Zobrazeno 1 - 10
of 29
pro vyhledávání: '"J.L. Oskins"'
Autor:
N. Schuelert, H.H. Bui, P.G. Mitchell, C. Lin, S. Albacete, Mark Chambers, J.L. Oskins, Jason J. McDougall
Publikováno v:
Osteoarthritis and Cartilage. 25:926-934
Summary Objective Emerging evidence suggests that osteoarthritis (OA) has a neuropathic component; however, the identity of the molecules responsible for this peripheral neuropathy is unknown. The aim of this study was to determine the contribution o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::71e77ea3f21d648a08190ea87de8404f
https://doi.org/10.1016/j.joca.2016.08.016
https://doi.org/10.1016/j.joca.2016.08.016
Autor:
Thomas James Beauchamp, Thomas J. Bleisch, Norman Earle Hughes, Daniel R. Mudra, Srinivasan Chandrasekhar, Bryan H. Norman, Hai Bui, Jim D. Durbin, Spencer B. Jones, Yen Dao, Kannan Thirunavukkarasu, Mark Chambers, Denis J. McCann, J.L. Oskins, Joseph Michael Gruber, Lance Allen Pfeifer, Craig A. Swearingen, Christopher John Rito, V. Joseph Klimkowski, C. Lin
Publikováno v:
ACS Medicinal Chemistry Letters. 7:857-861
In an effort to develop a novel therapeutic agent aimed at addressing the unmet need of patients with osteoarthritis pain, we set out to develop an inhibitor for autotaxin with excellent potency and physical properties to allow for the clinical inves
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::095ce4b285974ea117e2612b0b46c193
https://doi.org/10.1021/acsmedchemlett.6b00207
https://doi.org/10.1021/acsmedchemlett.6b00207
Autor:
Daniel R. Mudra, Matthew J. Fisher, Maria-Jesus Blanco, Warshawsky Alan M, Xiao-Peng Yu, Tatiana Natali Vetman, Anita K. Harvey, Srinivasan Chandrasekhar, Xushan Wang, Kuklish Steven Lee, J.L. Oskins, Mark Chambers, C. Lin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:2303-2307
Continued SAR optimization of a series of 3-methylpyridine-2-carbonyl amino-2,4-dimethyl-benzoic acid led to the selection of compound 4f for clinical studies. Compound 4f showed an IC50 of 123nM for inhibition of PGE2-induced TNFα reduction in an e
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::14c5fc831a41c4d4dae2d9bc322b91a3
https://doi.org/10.1016/j.bmcl.2016.03.041
https://doi.org/10.1016/j.bmcl.2016.03.041
Autor:
J.L. Oskins, Bryan H. Norman, Mark Chambers, Norman Earle Hughes, Stefan Jon Thibodeaux, Matthew Allen Schiffler, Matthew J. Fisher, Thomas W. Seng, Xiao-Peng Yu, C. Lin, Srinivasan Chandrasekhar, Anita K. Harvey
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 356:635-644
Prostaglandin (PG) E2 plays a critical role in eliciting inflammation. Nonsteroidal anti-inflammatory drugs and selective inhibitors of cyclooxygenase, which block PGE2 production, have been used as key agents in treating inflammation and pain associ
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::61706c85be6f948a476e83f92edb49d2
https://doi.org/10.1124/jpet.115.228932
https://doi.org/10.1124/jpet.115.228932
Autor:
John Palmer, Michael P. Johnson, J.L. Oskins, Sean P. Hollinshead, Adam J. Sanderson, Peter C. Astles, Robert E. Stratford, Tidwell Michael Wade, Mark Chambers, Rossella Guidetti
Publikováno v:
Journal of Medicinal Chemistry. 56:5722-5733
A focused screening strategy identified thienopyrimidine 12 as a cannabinoid receptor type 2 agonist (hCB2) with moderate selectivity over the hCB1 receptor. This initial hit suffered from poor in vitro metabolic stability and high in vivo clearance.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2c8682b65f415f95103b7810db27700f
