a placebo gel (HEC universal placebo) in place. These studies will provide urgently needed data regarding topical microbicide use with coital activity. ..
  25. Efficacy of 25-hydroxyvitamin D3 in colon cancer chemoprevention
    Rajendra G Mehta; Fiscal Year: 2010
    ..The studies will provide a rationale for using 25(OH)D3 for the prevention of colon carcinogenesis. ..
  26. Computational Approach to Ligand Discovery for LPA GPCR and PPAR
    Abby L Parrill; Fiscal Year: 2010
    ..This research can therefore lead to new treatments for cardiovascular disease and cancer. ..
  27. MEMBRANE TRAFFICKING IN MAMMALIAN CELLS
    William Brown; Fiscal Year: 2009
    ..These studies will reveal novel biological roles for PLA2 and LPAT enzymes in mediating intracellular trafficking events in the secretory and endocytic pathways. ..
  28. delta-Catenin and Cell-Cell Adhesion in Prostate Cancer
    Qun Lu; Fiscal Year: 2010
    ..Understanding the posttranslational modifications that control 8-catenin functions will unravel mechanisms by which S-catenin modulates gene expression and promotes CaP in vivo. ..
  29. Genetic effectors of TGF-beta induced growth and arrest.
    BEN H PARK; Fiscal Year: 2010
    ..Isolated genes will be verified and validated by restoration of the putative gene and correlated with immunohistochemical studies using tissue microarrays. ..
  30. Farnesyltransferase Inhibitor Therapy for Myelodysplasia
    Razelle Kurzrock; Fiscal Year: 2002
    ....
  31. Hypothalamic Type 2 Deiodinase in Metabolism Regulation
    Sabrina Diano; Fiscal Year: 2005
    ....
  32. PS-341 in Hepatocellular Carcinoma: A Phase II Trial
    Jordan Berlin; Fiscal Year: 2004
    ..abstract_text> ..
  33. Anti-HIV Microbicide: Cellulose Acetate Phthalate (CAP)
    A Robert Neurath; Fiscal Year: 2004
    ..The proposed research is expected to help transform this ideal into a reality. ..
  34. Chronobiological Principles to Maximize Efficacy of Alt*
    Jack Burton; Fiscal Year: 2004
    ..The results of this work will lend itself to (a) future chronobiological studies of other dietary agents for both therapy and chemoprevention and (b) translation of results into clinical trials. ..
  35. IMPACT OF CO-RECEPTOR AND HIV VIRAL BURDEN ON GUT MUCOSA
    Peter Anton; Fiscal Year: 2004
    ..This will be done by looking for decreased mucosal viral burden and evidence of immune reconstitution after therapeutic intervention. ..
  36. SYNTHESIS OF DIAZONAMIDES
    Philip Magnus; Fiscal Year: 2004
    ..Part of the synthetic studies will involve the generation of persistent radical intermediates that should add to pi-deficient heterocycles and form the key central hindered bond present in the diazonamides. ..
  37. Genetic Risk Profiling in Metastatic Prostate Carcinoma
    Adam Kibel; Fiscal Year: 2004
    ..At the conclusion of this study, we will have a panel of markers with the potential to predict, in future prospective studies, which patients are at high risk of eventual death from prostate carcinoma. ..
  38. PATIENT SPECIFIC MODELS IN LUNG CANCER SCREENING WITH CT
    Matthew Brown; Fiscal Year: 2004
    ..4] To compare radiologist accuracy and interpretation times of HR-hCT scans, both with and without assistance from the automated detection system, against pre-existing nodule detection methods. ..
  39. ACTIONS OF ESTROGEN IN MATURING GRAAFIAN FOLLICLES
    Johannes Veldhuis; Fiscal Year: 2005
    ..Understanding such fundamental interactions is important to the rational design of alternative strategies to interrupt normal and rescue impaired steroidogenesis in the maturing Graafian follicle and corpus luteum. ..
  40. IDENTIFICATION OF A 12P PROSTATE TUMOR SUPPRESSOR GENE
    Adam Kibel; Fiscal Year: 2006
    ..The identification of a novel tumor suppressor would provide a target for better prostate cancer therapy and/or more accurate prognostic information for men newly diagnosed with the disease. ..
