Genomes and Genes
Summary: Azoles of two nitrogens at the 1,2 positions, next to each other, in contrast with IMIDAZOLES in which they are at the 1,3 positions.
Publications330 found, 100 shown here
- Role of AMP-activated protein kinase in mechanism of metformin actionG Zhou
Department of Molecular Endocrinology, Merck Research Laboratories, Rahway, New Jersey 07065, USA
J Clin Invest 108:1167-74. 2001..Activation of AMPK provides a unified explanation for the pleiotropic beneficial effects of this drug; these results also suggest that alternative means of modulating AMPK should be useful for the treatment of metabolic disorders...
- JAK inhibition with ruxolitinib versus best available therapy for myelofibrosisClaire Harrison
Guy s and St Thomas National Health Service Foundation Trust, Guy s Hospital, London, United Kingdom
N Engl J Med 366:787-98. 2012..Treatment options for myelofibrosis are limited. We evaluated the efficacy and safety of ruxolitinib, a potent and selective Janus kinase (JAK) 1 and 2 inhibitor, as compared with the best available therapy, in patients with myelofibrosis...
- Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolismPaul B Yu
Cardiovascular Research Center and Division of Cardiology, Department of Medicine, Massachusetts General Hospital, Harvard Medical School, 149 13th Street, Charlestown, Massachusetts 02129, USA
Nat Chem Biol 4:33-41. 2008..These findings suggest an essential physiological role for hepatic BMP signaling in iron-hepcidin homeostasis...
- A double-blind, placebo-controlled trial of ruxolitinib for myelofibrosisSrdan Verstovsek
Leukemia Department, University of Texas M D Anderson Cancer Center, Houston, TX 77030, USA
N Engl J Med 366:799-807. 2012..Ruxolitinib, a selective inhibitor of Janus kinase (JAK) 1 and 2, has clinically significant activity in myelofibrosis...
- Apixaban in patients with atrial fibrillationStuart J Connolly
Population Health Research Institute, McMaster University and Hamilton Health Sciences, Hamilton, ON, Canada
N Engl J Med 364:806-17. 2011..Apixaban, a novel factor Xa inhibitor, may be an alternative treatment for such patients...
- Safety and efficacy of INCB018424, a JAK1 and JAK2 inhibitor, in myelofibrosisSrdan Verstovsek
M D Anderson Cancer Center, Houston, TX 77030, USA
N Engl J Med 363:1117-27. 2010..INCB018424 is a potent and selective Janus kinase 1 (JAK1) and JAK2 inhibitor...
- The JAK2 inhibitor AZD1480 potently blocks Stat3 signaling and oncogenesis in solid tumorsMichael Hedvat
Molecular Medicine, Beckman Research Institute, Irell and Manella Graduate School of Biological Sciences, City of Hope Cancer Center, Duarte, CA 91010, USA
Cancer Cell 16:487-97. 2009..We demonstrate the essential role of Stat3 downstream of Jaks by inhibition of tumor growth using short hairpin RNA targeting Stat3. Our data support a key role of Jak kinase activity in Stat3-dependent tumorigenesis...
- Design of a potent and selective inhibitor of the intermediate-conductance Ca2+-activated K+ channel, IKCa1: a potential immunosuppressantH Wulff
Department of Physiology and Biophysics, University of California, Irvine, CA 92697, USA
Proc Natl Acad Sci U S A 97:8151-6. 2000..A series of pyrazoles, acetonitriles, and tetrazoles were synthesized and found to selectively block IKCa1...
- Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasmsAlfonso Quintas-Cardama
Department of Leukemia, University of Texas M D Anderson Cancer Center, Houston, TX 77030, USA
Blood 115:3109-17. 2010..Preliminary clinical results support these preclinical data and establish INCB018424 as a promising oral agent for the treatment of MPNs...
- Blockade of the intermediate-conductance calcium-activated potassium channel as a new therapeutic strategy for restenosisRalf Köhler
Department of Nephrology, Benjamin Franklin Medical Center, Berlin, Germany
Circulation 108:1119-25. 2003..In a rat model of balloon catheter injury (BCI), we investigated whether alterations in expression of Ca2+-activated K+ channels (KCa) contribute to intimal hyperplasia and vascular restenosis...
- The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancyLee A Honigberg
Pharmacyclics, Sunnyvale, CA 94085 4521, USA
Proc Natl Acad Sci U S A 107:13075-80. 2010..These findings support Btk inhibition as a therapeutic approach for the treatment of human diseases associated with activation of the BCR pathway...
- Bruton tyrosine kinase represents a promising therapeutic target for treatment of chronic lymphocytic leukemia and is effectively targeted by PCI-32765Sarah E M Herman
Integrated Biomedical Science Graduate Program, The Ohio State University Medical Center, Columbus, OH, USA
Blood 117:6287-96. 2011..Based on these collective data, future efforts targeting BTK with the irreversible inhibitor PCI-32765 in clinical trials of CLL patients is warranted...
- Apixaban versus enoxaparin for thromboprophylaxis after hip replacementMichael Rud Lassen
Department of Orthopedics, Spine Clinic, and Clinical Trial Unit, Hørsholm Hospital, University of Copenhagen, Hørsholm, Denmark
N Engl J Med 363:2487-98. 2010..Orally active, specific factor Xa inhibitors such as apixaban may provide effective thromboprophylaxis with a lower risk of bleeding and improved ease of use...
- Celecoxib for the prevention of colorectal adenomatous polypsNadir 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...
- The intermediate-conductance calcium-activated potassium channel KCa3.1 contributes to atherogenesis in mice and humansKazuyoshi Toyama
Department of Medicine and Cardiovascular Center, Medical College of Wisconsin, Milwaukee, Wisconsin 53226, USA
J Clin Invest 118:3025-37. 2008..These data suggest that KCa3.1 blockers represent a promising therapeutic strategy for atherosclerosis...
- Considerations when measuring myocardial perfusion reserve by cardiovascular magnetic resonance using regadenosonNicole M Bhave
Departments of Medicine and Radiology, University of Chicago, Cardiac Imaging Center, Chicago, IL 60637, USA
J Cardiovasc Magn Reson 14:89. 2012..We sought to determine the optimal regadenoson CMR protocol for quantifying myocardial perfusion reserve index (MPRi) - more specifically, whether regadenoson stress imaging should be performed before or after rest imaging...
- Celecoxib versus omeprazole and diclofenac in patients with osteoarthritis and rheumatoid arthritis (CONDOR): a randomised trialFrancis 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...
- Evaluation of the PBR/TSPO radioligand [(18)F]DPA-714 in a rat model of focal cerebral ischemiaAbraham Martin
INSERM U803, Orsay, France
J Cereb Blood Flow Metab 30:230-41. 2010..These results show that [(18)F]DPA-714 provides accurate quantitative information of the time course of PBR/TSPO expression in experimental stroke...
- Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK)J Jean Cui
La Jolla Laboratories, Pfizer Worldwide Research and Development, San Diego, California 92121, USA
J Med Chem 54:6342-63. 2011....
- Applications of small molecule BMP inhibitors in physiology and diseaseCharles C Hong
Division of Cardiovascular Medicine and Center for Inherited Heart Disease, Department of Medicine, Vanderbilt University School of Medicine, Nashville, TN 37232, United States
Cytokine Growth Factor Rev 20:409-18. 2009..We also discuss several potential applications for small molecule BMP inhibitors, including stem cell manipulation, and the therapeutic modification of bone remodeling, heterotopic ossification, and iron homeostasis...
- A peripheral mechanism for CB1 cannabinoid receptor-dependent modulation of feedingRaquel Gomez
University Institute of Drug Dependencies, Department of Psychobiology, University Complutense of Madrid, Madrid 28223, Spain
J Neurosci 22:9612-7. 2002..Pretreatment with SR141716A enhanced the inhibition of feeding induced by intraperitoneal administration of oleoylethanolamide. The results reveal an unexpected role for peripheral CB1 receptors in the regulation of feeding...
- The potential of celecoxib-loaded hydroxyapatite-chitosan nanocomposite for the treatment of colon cancerP 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...
- PHA-739358, a potent inhibitor of Aurora kinases with a selective target inhibition profile relevant to cancerPatrizia Carpinelli
Nerviano Medical Sciences S r l Oncology, Viale Pasteur 10, 20014 Nerviano, Milan, Italy
Mol Cancer Ther 6:3158-68. 2007..We conclude that PHA-739358, which is currently tested in clinical trials, has great therapeutic potential in anticancer therapy in a wide range of cancers...
- Apixaban or enoxaparin for thromboprophylaxis after knee replacementMichael Rud Lassen
Department of Orthopedics, Spine Clinic, Clinical Trial Unit, Hørsholm Hospital, University of Copenhagen, Hørsholm, Denmark
N Engl J Med 361:594-604. 2009..Apixaban, a specific factor Xa inhibitor, may provide effective thromboprophylaxis with a low risk of bleeding and improved ease of use...
- Blockade of T-lymphocyte KCa3.1 and Kv1.3 channels as novel immunosuppression strategy to prevent kidney allograft rejectionI Grgic
Department of Internal Medicine and Nephrology, University Hospital, Philipps University, Marburg, Germany
Transplant Proc 41:2601-6. 2009..Thus, selective blockade of T-lymphocyte K(Ca)3.1 and K(v)1.3 channels may represent a novel alternative therapy for prevention of kidney allograft rejection...
- The cannabinoid CB1 receptor antagonist SR141716 blocks the orexigenic effects of intrahypothalamic ghrelinSonia A Tucci
School of Psychology, University of Liverpool, Eleanor Rathbone Building, Bedford Street South, Liverpool L69 7ZA
Br J Pharmacol 143:520-3. 2004....
- Cyclooxygenase-2 inhibition by celecoxib reduces proliferation and induces apoptosis in angiogenic endothelial cells in vivoKathleen 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...
- Retrograde inhibition of presynaptic calcium influx by endogenous cannabinoids at excitatory synapses onto Purkinje cellsA C Kreitzer
Department of Neurobiology, Harvard Medical School, Boston, MA 02115, USA
Neuron 29:717-27. 2001..DSE may provide a way for cells to use their firing rate to dynamically regulate synaptic inputs. Together with previous studies, these findings suggest a widespread role for endogenous cannabinoids in retrograde synaptic inhibition...
- Apixaban with antiplatelet therapy after acute coronary syndromeJohn H Alexander
Duke Clinical Research Institute, Duke University Medical Center, Durham, NC 27715, USA
N Engl J Med 365:699-708. 2011..Apixaban, an oral, direct factor Xa inhibitor, may reduce the risk of recurrent ischemic events when added to antiplatelet therapy after an acute coronary syndrome...
- Effects of rimonabant on metabolic risk factors in overweight patients with dyslipidemiaJean Pierre Despres
Quebec Heart Institute, Laval Hospital Research Center, and the Division of Kinesiology, Department of Social and Preventive Medicine, Laval University, Ste Foy, Que, Canada
N Engl J Med 353:2121-34. 2005..The Rimonabant in Obesity-Lipids (RIO-Lipids) study examined the effects of rimonabant on metabolic risk factors, including adiponectin levels, in high-risk patients who are overweight or obese and have dyslipidemia...
- Apixaban versus enoxaparin for thromboprophylaxis after knee replacement (ADVANCE-2): a randomised double-blind trialMichael Rud Lassen
Department of Orthopaedics, Spine Clinic, Clinical Trial Unit, Hørsholm Hospital, University of Copenhagen, Hørsholm, Denmark
Lancet 375:807-15. 2010..Apixaban, an orally active factor Xa inhibitor, might be as effective, have lower bleeding risk, and be easier to use than is enoxaparin. We assessed efficacy and safety of these drugs after elective total knee replacement...
- Efficacy and safety of the weight-loss drug rimonabant: a meta-analysis of randomised trialsRobin Christensen
The Parker Institute, Musculoskeletal Statistics Unit, Frederiksberg Hospital, Frederiksberg, Denmark
Lancet 370:1706-13. 2007..We did a meta-analysis of all published randomised controlled trials to assess the efficacy and safety of the newly approved anti-obesity agent rimonabant...
- Celecoxib: a review of its use for symptomatic relief in the treatment of osteoarthritis, rheumatoid arthritis and ankylosing spondylitisPaul L McCormack
Adis, a Wolters Kluwer Business, Auckland, New Zealand
Drugs 71:2457-89. 2011....
- Antagonists selective for estrogen receptor alphaJun Sun
Department of Molecular and Integrative Physiology, University of Illinois and University of Illinois College of Medicine, Urbana, Illinois 61801, USA
Endocrinology 143:941-7. 2002..In this way we have developed basic side-chain pyrazoles (BSC-pyrazoles) that are high affinity, potent, selective antagonists on ER(alpha)...
- The effect of obesity on regadenoson-induced myocardial hyperemia: a quantitative magnetic resonance imaging studyEdward V R DiBella
UCAIR, Department of Radiology, University of Utah, Salt Lake City, UT, USA
Int J Cardiovasc Imaging 28:1435-44. 2012..Fixed dose regadenoson and weight adjusted adenosine produce similar measures of MPR in patients with a wide range of body sizes. Regadenoson is a potentially useful vasodilator for stress MRI studies...
- Identification of N-(4-piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a novel cyclin dependent kinase inhibitor using fragment-based X-ray crystallography and structure based drug designPaul G Wyatt
Astex Therapeutics Ltd, 436 Cambridge Science Park, Milton Road, Cambridge, CB4 0QA, United Kingdom
J Med Chem 51:4986-99. 2008..Optimisation of cellular activity and characterization of pharmacokinetic properties led to the identification of 33 (AT7519), which is currently being evaluated in clinical trials for the treatment of human cancers...