https://doi.org/10.1021/jm400305d
https://doi.org/10.1021/jm400305d
Autor:
James Nelson, X.-F. Wang, Baolin Li, B. Gaynor, C. Lin, Donmienne Doen Mun Leung, R.A. Lynch, E.C. Collins, E.M. Conner, D. McCarty, E.S. Nisenbaum, Kirk W. Johnson, J.L. Oskins, Robert J. Benschop, Barrett Allan, Jing Xu, Ryan James Darling, Mark Chambers
Publikováno v:
Osteoarthritis and Cartilage. 22(11)
Corrigendum to “Development of a novel antibody to Calcitonin Gene-Related Peptide for the treatment of osteoarthritis-related pain” [Osteoarthritis Cartilage 22 (2014) 578e585] R.J. Benschop y , E.C. Collins y, R.J. Darling y, B.W. Allan z, D. L
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b1f9dca113c685b9a8776d47bb16b1f8
Autor:
Bryan H. Norman, Spencer B. Jones, Kannan Thirunavukkarasu, Mark Chambers, Craig A. Swearingen, P.G. Mitchell, Lance Allen Pfeifer, J.L. Oskins, H.H. Bui, C. Lin
Publikováno v:
Osteoarthritis and cartilage. 25(6)
Summary Objective Autotaxin is a secreted lysophospholipase that mediates the conversion of lysophosphatidyl choline (LPC) to lysophosphatidic acid (LPA), a bioactive lipid mediator. Autotaxin levels in plasma and synovial fluid correlate with diseas
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::674054280c92bb3b1ec61ef980d93c84
https://pubmed.ncbi.nlm.nih.gov/27638130
https://pubmed.ncbi.nlm.nih.gov/27638130
Autor:
Mark Chambers, Michael P. Johnson, Jason J. McDougall, J.L. Oskins, Karandeep Jassal, Niklas Schuelert
Publikováno v:
Pain. 152:975-981
The present study examined whether enhancement of endogenous cannabinoid levels by administration of the fatty acid amide hydrolase inhibitor URB597 could modulate joint nociception in 2 rodent models of osteoarthritis (OA). OA-like changes were indu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7a08ea019476b9e1020016fd216e4d96
https://doi.org/10.1016/j.pain.2010.11.025
https://doi.org/10.1016/j.pain.2010.11.025
Autor:
C. Lin, Daniel R. Mudra, Srinivasan Chandrasekhar, Maria-Jesus Blanco, Warshawsky Alan M, Anita K. Harvey, Mark Chambers, J.L. Oskins, Xiao-Peng Yu, Matthew J. Fisher, Tatiana Natali Vetman, Xushan Wang
Publikováno v:
Bioorganicmedicinal chemistry letters. 26(3)
Two new series of EP4 antagonists containing a 3-methylaryl-2-carbonyl core have been identified. One series has a 3-substituted-phenyl core, while the other one incorporates a 3-substituted pyridine. Both series led to compounds with potent activity
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::86325769c3f800f2e396e92da7d6eb72
https://pubmed.ncbi.nlm.nih.gov/26764191
https://pubmed.ncbi.nlm.nih.gov/26764191
Autor:
Anita K. Harvey, Srinivasan Chandrasekhar, C. Lin, Tatiana Natali Vetman, Xushan Wang, Matthew Allen Schiffler, Warshawsky Alan M, J.L. Oskins, Jeremy Schulenburg York, Mark Chambers, Alison M. Bendele, Matthew J. Fisher, Maria-Jesus Blanco, Xiao-Peng Yu, Kuklish Steven Lee
Publikováno v:
Pharmacology Research & Perspectives
Prostaglandin (PG) E2 is the key driver of inflammation associated with arthritic conditions. Inhibitors of PGE 2 production (NSAIDs and Coxibs) are used to treat these conditions, but carry significant side effect risks due to the inhibition of all
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4ffbf1e41fe7c0346232633521ef9bb7
https://doi.org/10.1002/prp2.316
https://doi.org/10.1002/prp2.316