Zobrazeno 1 - 10
of 60
pro vyhledávání: '"Arthur Gomtsyan"'
Autor:
Kathy Sarris, Philip J. Hajduk, Ihle David C, Diana L. Donnelly-Roberts, Arthur Gomtsyan, Christian Goess, David B. Duignan, Danying Song, Chaohong Sun, Andrea Mcclure, Adrian D. Hobson, Robert H. Stoffel, Anil Vasudevan, John A. Mankovich, Sanjay C. Panchal, A. Chris Krueger, Steven L. Swann, Kenneth M. Comess, Andrew M. Petros, Wilson Noel S, Jill M. Wetter, Paul G. Richardson, Kenton L. Longenecker, Paul M. Jung, Vincent S. Stoll, Amanda W. Dombrowski, Suzanne Mathieu, Justin D. Dietrich, Philip B. Cox
Publikováno v:
Journal of Medicinal Chemistry. 64:417-429
Tumor necrosis factor α (TNFα) is a soluble cytokine that is directly involved in systemic inflammation through the regulation of the intracellular NF-κB and MAPK signaling pathways. The development of biologic drugs that inhibit TNFα has led to
Autor:
Jill-Desiree Brederson, Michael J. Dart, Robert G. Schmidt, Steve McGaraughty, Philip R. Kym, Arthur Gomtsyan, Laura Leys, Katharine L. Chu, Richard J. Radek, Jun Xu
Publikováno v:
Journal of Neurophysiology. 118:904-916
TRPV3 is a nonselective cation channel activated by temperatures above 33°C and is reported to be localized in keratinocytes and nervous tissue. To investigate a role for TRPV3 in pain modulation, we conducted a series of in vivo electrophysiologica
Autor:
Philip R. Kym, Arthur Gomtsyan, Gregory A. Gfesser, Bin Li, Regina M. Reilly, Bruce Clapham, Jerome F. Daanen, Rodger F. Henry, Torben R. Neelands, Pamela S. Puttfarcken, Susan M. Huang, Robert G. Schmidt, Robert J. Altenbach, S.K. Joshi, Huaqing Liu, Marlon D. Cowart, David N. Whittern, Phil B. Cox, Jill-Desiree Brederson, Michael J. Dart, Anurupa Shrestha, Donna Gauvin, Michael E. Kort, Erol K. Bayburt, Ping Song, Steve McGaraughty, Connie R. Faltynek, Heath A. McDonald, Patricia N. Banfor, Diana Schmidt, Eric A. Voight, Mohamad Shebley, Jason A. Segreti
Publikováno v:
Journal of Medicinal Chemistry. 59:4926-4947
Transient receptor potential vanilloid 3 (TRPV3) is a Ca(2+)- and Na(+)-permeable channel with a unique expression pattern. TRPV3 is found in both neuronal and non-neuronal tissues, including dorsal root ganglia, spinal cord, and keratinocytes. Recen
Autor:
Arthur Gomtsyan, Kort Michael E, Michael J. Dart, Regina M. Reilly, Jason A. Segreti, Heath A. McDonald, Philip R. Kym, Pamela S. Puttfarcken, Robert G. Schmidt, Jerome F. Daanen, Voight Eric
Publikováno v:
Temperature: Multidisciplinary Biomedical Journal
Transient receptor potential vanilloid 1 (TRPV1) is a multifunctional ion channel playing important roles in a numerous biological processes including the regulation of body temperature. Within distinct and tight chemical space of chromanyl ureas TRP
Stereoselective Synthesis of a Dipyridyl Transient Receptor Potential Vanilloid-3 (TRPV3) Antagonist
Autor:
Robert G. Schmidt, Jerome F. Daanen, Arthur Gomtsyan, Philip R. Kym, Michael J. Dart, Eric A. Voight
Publikováno v:
The Journal of organic chemistry. 81(23)
An efficient asymmetric synthesis of dipyridyl TRPV3 antagonist 1 is reported. The four-step route involves two C–C bond-forming steps, a highly diastereoselective alkene hydration, and asymmetric ketone hydrosilylation in 97% ee.