- General Sensitization of melanoma cells for TRAIL-induced apoptosis by the potassium channel inhibitor TRAM-34 depends on release of SMACSandra Annika Quast
Department of Dermatology and Allergy, Skin Cancer Center, University Medical Center Charite, Berlin, Germany
PLoS ONE 7:e39290. 2012..As both TRAIL and IK1 inhibitors had shown only minor side effects in clinical trials, a clinical application of this combination is conceivable...
- Cardiovascular risk and inhibition of cyclooxygenase: a systematic review of the observational studies of selective and nonselective inhibitors of cyclooxygenase 2Patricia 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...
- BMP4 promotes prostate tumor growth in bone through osteogenesisYu Chen Lee
Department of Molecular Pathology, The University of Texas MD Anderson Cancer Center, USA
Cancer Res 71:5194-203. 2011..Treatment of SCID mice bearing MDA-PCa-118b tumors with LDN-193189 significantly reduced tumor growth. Thus, these studies support a role of BMP4-mediated osteogenesis in the progression of prostate cancer in bone...
- Endocannabinoids in the rat basolateral amygdala enhance memory consolidation and enable glucocorticoid modulation of memoryPatrizia Campolongo
Department of Physiology and Pharmacology, Sapienza University of Rome, Piazzale Aldo Moro 5, 00185 Rome, Italy
Proc Natl Acad Sci U S A 106:4888-93. 2009..c.). These findings indicate that endocannabinoids in the BLA enhance memory consolidation and suggest that CB1 activity within this brain region is required for enabling glucocorticoid effects on memory consolidation enhancement...
- Therapeutic potential of AZD1480 for the treatment of human glioblastomaBraden C McFarland
Department of Cell Biology, 1918 University Blvd, MCLM 313, University of Alabama at Birmingham, Birmingham, AL 35294, USA
Mol Cancer Ther 10:2384-93. 2011....
- Phase II, randomized, placebo-controlled trial of neoadjuvant celecoxib in men with clinically localized prostate cancer: evaluation of drug-specific biomarkersEmmanuel 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...
- Adenosine versus regadenoson comparative evaluation in myocardial perfusion imaging: results of the ADVANCE phase 3 multicenter international trialAmi E Iskandrian
University of Alabama at Birmingham, Birmingham, AL 35294 0006, USA
J Nucl Cardiol 14:645-58. 2007..Earlier phase 1 and 2 studies have shown that regadenoson has desirable features as a stress agent for myocardial perfusion imaging...
- In vivo structure-activity relationship study of dorsomorphin analogues identifies selective VEGF and BMP inhibitorsJijun Hao
Division of Cardiovascular Medicine, Department of Medicine, Vanderbilt University School of Medicine, Nashville, Tennessee 37232, USA
ACS Chem Biol 5:245-53. 2010....
- Modulation of anxiety through blockade of anandamide hydrolysisSatish Kathuria
Department of Pharmacology, University of California, Irvine, California, USA
Nat Med 9:76-81. 2003..Our results indicate that anandamide participates in the modulation of emotional states and point to fatty acid amide hydrolase inhibition as an innovative approach to anti-anxiety therapy...
- Comparative pharmacodynamics and pharmacokinetics of oral direct thrombin and factor xa inhibitors in developmentBengt I Eriksson
Orthopaedics Department, University Hospital Sahlgrenska Ostra, Gothenburg, Sweden
Clin Pharmacokinet 48:1-22. 2009..Here, we compare the pharmacokinetic and pharmacodynamic features of these new oral agents...
- Clinical and pharmacodynamic evaluation of metronomic cyclophosphamide, celecoxib, and dexamethasone in advanced hormone-refractory prostate cancerAndrea Fontana
Division of Medical Oncology, Azienda USL 6 of Livorno, Italy
Clin Cancer Res 15:4954-62. 2009..v. standard dose of cyclophosphamide (CTX) immediately followed by an oral metronomic CTX regimen with celecoxib (CXB) and dexamethasone (DEX) in advanced hormone-refractory prostate cancer patients...
- Tachycardia caused by A2A adenosine receptor agonists is mediated by direct sympathoexcitation in awake ratsArvinder K Dhalla
Department of Pharmacology, CV Therapeutics, Palo Alto, CA 94304, USA
J Pharmacol Exp Ther 316:695-702. 2006....
- Targeting the replication checkpoint using SCH 900776, a potent and functionally selective CHK1 inhibitor identified via high content screeningTimothy J Guzi
Merck Research Laboratory, Cambridge, Masachusetts, USA
Mol Cancer Ther 10:591-602. 2011..SCH 900776 exposure phenocopies short interfering RNA-mediated CHK1 ablation and interacts synergistically with DNA antimetabolite agents in vitro and in vivo to selectively induce dsDNA breaks and cell death in tumor cell backgrounds...
- Phase II trial of celecoxib in prostate-specific antigen recurrent prostate cancer after definitive radiation therapy or radical prostatectomyRaj 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...
- Endocannabinoid control of food intake and energy balanceVincenzo Di Marzo
Endocannabinoid Research Group, Institute of Biomolecular Chemistry, Consiglio Nazionale delle Ricerche, Via Campi Flegrei 34, 80078, Pozzuoli, Naples, Italy
Nat Neurosci 8:585-9. 2005..Here we discuss the multifaceted regulation of energy homeostasis by endocannabinoids, together with its applications to the treatment of eating disorders and metabolic syndromes...
- Maximal COX-2 immunostaining and clinical response to celecoxib and interferon alpha therapy in metastatic renal cell carcinomaBrian 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...
- Small molecule modulation of Smoothened activityJames K Chen
Department of Molecular Biology and Genetics, Howard Hughes Medical Institute, Johns Hopkins University School of Medicine, Baltimore, MD 21205, USA
Proc Natl Acad Sci U S A 99:14071-6. 2002..The mechanistic differences between the Smo antagonists may be useful in the therapeutic manipulation of Hh signaling...
- Cardiovascular risk of celecoxib in 6 randomized placebo-controlled trials: the cross trial safety analysisScott D Solomon
Cardiovascular Division, Brigham and Women s Hospital, 75 Francis St, Boston, MA 02115, USA
Circulation 117:2104-13. 2008..Our aim was to assess the cardiovascular risk associated with celecoxib in 3 dose regimens and to assess the relationship between baseline cardiovascular risk and effect of celecoxib on cardiovascular events...
- Cardiovascular risk associated with celecoxib in a clinical trial for colorectal adenoma preventionScott D Solomon
Cardiovascular Division, Department of Medicine, Brigham and Women s Hospital, Harvard Medical School, Boston, MA 02115, USA
N Engl J Med 352:1071-80. 2005..Experimental research suggesting that these drugs may contribute to a prothrombotic state provides support for this concern...