  41. Survey of oncology providers on psychosocial distress
    William Pirl; Fiscal Year: 2005
    ..abstract_text> ..
  42. Vitamin D5 in Prevention of Mammary Carcinogenesis
    Rajendra Mehta; Fiscal Year: 2006
    ..Whether prohibitin plays a role in cell transformation and chemopreventive efficacy in these cells? 3. How is 1alpha(OH)D5 metabolized in normal and neoplastic mammary epithelial cells and tissues? ..
  43. Delta-Catenin Cleavage by Presenilin and Synaptic Remodeling
    Qun Lu; Fiscal Year: 2006
    ..It will also lay the foundation for future R01 investigation of the roles of delta-catenin proteolytic fragments in AD pathogenesis. ..
  44. Cell Cycle Variants and Metastatic Prostate Cancer Risk
    Adam Kibel; Fiscal Year: 2009
    ..At the conclusion of this study, we will have a panel of markers that can be used to predict which patients are at high risk of treatment failure and eventual death from prostate carcinoma. ..
  45. PPAR gamma Signaling and Lung Fibroblast Transdifferentiation
    Virender Rehan; Fiscal Year: 2009
    ..abstract_text> ..
  46. Role of BAF57 in AR control and prostate cancer growth
    Karen E Knudsen; Fiscal Year: 2010
    ..Together, these studies will reveal the efficacy of BAF57 as a therapeutic target in both early and late stage prostate cancer. ..
  47. 2003 FASEB Summer Conference on Lysophospholipids
    Gabor Tigyi; Fiscal Year: 2003
    ..The conference should provide a contemporary perspective of this rapidly moving field and allow the evaluation of future directions, as well as critical review of recent research. ..
  48. Phase II Trial of Tetrathiomolybdate in Prostate Cancer
    David Smith; Fiscal Year: 2002
    ..The levels of these growth factors/cytokines will then be correlated with the degree of copper depletion, PSA level and response to therapy. ..
  49. Can beta-lactam antibiotics decrease morphine physical dependence?
    SCOTT RAWLS; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  50. Targeting of the Androgen Receptor in Prostate Cancer
    John Isaacs; Fiscal Year: 2005
    ..These peptide prodrugs will be designed so that they are substrates for the enzymatic activity of either Prostate Specific Antigen. ..
  51. Chronochemoprevention of Prostate Cancer
    Jack Burton; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  52. Role of Immunization Site in Eliciting Mucosal Immunity
    Peter Anton; Fiscal Year: 2004
    ....
  53. THE AGING GH AXIS IN POSTMENOPAUSAL WOMEN
    Johannes Veldhuis; Fiscal Year: 2005
    ..An enhanced knowledge base should aid ultimately in formulating more innovative preventive and interventional strategies to limit hyposomatotropism in older and/or estrogen-deficient humans. ..
  54. Novel Active Repressor Model of Human LDL-Receptor Regulation
    Johannes Veldhuis; Fiscal Year: 2008
    ..This would represent a new treatment approach for patients with atherosclerotic disease. [unreadable] [unreadable] [unreadable] [unreadable]..
  55. Analytical Reconstruction of Feedback Signaling in Aging Men
    Johannes Veldhuis; Fiscal Year: 2008
    ..The present proposal develops a general biomathematical framework for dissecting otherwise observed pathways that control hormone output in aging, stress and disease. [unreadable] [unreadable] [unreadable]..
  56. Analysis of Apigenin in Inhibiting Ovarian Tumorigenesis
    Bing Hua Jiang; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  57. Novel Ternary Ligand 99m Tc-Nitrido Complexes as Heart Imaging Agents
    Shuang Liu; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  58. Schizophrenia: Molecular Markers of Disease Progression
    Elizabeth Thomas; Fiscal Year: 2008
    ..Overall, these studies may lead to approaches that will favorably alter the course, treatment and outcome of schizophrenia. ..
  59. PPARGamma in Sepsis-Induced Immunosuppression
    Raju Reddy; Fiscal Year: 2006
    ..abstract_text> ..
  60. 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. ..