Autor:
Jerome F. Daanen, Joseph P. Mikusa, Chih Hung Lee, Chengmin Zhong, Jason A. Segreti, Patrick W. Mantyh, Torben R. Neelands, Patricia N. Banfor, Michael F. Jarvis, Arthur Gomtsyan, Prasant Chandran, Molly A. Sevcik, Philip R. Kym, Donna M. Gauvin, Regina M. Reilly, Kennan C. Marsh, Michael E. Kort, Connie R. Faltynek, James P. Sullivan, Erol K. Bayburt, Carol S. Surowy, Joseph R. Ghilardi, Prisca Honore, Gricelda Hernandez, Ryan M. Fryer, Shailen K. Joshi
Publikováno v:
Pain. 142:27-35
Transient receptor potential vanilloid type 1 (TRPV1) is a ligand-gated ion channel that functions as an integrator of multiple pain stimuli including heat, acid, capsaicin and a variety of putative endogenous lipid ligands. TRPV1 antagonists have be
Autor:
Carol S. Surowy, Katharine L. Chu, Prisca Honore, Rachid El Kouhen, Connie R. Faltynek, Bruce R. Bianchi, Ping Han, James P. Sullivan, Steve McGaraughty, Wende Niforatos, Arthur Gomtsyan, Erol K. Bayburt, Chih-Hung Lee, Torben R. Neelands, Heath A. McDonald, Melissa H. Vos, Michael F. Jarvis
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 326:879-888
The transient receptor potential vanilloid (TRPV) 1 receptor, a nonselective cation channel expressed on peripheral sensory neurons and in the central nervous system, plays a key role in pain. TRPV1 receptor antagonism is a promising approach for pai
Autor:
Prisca Honore, Connie R. Faltynek, James P. Sullivan, Jill M. Wetter, Arthur Gomtsyan, Michael F. Jarvis, Carol S. Surowy, Steven M. Hannick, Robert G. Schmidt, Erol K. Bayburt, Chih-Hung Lee, Kennan C. Marsh, Heath A. McDonald
Publikováno v:
Journal of Medicinal Chemistry. 51:392-395
Vanilloid receptor TRPV1 is a cation channel that can be activated by a wide range of noxious stimuli, including capsaicin, acid, and heat. Blockade of TRPV1 activation by selective antagonists is under investigation by several pharmaceutical compani
Autor:
Sriajan N. Vaidyanathan, Bruce R. Bianchi, Torben R. Neelands, Robert B. Moreland, Bruce Surber, Carol S. Surowy, Rachid El Kouhen, Michael F. Jarvis, Chih-Hung Lee, Shirish N. Raja, Connie R. Faltynek, Arthur Gomtsyan, Heath A. McDonald, Pamela S. Puttfarcken
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 323:285-293
1-((R)-5- tert -Butyl-indan-1-yl)-3-isoquinolin-5-yl-urea (A-778317) is a novel, stereoselective, competitive antagonist that potently blocks transient receptor potential vanilloid-1 (TRPV1) receptor-mediated changes in intracellular calcium concentr
Autor:
Connie R. Faltynek, Joe Mikusa, Richard J. Perner, Jill M. Wetter, Stanley Didomenico, Tammie K. Jinkerson, Kennan C. Marsh, Chih-Hung Lee, John R. Koenig, Heath A. McDonald, Sean C. Turner, Arthur Gomtsyan, Erol K. Bayburt, Carol S. Surowy, Irene Drizin, Ryan G. Keddy, Prisca Honore
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:3894-3899
SAR studies for N-aryl-N′-benzyl urea class of TRPV1 antagonists have been extended to cover α-benzyl alkylation. Alkylated compounds showed weaker in vitro potencies in blocking capsaicin activation of TRPV1 receptor, but possessed improved pharm