- The novel NF-κB inhibitor DHMEQ synergizes with celecoxib to exert antitumor effects on human liver cancer cells by a ROS-dependent mechanismNadia Lampiasi
Institute of Biomedicine and Molecular Immunology Alberto Monroy, National Research Council, Palermo, Italy
Cancer Lett 322:35-44. 2012..These data suggest that the DHMEQ-CLX combination kills hepatoma cells via ROS production, ER stress response and the activation of intrinsic and extrinsic apoptotic pathways...
- Apixaban metabolism and pharmacokinetics after oral administration to humansNirmala Raghavan
Pharmaceutical Candidate Optimization, Bristol Myers Squibb Research and Development, Princeton, New Jersey 08543 4000, USA
Drug Metab Dispos 37:74-81. 2009..Thus, apixaban is an orally bioavailable inhibitor of factor Xa with elimination pathways that include metabolism and renal excretion...
- The neuroblastoma-associated F1174L ALK mutation causes resistance to an ALK kinase inhibitor in ALK-translocated cancersTakaaki Sasaki
Lowe Center for Thoracic Oncology, Dana Farber Cancer Institute, D820, 44 Binney Street, Boston, MA 02115, USA
Cancer Res 70:10038-43. 2010..Our findings highlight the importance of studying drug resistance mechanisms in order to develop effective clinical treatments for patients with ALK-translocated cancers...
- Inhibition of the Ca²⁺-dependent K⁺ channel, KCNN4/KCa3.1, improves tissue protection and locomotor recovery after spinal cord injuryDelphine Bouhy
Centre for Research in Neuroscience, The Research Institute of the McGill University Health Center, Montreal, Quebec H3G1A4, Canada
J Neurosci 31:16298-308. 2011..These results suggest that blocking the KCa3.1 channel could be a potential therapeutic approach for treating secondary damage after spinal cord injury...
- Clinical laboratory measurement of direct factor Xa inhibitors: anti-Xa assay is preferable to prothrombin time assayYu Chen Barrett
Bristol Myers Squibb, Princeton, New Jersey, USA
Thromb Haemost 104:1263-71. 2010..88-0.89) compared with PT/INR (r2 = 0.36) in patients undergoing VTE treatment suggested that anti-Xa activity was the better indicator of apixaban plasma concentrations...
- Apixaban, an oral, direct and highly selective factor Xa inhibitor: in vitro, antithrombotic and antihemostatic studiesP C Wong
Thrombosis Research, Bristol Myers Squibb Company, Pennington, NJ 08534, USA
J Thromb Haemost 6:820-9. 2008..Apixaban is an oral, direct and highly selective factor Xa (FXa) inhibitor in late-stage clinical development for the prevention and treatment of thromboembolic diseases...
- Efficacy and safety of the oral direct factor Xa inhibitor apixaban for symptomatic deep vein thrombosis. The Botticelli DVT dose-ranging studyH Buller
Department of Vascular Medicine, Academic Medical Centre, University of Amsterdam, Amsterdam, The Netherlands
J Thromb Haemost 6:1313-8. 2008..We conducted a dose-ranging study in patients with deep vein thrombosis...
- Riociguat for chronic thromboembolic pulmonary hypertension and pulmonary arterial hypertension: a phase II studyH A Ghofrani
Dept of Internal Medicine, Medical Clinic II V, University Hospital Giessen and Marburg GmbH, Klinikstrasse 36, 35392 Giessen, Germany
Eur Respir J 36:792-9. 2010..These preliminary data show that riociguat has a favourable safety profile and improves exercise capacity, symptoms and pulmonary haemodynamics in CTEPH and PAH. Randomised controlled trials are underway...
- NO-independent regulatory site on soluble guanylate cyclaseJ P Stasch
Pharma Research Center, Bayer AG, Aprather Wey 18a, D 42096 Wuppertal, Germany
Nature 410:212-5. 2001..This results in antiplatelet activity, a strong decrease in blood pressure and an increase in survival in a low-NO rat model of hypertension, and as such may offer an approach for treating cardiovascular diseases...
- Comparative evaluation of the translocator protein radioligands 11C-DPA-713, 18F-DPA-714, and 11C-PK11195 in a rat model of acute neuroinflammationFabien Chauveau
CEA, DSV, I2BM, LIME, Orsay, France
J Nucl Med 50:468-76. 2009....
- PHA-680632, a novel Aurora kinase inhibitor with potent antitumoral activityChiara Soncini
Nerviano Medical Sciences S r l Oncology, Milan, Italy
Clin Cancer Res 12:4080-9. 2006..The aim of this study was to determine the preclinical profile of a novel, highly selective Aurora kinase inhibitor, PHA-680632, as a candidate for anticancer therapy...
- Inhibition of bone morphogenetic protein signaling attenuates anemia associated with inflammationAndrea U Steinbicker
Department of Anesthesia, Harvard Medical School, Boston, MA, USA
Blood 117:4915-23. 2011..Our studies support the concept that BMP and IL-6 act together to regulate iron homeostasis and suggest that inhibition of BMP signaling may be an effective strategy for the treatment of anemia of inflammation...
- Cannabinoid receptor 1 (CB1) antagonism enhances glucose utilisation and activates brown adipose tissue in diet-induced obese miceM Bajzer
Metabolic Diseases Institute, University of Cincinnati, 2140 East Galbraith Road, Building B, Room 332, Cincinnati, OH 45237 1625, USA
Diabetologia 54:3121-31. 2011....
- Preclinical pharmacokinetics and pharmacodynamics of apixaban, a potent and selective factor Xa inhibitorKan He
Pharmaceutical Candidate Optimization, Bristol Myers Squibb Company, Princeton, NJ, USA
Eur J Drug Metab Pharmacokinet 36:129-39. 2011..3 μM for dog. Apixaban exhibits desirable PK and PD properties for clinical development with good oral bioavailability, small Vd, low CL, and direct, predictable, concentration-dependent PD responses...
- Structure-activity relationship study of bone morphogenetic protein (BMP) signaling inhibitorsGregory D Cuny
Laboratory for Drug Discovery in Neurodegeneration, Harvard NeuroDiscovery Center, Brigham and Women s Hospital and Harvard Medical School, 65 Landsdowne Street, Cambridge, MA 02139, USA
Bioorg Med Chem Lett 18:4388-92. 2008..g., plasma t(1/2)=1.6h) following intraperitoneal administration in mice. These studies provide useful molecular probes for examining the in vivo pharmacology of BMP signaling inhibition...
- Acute cannabinoid receptor type 1 (CB1R) modulation influences insulin sensitivity by an effect outside the central nervous system in miceD Song
Department of Medicine, University of Toronto, Toronto, ON, Canada
Diabetologia 54:1181-9. 2011..Here we examined the relative contributions of acute CNS and extra-CNS CB1R modulation on insulin sensitivity using pharmacological gain- and loss-of-function of CB1R in mice...
