Zobrazeno 1 - 10
of 53
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::72dbe3ede703ddd1435f27709b6c8281
https://doi.org/10.1021/acs.jmedchem.0c01280
https://doi.org/10.1021/acs.jmedchem.0c01280
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0b71e35732be381557da3e884c36cd80
https://doi.org/10.1152/jn.00104.2017
https://doi.org/10.1152/jn.00104.2017
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bd1b773984159dd5e2a719a0398228e6
https://doi.org/10.1021/acs.jmedchem.6b00287
https://doi.org/10.1021/acs.jmedchem.6b00287
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f97219b310e316ae06bf27bb69c1321c
https://doi.org/10.1080/23328940.2015.1046013
https://doi.org/10.1080/23328940.2015.1046013
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.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0c872a552827bd07e374fa2534ad6a6e
https://pubmed.ncbi.nlm.nih.gov/27934457
https://pubmed.ncbi.nlm.nih.gov/27934457
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f26cec77f1eb7a5454a08a328e395101
https://doi.org/10.1016/j.pain.2008.11.004
https://doi.org/10.1016/j.pain.2008.11.004
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d345e34dd8700b32db5ac00c4d0fbd47
https://doi.org/10.1124/jpet.108.138511
https://doi.org/10.1124/jpet.108.138511
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::65762e92fd878ae91ff241f6133f0ff1
https://doi.org/10.1021/jm701007g
https://doi.org/10.1021/jm701007g
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2d56c87efa9cefdc29bae60c6ca62103
https://doi.org/10.1124/jpet.107.124305
https://doi.org/10.1124/jpet.107.124305
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b94d6173302f6adb4d15301008d5dc2f
https://doi.org/10.1016/j.bmcl.2007.04.105
https://doi.org/10.1016/j.bmcl.2007.04.105