Zobrazeno 1 - 10
of 65
pro vyhledávání: '"Srinivasan Chandrasekhar"'
Autor:
Stephen Antonysamy, Milan Maletic, Srinivasan Chandrasekhar, Michael J. Hickey, Karen Gooding, Joseph D. Ho, Anita K. Harvey, Norman Earle Hughes, Steven D. Kahl, John G. Luz, Matthew R. Lee, Kristen Aznavour, Aiping Zhang, Xiao-Peng Yu, Jonathan S. Park, Bryan H. Norman, Bradley Condon, Charles Rauch, Ashley V. Sloan
Publikováno v:
Biochimica et Biophysica Acta (BBA) - General Subjects. 1865:129800
Background Due to the importance of both prostaglandins (PGs) and leukotrienes (LTs) as pro-inflammatory mediators, and the potential for eicosanoid shunting in the presence of pathway target inhibitors, we have investigated an approach to inhibiting
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c93d058704c9d408a3ef614e240c5014
https://doi.org/10.1016/j.bbagen.2020.129800
https://doi.org/10.1016/j.bbagen.2020.129800
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:
Srinivasan Chandrasekhar, Tatiana Natali Vetman, Xushan Wang, Anita K. Harvey, Matthew Allen Schiffler, Maria-Jesus Blanco, Xiao-Peng Yu, Warshawsky Alan M, Matthew J. Fisher, Daniel R. Mudra
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:105-109
A novel series of EP4 antagonists, based on a quinoline scaffold, has been discovered. Medicinal chemistry efforts to optimize the potency of the initial hit are described. A highly potent compound in a clinically relevant human whole blood assay was
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8005a33b12336736a42cb91a1af334d7
https://doi.org/10.1016/j.bmcl.2015.11.023
https://doi.org/10.1016/j.bmcl.2015.11.023
Autor:
Srinivasan Chandrasekhar, Bradley Condon, Matthew Allen Schiffler, Kuklish Steven Lee, Kim Euibong Jemes, Bryan H. Norman, John R. Rizzo, Jeremy Schulenburg York, Kristina M. Campanale, Stefan Jon Thibodeaux, Richard E. Rathmell, Michael J. Hickey, Christopher Groshong, Shobha N. Bhattachar, Norman Earle Hughes, Anita K. Harvey, John G. Luz, Stephen Antonysamy, Scott Alan Jones, Timothy Andrew Woods, Prashant V. Desai, Matthew J. Fisher, Xiao-Peng Yu, Thomas W. Seng
Publikováno v:
Journal of Medicinal Chemistry. 59:194-205
As part of a program aimed at the discovery of antinociceptive therapy for inflammatory conditions, a screening hit was found to inhibit microsomal prostaglandin E synthase-1 (mPGES-1) with an IC50 of 17.4 μM. Structural information was used to impr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::56fa147abbccd68e15b02f28a0c1735a
https://doi.org/10.1021/acs.jmedchem.5b01249
https://doi.org/10.1021/acs.jmedchem.5b01249
Autor:
Kuklish Steven Lee, Dagart Allison, Bradley Condon, Aiping Zhang, Anita K. Harvey, Ashley V. Sloan, Xiao-Peng Yu, Ryan Thomas Backer, Matthew R. Lee, John G. Luz, Marijane Russell, Srinivasan Chandrasekhar, Matthew Fisher, Shawn Chang, Stephen Antonysamy
Publikováno v:
Journal of Medicinal Chemistry. 58:4727-4737
Microsomal prostaglandin E synthase 1 (mPGES-1) is an α-helical homotrimeric integral membrane inducible enzyme that catalyzes the formation of prostaglandin E2 (PGE2) from prostaglandin H2 (PGH2). Inhibition of mPGES-1 has been proposed as a therap
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::52f51d736c36586dd49c583231b9633f
https://doi.org/10.1021/acs.jmedchem.5b00330
https://doi.org/10.1021/acs.jmedchem.5b00330
Autor:
Srinivasan Chandrasekhar, Warshawsky Alan M, Xiao-Peng Yu, Xushan Wang, Kuklish Steven Lee, Anita K. Harvey, Jeremy Schulenburg York, Matthew J. Fisher, Matthew Allen Schiffler
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:3176-3178
EP4 is a prostaglandin E2 receptor that is a target for potential anti-nociceptive therapy. Described herein is a class of amphoteric EP4 antagonists which reverses PGE2-induced suppression of TNFα production in human whole blood. From this class, a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c528986c49be67d3c54d5743ad9ec0b8
https://doi.org/10.1016/j.bmcl.2015.05.091
https://doi.org/10.1016/j.bmcl.2015.05.091
Autor:
Karen Gooding, Peter R. Manninen, James McGee, Matthew J. Fisher, Antonio Navarro, Warshawsky Alan M, Srinivasan Chandrasekhar, Daniel R. Mudra, Stephen Antonysamy, Adrian J. Fretland, Xiao-Peng Yu, Jeremy Schulenburg York, Jennifer M. Weller, Kuklish Steven Lee, Ashley V. Sloan, Shobha N. Bhattachar, Anita K. Harvey, Katherine M. Partridge, Steven James Quimby, Norman Earle Hughes, John G. Luz, Bryan H. Norman, Matthew Allen Schiffler
Publikováno v:
Bioorganicmedicinal chemistry letters. 27(6)
We describe a novel class of acidic mPGES-1 inhibitors with nanomolar enzymatic and human whole blood (HWB) potency. Rational design in conjunction with structure-based design led initially to the identification of anthranilic acid 5, an mPGES-1 inhi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9c8874e4d61e571fda29a8ef5a34ecc7
https://pubmed.ncbi.nlm.nih.gov/28190634
https://pubmed.ncbi.nlm.nih.gov/28190634
Autor:
Shobha N. Bhattachar, Stephen Antonysamy, Warshawsky Alan M, Norman Earle Hughes, Matthew Allen Schiffler, Anita K. Harvey, Jeremy Schulenburg York, Antonio Navarro, John G. Luz, Bryan H. Norman, Katherine M. Partridge, Steven James Quimby, Xiao-Peng Yu, Karen Gooding, James McGee, Matthew J. Fisher, Kuklish Steven Lee, Srinivasan Chandrasekhar, Ashley V. Sloan, Peter R. Manninen, Adrian J. Fretland
Publikováno v:
Bioorganicmedicinal chemistry letters. 26(19)
Here we report on novel, potent 3,3-dimethyl substituted N-aryl piperidine inhibitors of microsomal prostaglandin E synthases-1(mPGES-1). Example 14 potently inhibited PGE2 synthesis in an ex vivo human whole blood (HWB) assay with an IC50 of 7 nM. I
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cb209c9927e6ec9b4992a099a600c70b
https://pubmed.ncbi.nlm.nih.gov/27554445
https://pubmed.ncbi.nlm.nih.gov/27554445