- Reduced PBR/TSPO expression after minocycline treatment in a rat model of focal cerebral ischemia: a PET study using [(18)F]DPA-714Abraham Martin
CEA, DSV, I BM, SHFJ, Laboratoire Imagerie Moléculaire Expérimentale, INSERM U803, 4 Place Géneral Leclerc, 91406 Orsay Cedex, France
Mol Imaging Biol 13:10-5. 2011..This overexpression can be imaged with positron emission tomography (PET) using PBR/TSPO-selective radioligands such as [(18)F]DPA-714...
- Phase I and pharmacologic trial of cytosine arabinoside with the selective checkpoint 1 inhibitor Sch 900776 in refractory acute leukemiasJudith E Karp
Division of Hematologic Malignancies, Johns Hopkins Sidney Kimmel Comprehensive Cancer Center, The Johns Hopkins Hospital, Baltimore, Maryland 21287, USA
Clin Cancer Res 18:6723-31. 2012..To extend these findings to the clinical setting, we have conducted a phase I study of cytarabine and SCH 900776...
- Cannabinoid type-1 receptor reduces pain and neurotoxicity produced by chemotherapyIryna A Khasabova
Department of Diagnostic and Biological Sciences, University of Minnesota, Minneapolis, Minnesota 55455, USA
J Neurosci 32:7091-101. 2012..Collectively, these results suggest that pharmacological facilitation of AEA signaling is a promising strategy for attenuating cisplatin-associated sensory neuropathy...
- COX-2 as a target for cancer chemotherapyNilanjan Ghosh
Dr B C Roy College of Pharmacy and Allied Health Sciences, Durgapur, India
Pharmacol Rep 62:233-44. 2010..Thus, it appears that targeting the COX-2 pathway is a promising strategy in the prevention and treatment of solid tumors...
- Effect of the AMP-kinase modulators AICAR, metformin and compound C on insulin secretion of INS-1E rat insulinoma cells under standard cell culture conditionsChristian Langelueddecke
Institute of Physiology and Pathophysiology, Paracelsus Medical University, Salzburg, Austria
Cell Physiol Biochem 29:75-86. 2012....
- Preclinical development of the novel Chk1 inhibitor SCH900776 in combination with DNA-damaging agents and antimetabolitesRyan Montano
Department of Pharmacology and Toxicology, Dartmouth Medical School, Lebanon, New Hampshire, USA
Mol Cancer Ther 11:427-38. 2012..Delayed administration of SCH900776 may be more effective than concurrent treatment. SCH900776 is currently in phase I clinical trials, and these results provide the rationale and schedule for future clinical trials...
- Synergistic effects of p38 mitogen-activated protein kinase inhibition with a corticosteroid in alveolar macrophages from patients with chronic obstructive pulmonary diseaseJ Armstrong
Medicines Evaluation Unit, National Institute for Health Research Translational Research Facility, University Hospital of South Manchester Foundation Trust, University of Manchester, Manchester, United Kingdom
J Pharmacol Exp Ther 338:732-40. 2011..Combining a p38 MAPK inhibitor with a corticosteroid synergistically enhances the anti-inflammatory effects on LPS-mediated cytokine production by alveolar macrophages from patients with COPD and controls...
- Death receptor regulation and celecoxib-induced apoptosis in human lung cancer cellsXiangguo Liu
Winship Cancer Institute, Emory University School of Medicine, Atlanta, GA 30322, USA
J Natl Cancer Inst 96:1769-80. 2004..We investigated the mechanism of celecoxib-induced apoptosis further...
- Ibrutinib as initial therapy for elderly patients with chronic lymphocytic leukaemia or small lymphocytic lymphoma: an open-label, multicentre, phase 1b/2 trialSusan O'Brien
Department of Leukemia, The University of Texas MD Anderson Cancer Center, Houston, TX, USA Electronic address
Lancet Oncol 15:48-58. 2014..We aimed to assess safety and activity of ibrutinib, an orally administered covalent inhibitor of Bruton tyrosine kinase (BTK), in treatment-naive patients aged 65 years and older with chronic lymphocytic leukaemia...
- Long-term outcomes of 107 patients with myelofibrosis receiving JAK1/JAK2 inhibitor ruxolitinib: survival advantage in comparison to matched historical controlsSrdan Verstovsek
Department of Leukemia, The University of Texas MD Anderson Cancer Center, Houston, TX 77030, USA
Blood 120:1202-9. 2012....
- Compound C prevents the unfolded protein response during glucose deprivation through a mechanism independent of AMPK and BMP signalingSakae Saito
Cancer Chemotherapy Center, Japanese Foundation for Cancer Research, Tokyo, Japan
PLoS ONE 7:e45845. 2012..Our findings demonstrate that compound C could be a unique tool for developing a UPR-targeted antitumor therapy...
- Dual blockade of the EGFR and COX-2 pathways: a phase II trial of cetuximab and celecoxib in patients with chemotherapy refractory metastatic colorectal cancerEmily Chan
Vanderbilt University Medical Center, Department of Veterans Affairs, Nashville, TN, USA
Am J Clin Oncol 34:581-6. 2011..This study explores the clinical and biological effects of combined blockade of these pathways...
- Peripheral endocannabinoid system-mediated actions of rimonabant on growth hormone secretion are ghrelin-dependentO Al-Massadi
Instituto de Investigaciones Sanitarias, Complejo Hospitalario Universitario de Santiago de Compostela, SERGAS, Santiago de Compostela, Spain
J Neuroendocrinol 22:1127-36. 2010..In conclusion, the data reported in the present study establish, from a physiological point of view, the existence of a novel mechanism of GH regulation implicating the action of the cannabinoid receptor on the somatotroph axis...
- Cyclooxygenase-2 promotes hepatocellular carcinoma cell growth through Akt activation: evidence for Akt inhibition in celecoxib-induced apoptosisJing Leng
Department of Pathology, University of Pittsburgh School of Medicine, Pittsburgh, PA, USA
Hepatology 38:756-68. 2003..01). In conclusion, our results suggest the involvement of COX-2-dependent and -independent mechanisms in celecoxib-mediated HCC cell apoptosis...
- Eltrombopag for management of chronic immune thrombocytopenia (RAISE): a 6-month, randomised, phase 3 studyGregory Cheng
Chinese University of Hong Kong, Shatin, NT, Hong Kong SAR, China
Lancet 377:393-402. 2011..We aimed to compare the response to once daily eltrombopag versus placebo in patients with chronic immune thrombocytopenia during a 6-month period...
- MK1775, a selective Wee1 inhibitor, shows single-agent antitumor activity against sarcoma cellsJenny M Kreahling
Experimental Therapeutics Program, H Lee Moffitt Cancer Center and Research Institute, Tampa, Florida 33612, USA
Mol Cancer Ther 11:174-82. 2012..Finally, in patient-derived sarcoma samples, we showed that MK1775 as a single agent causes significant apoptotic cell death, suggesting that Wee1 inhibition may represent a novel approach in the treatment of sarcomas...
- COX-2 inhibitor celecoxib prevents chronic morphine-induced promotion of angiogenesis, tumour growth, metastasis and mortality, without compromising analgesiaM Farooqui
1Division of Hematology, Oncology and Transplantation, the Vascular Biology Center, Department of Medicine, University of Minnesota, Minneapolis, MN 55455, USA
Br J Cancer 97:1523-31. 2007..In fact, the combination provided significantly better analgesia than with morphine or celecoxib alone. Clinical trials of this combination for analgesia in chronic and severe pain in cancer are warranted...
- Pharmacological suppression of hepcidin increases macrophage cholesterol efflux and reduces foam cell formation and atherosclerosisOmar Saeed
Emory University Hospital Midtown, 550 Peachtree St NE, Atlanta, GA 30308, USA
Arterioscler Thromb Vasc Biol 32:299-307. 2012..In this study, we explored whether reducing macrophage intracellular iron levels via pharmacological suppression of hepcidin can increase macrophage-specific expression of cholesterol efflux transporters and reduce atherosclerosis...
- Structure-activity relationships and X-ray structures describing the selectivity of aminopyrazole inhibitors for c-Jun N-terminal kinase 3 (JNK3) over p38Ted Kamenecka
Department of Molecular Therapeutics and Translational Research Institute, The Scripps Research Institute, Jupiter, FL 33458, USA
J Biol Chem 284:12853-61. 2009....
- Rationale, design, and governance of Prospective Randomized Evaluation of Celecoxib Integrated Safety versus Ibuprofen Or Naproxen (PRECISION), a cardiovascular end point trial of nonsteroidal antiinflammatory agents in patients with arthritisMatthew C Becker
Department of Cardiology, Cleveland Clinic Foundation, OH 44195, USA
Am Heart J 157:606-12. 2009..Pain management in patients with osteoarthritis or rheumatoid arthritis often requires long-term use of nonsteroidal antiinflammatory drugs (NSAIDs). However, the relative cardiovascular safety of these therapies remains uncertain...
- CH223191 is a ligand-selective antagonist of the Ah (Dioxin) receptorBin Zhao
Department of Environmental Toxicology, University of California, Davis, California 95616 8588, USA
Toxicol Sci 117:393-403. 2010....
- Targeted inhibition of activin receptor-like kinase 5 signaling attenuates cardiac dysfunction following myocardial infarctionSih Min Tan
Department of Medicine, St Vincent s Hospital, 29 Regent St, Fitzroy, Victoria 3065, Australia
Am J Physiol Heart Circ Physiol 298:H1415-25. 2010....
- Identification and characterization of the first small molecule inhibitor of MDMXDamon Reed
Department of Developmental Neurobiology, St Jude Children s Research Hospital, Memphis, Tennessee 38105, USA
J Biol Chem 285:10786-96. 2010..When combined with selective MDM2 inhibitors, SJ-172550 may also be useful for treating tumors that express wild-type p53...
- Receptors and channels targeted by synthetic cannabinoid receptor agonists and antagonistsR G Pertwee
Institute of Medical Sciences, University of Aberdeen, Foresterhill, Scotland, UK
Curr Med Chem 17:1360-81. 2010..It begins with a brief description of how each of these ligands interacts with CB(1) and/or CB(2) receptors...
- Cyclooxygenase-2 pathway correlates with VEGF expression in head and neck cancer. Implications for tumor angiogenesis and metastasisO Gallo
Department of Oto Neuro Ophthalmologic Surgery, University of Florence, 50139 Florence, Italy
Neoplasia 3:53-61. 2001..This study suggests a central role of COX-2 pathway in HNC angiogenesis by modulating VEGF production and indicates that COX-2 inhibitors may be useful in HNC treatment...
- QSAR analysis for some diaryl-substituted pyrazoles as CCR2 inhibitors by GA-stepwise MLRLotfollah Saghaie
Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, Iran
Chem Biol Drug Des 77:75-85. 2011Quantitative relationships between calculated molecular structure and 26 diaryl-substituted pyrazoles CCR2 inhibitors were investigated by GA-stepwise multiple linear regression...
- Phase II nonrandomized study of the efficacy and safety of COX-2 inhibitor celecoxib on patients with cancer cachexiaGiovanni Mantovani
Department of Medical Oncology, University of Cagliari, Cagliari, Italy
J Mol Med (Berl) 88:85-92. 2010..Therefore, phase III clinical trials are warranted to test the efficacy and safety of celecoxib...
- A small-molecule modulator interacts directly with deltaPhe508-CFTR to modify its ATPase activity and conformational stabilityLeigh Wellhauser
Research Institute, Hospital for Sick Children and Departments of Biochemistry and Physiology, University of Toronto, Canada
Mol Pharmacol 75:1430-8. 2009..These findings suggest that direct binding of this small molecule induces and/or stabilizes a structure that promotes the channel open state and may underlie its efficacy as a corrector of DeltaPhe508-CFTR...
- Crizotinib in ALK-rearranged inflammatory myofibroblastic tumorJames E Butrynski
Dana Farber Cancer Institute, Boston, MA 02115, USA
N Engl J Med 363:1727-33. 2010..Funded by Pfizer and others; ClinicalTrials.gov number, NCT00585195.)...
- Therapeutic strategies to overcome crizotinib resistance in non-small cell lung cancers harboring the fusion oncogene EML4-ALKRyohei Katayama
Massachusetts General Hospital Cancer Center, Boston, MA 02129, USA
Proc Natl Acad Sci U S A 108:7535-40. 2011..Thus, we have developed a model of acquired resistance to ALK inhibitors and have shown that second-generation ALK TKIs or Hsp90 inhibitors are effective in treating crizotinib-resistant tumors harboring secondary gatekeeper mutations...
- Synthesis of Medicinally Important HeterocyclesRICHARD LAROCK; Fiscal Year: 2007..benzopyrans, chromones and heteroatom analogues, furans, thiophenes, pyrroles, oxazoles, isoxazoles, pyrazoles, pyridines, quinolines, coumarins, indenes, indenones, naphthols, and phenols...
- Phase II Environmentally greener, efficient, and safe synthetic platform for thePAUL MATTHEW HERRINTON; Fiscal Year: 2011..portfolio of borylated pyridine derivatives and add quinolines, pyrazines, pyrimidines, diazenes, imidazoles, pyrazoles, oxazoles, etc. Produce oxidized products (e.g. hydroxyquinolines) where applicable. 2...
- Molecular Pathways Targeted by Potent Antimalarial Pyrazole CompoundsAkhil B Vaidya; Fiscal Year: 2013..Recent studies suggest that pyrazoles and another series of potent antimalarials, spiroindolones, may be working through a common pathway...
- NMR/COMPUTER MODELING FOR CANNABINOID LIGAND DESIGNXiang Qun Xie; Fiscal Year: 2002..to three known cannabimimetic groups, namely arachidonylethanolamides (AEAs), aminoalkylindoles (AAIs), and pyrazoles (PRZs) will be studied using NMR methods and then refined using computer modeling approaches...
- Apoptosis in myelofibrosis with myeloid metaplasiaRuben Mesa; Fiscal Year: 2006..abstract_text> ..
- Developmental Psychopharmacology of AntipsychoticsJENNY WILEY; Fiscal Year: 2007..This information will help to provide a more rational basis for making treatment decisions concerning children and adolescents who may benefit from treatment with an antipsychotic. [unreadable] [unreadable]..
- CB1 Receptors: Cocaine Reinforcement and RelapseSara Ward; Fiscal Year: 2007..The second goal is to employ this set of procedures to assess the role of the CB1 receptor system in cocaine's reinforcing effects and relapse to cocaine seeking. ..
- Proteomics and Biomarkers for Hepatocellular CancerNezam Afdhal; Fiscal Year: 2004..These studies may lead to identification of more specific and sensitive biomarkers for HCC in HCV which can then be validated further in prospective clinical trials. ..
- Antiviral Therapy in African Americans with HCVNezam Afdhal; Fiscal Year: 2005..Specimens of liver tissue and serum will be collected for basic studies on viral resistance. These studies should help determine the best therapy for AA with HCV. ..
- "Post-partum steroid withdrawal-induced depression"REBECCA CRAFT; Fiscal Year: 2006..Findings from the proposed model will enhance our understanding of the etiology of PPD and possibly lead to improved treatment options. ..
- Improving Contraceptive Effectiveness in Obese WomenAlison B Edelman; Fiscal Year: 2010..abstract_text> ..
- PROTEIN LIPID INTERACTIONS IN GALLSTONE PATHOGENESISNezam Afdhal; Fiscal Year: 2002..These studies may lead to strategies for the prevention and non-surgical therapy of this very common disease. ..
- Drug discrimination and THC withdrawal in monkeysLANCE MCMAHON; Fiscal Year: 2005..abstract_text> ..
- Pharmacotherapy of Cannabinoid Withdrawal: Pre-Clinical StudiesLance R McMahon; Fiscal Year: 2010..Collectively, these specific aims provide a framework for developing novel pharmacotherapies of marijuana withdrawal that could markedly decrease marijuana use and dependence. ..
- Contraceptive efficacy and body weight: Does obesity affect the risk of failure?Alison Edelman; Fiscal Year: 2007..unreadable] [unreadable] [unreadable]..
- Breast Cancer Prediction Using Nipple Aspirate FluidEdward Sauter; Fiscal Year: 2007..unreadable] [unreadable]..
- Protein Profiling in Nipple Aspirate FluidEdward Sauter; Fiscal Year: 2007..abstract_text> ..
- REGULATION OF SECRETION FROM HUMAN BASOPHILSDonald MacGlashan; Fiscal Year: 2009..A population of subjects will be examined for this relationship. ..
- The Effect of Black Cohosh Extract on the Human BreastEdward Sauter; Fiscal Year: 2004..The findings should allow us to design a high quality R01 submission involving a larger, randomized study of longer duration which should provide some answers on the potential role of BCE in breast cancer. ..
- HYPOXIC STRESS MECHANISMS IN RADIATION AND CHEMOTHERAPYKeith Laderoute; Fiscal Year: 2009..An understanding of these MTF-1-dependent properties should aid in the development of novel prognostic and new modalities for neoplastic diseases. ..
- NABTC - M.D. Anderson Clinical CenterMark Gilbert; Fiscal Year: 2008..The NABTC continues with the long-term goal of developing more effective treatments for patients with primary brain tumors, particularly malignant gliomas, combining longevity with the quality of survival. ..
- Sex Differences in Endocannabioid-Mediated BehaviorsChristian Reich; Fiscal Year: 2008..Fear conditioning will be performed with established classical-conditioning protocols. [unreadable] [unreadable]..
- Strengthening Botanical CAM Research: A Collaboration between CUNY and ColumbiaEdward 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. ..
- Symposium on Aldo-Keto Reductases & Toxicant MetabolismTREVOR PENNING; Fiscal Year: 2002..abstract_text> ..
- DRUGS AND DEVELOPMENT OF THE ADRENERGIC NERVOUS SYSTEMTheodore Slotkin; Fiscal Year: 2003....
- DNA and Phytochemical Fingerprinting of Actaea SpeciesEdward 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. ..
- Cell Survival Pathways and Inhibitors in LeukemiaAlan Eastman; Fiscal Year: 2003....
- The Role of Adenosine in Chronic Ischemic CardiomyopathyDAI TRANG LE; Fiscal Year: 2007..Joel Linden who is an authority on the role of adenosine in cardiovascular physiology and pharmacology. ..
- Periodontal Assessment in RA Study (PARAS)Clifton Bingham; Fiscal Year: 2007..unreadable] [unreadable] [unreadable] [unreadable]..
- Reproductive Consequences of Pubertal Morphine AbuseElizabeth Byrnes; Fiscal Year: 2002....
- Prenatal Cannabis Effect on the Endocannabinoid SystemVINOD YARAGUDRI; Fiscal Year: 2008..unreadable] [unreadable] [unreadable]..
- Predictive Markers of Glioblastoma Response to VEGF TrapJohn de Groot; Fiscal Year: 2008..unreadable] [unreadable] [unreadable]..
- 131 I-MIBG Escalating Dose Rapid Sequence Double Infusi*Katherine Matthay; Fiscal Year: 2004..Significance: The higher tumor-specific radiation doses possible with this protocol may provide a treatment to improve response and survival in children with resistant neuroblastoma. ..
- PHASE I TRIALS OF ANTICANCER AGENTSMartin Edelman; Fiscal Year: 2002....
- DESIGN AND SYNTHESIS OF NONPEPTIDE PROTEASE INHIBITORSArun 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. ..
- BEHAVIORAL TOXICITY OF MDMA IN RHESUS MONKEYSMICHAEL TAFFE; Fiscal Year: 2009..Specific Aim IV: To determine if a history of MDMA exposure impairs acquisition and performance of a battery of neuropsychological tests. ..
- NEUROPHARMACOLOGY OF PRIMATE COGNITIONMICHAEL TAFFE; Fiscal Year: 2002..abstract_text> ..
- Semiparametric ROC Curve Regression for Cancer Screening StudiesXiaofei Wang; Fiscal Year: 2008..With a growing interest in rigorous validation of screening tests for cancer and other diseases, the proposed methods may end broad usage. [unreadable] [unreadable] [unreadable]..
- AhR and reproductive agingBRIAN PETROFF; Fiscal Year: 2008..This project will provide crucial knowledge for the identification and prevention of infertility and birth defects due to the AhR pathway in older mothers. [unreadable] [unreadable] [unreadable]..
- TOXICOLOGY OF ENVIRONMENT CONTAMINANTSStephen Safe; Fiscal Year: 2007..The proposed training program will continue to provide trainees with a challenging academic and research environment that will prepare them for future careers in academic, industry and government. ..
- Inhibition of Pancreatic Cancer by New PPARgamma Agonis*Stephen Safe; Fiscal Year: 2008..PPAR? -active C-substituted DIMs that inhibit pancreatic cancer cell growth in vitro and in vivo, and these will serve as lead compounds for development of new drugs for clinical treatment of this devastating disease ..
- Serine-Protease Effects on the Epithelial Sodium ChannelRay Caldwell; Fiscal Year: 2006..Collectively, these components will be vital for him to emerge as an independent investigator [unreadable] [unreadable]..
- Regulation of Mammalian Oocyte MaturationStephen Downs; Fiscal Year: 2007..Furthermore, these studies will benefit the development of in vitro systems where either meiotic arrest or completion of meiotic maturation is the desired endpoint. ..
- Phase I Trial of Safingol and CisplatinGary Schwartz; Fiscal Year: 2006..conduct "proof of principle" biological assays to measure the degree of ceramide production and/or S1P inhibition, either of which may be predictive of clinical outcome or toxicity. ..
- MECHANISMS OF CHLORPYRIFOS DEVELOPMENTAL NEUROTOXICITYTheodore Slotkin; Fiscal Year: 2004..Molecular mechanisms of developmental neurotoxicity can be determined and linked to eventual alterations in behavioral performance. ..
- Coactivation of Estrogen Receptor alpha/Sp1Stephen Safe; Fiscal Year: 2006..abstract_text> ..
- Identification of Alcohol Binding Site(s) in Protein Kinase C EpsilonJoydip Das; Fiscal Year: 2007..unreadable] [unreadable] [unreadable]..
- FORMAL METHODS APPLIED TO BIOLOGICAL SIGNALING NETWORKSKeith Laderoute; Fiscal Year: 2006..abstract_text> ..
- Calcium entry and vascular smooth muscle excitationKENNETH BYRON; Fiscal Year: 2006..abstract_text> ..
- ETHANOL EFFECTS ON BONE FORMATION IN PREGNANCYMartin Ronis; Fiscal Year: 2006..The role of CYP2E1 and free radicals in the skeletal toxicity of ethanol during these periods will also be studied. ..
- OU Developmental Center for Injury Prevention ResearchGary Raskob; Fiscal Year: 2005..abstract_text> ..
- EVALUATION OF THE NA+ CHANNEL OUTER VESTIBULESAMUEL DUDLEY; Fiscal Year: 2004..Multiple toxins will used to probe as much of the outer vestibule as possible, to serve as validation of results obtain with other ligands, and to develop sufficient interaction points to constrain adequately the model. ..
- Hu1D10 in CLL: CLINICAL AND LABORATORY STUDIESJohn Byrd; Fiscal Year: 2006..abstract_text> ..
- Fetal & Adolescent Nicotine Effects on CNS 5HT SystemsTheodore Slotkin; Fiscal Year: 2003..abstract_text> ..
- CELL DEATH INDUCED BY ANTICANCER AGENTSAlan Eastman; Fiscal Year: 2007..The ultimate goal of this research program will be to define which pathway and effector a specific leukemia uses, and then prescribe effective drug combinations that will be individualized for that patient. ..
- MENTORING FOR NEW CANCER THERAPEAUTICSGary Schwartz; Fiscal Year: 2005..This K24 award mechanism represents the essence of what we are proposing and for which support is needed. ..
- SIV Behavioral Pathology: Manipulation of Viral LoadMICHAEL TAFFE; Fiscal Year: 2004..abstract_text> ..
- Transporter maintenance of dopamine homeostasisCLARE WILHELM; Fiscal Year: 2005....
- Pharmacoresistance in rats with kainate-induced epilepsyF Dudek; Fiscal Year: 2005..abstract_text> ..
- IMAGING DOPAMINE RELEASE/ENDOCRINE CHANGES IN ALCOHOLISMDEAN WONG; Fiscal Year: 2004..If the initial D2 receptor deficits are exacerbated by alcohol abuse one can envision a positive feedback loop hard to break. ..
- Dedicated High Performance Human Brain/Preclinical PETDEAN WONG; Fiscal Year: 2004..abstract_text> ..
- LOCAL INTERACTIONS BETWEEN HIPPOCAMPAL NEURONSF Edward Dudek; Fiscal Year: 2006....
- High End Computing for PET/SPECTDEAN WONG; Fiscal Year: 2007..unreadable] [unreadable] [unreadable]..
- IMAGING DOPAMINE/SEROTONIN MECHANISMS IN COCAINE CRAVINGDEAN WONG; Fiscal Year: 2003..Testing of these hypotheses will provide novel and fundamental answers to craving mechanisms. ..
- Gene Expression in Prediabetes: Potential Role of PGC-1MARY PATTI; Fiscal Year: 2006..abstract_text> ..
- MECHANISMS OF DOPAMINE & SEROTONIN IN TOURETTE SYNDROMEDEAN WONG; Fiscal Year: 2003..We propose to carry out experiments using PET to establish a more complete understanding of the neurotransmission in TS. This will also help establish new ationales for improved therapeutics in TS. ..
- Progression of temporal lobe epilepsyF Edward Dudek; Fiscal Year: 2007..abstract_text> ..
- Fluorescent Zinc Sensors for Cellular ImagingCHRISTOPH FAHRNI; Fiscal Year: 2008..The lack of a non-invasive zinc specific fluorescent sensor is currently a limiting factor in the study of intracellular zinc regulation and trafficking. ..
- ETHANOL METABOLISM IN PREGNANCY--ROLE OF DIETMartin Ronis; Fiscal Year: 2005....
- Lipitor/Celebrex: effect on prostate cancer progressionXi Zheng; Fiscal Year: 2007..This combination of drugs may significantly improve the management of prostate cancer. [unreadable] [unreadable] [unreadable]..
- Role of inositol trisphosphate in preconditioningKarin Przyklenk; Fiscal Year: 2004....
- Aging, Adenosine and Platelet-Mediated ThrombosisKarin Przyklenk; Fiscal Year: 2008..unreadable] [unreadable] [unreadable]..
- DOMINANT NEGATIVE ESTROGEN RECEPTORS AND BREAST CANCERBenita Katzenellenbogen; Fiscal Year: 2002..I. will introduce the gene- selective DN-ERs into cells using her efficient adenovirus system, determine their effects on gene expression, and examine their importance in ER regulated breast cancer cell proliferation and invasiveness. ..
- Preconditioning Improves Coronary PatencyKarin Przyklenk; Fiscal Year: 2007..The resulting mechanistic insights may, ultimately, be exploited in the future design of novel therapies for the clinical treatment of recurrent thrombosis. ..