Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Matthew Allen Schiffler"'
Autor:
Boris A. Czeskis, Bryan H. Norman, Norman Earle Hughes, Kenneth C. Cassidy, Kuklish Steven Lee, Debra Luffer-Atlas, Matthew Fisher, Trent L. Abraham, Matthew Allen Schiffler, Jeffrey J. Alberts
Publikováno v:
Journal of Medicinal Chemistry. 61:2041-2051
Two 2-aminoimidazole-based inhibitors, LY3031207 (1) and LY3023703 (2), of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme were found to cause drug-induced liver injury (DILI) in humans. We studied imidazole ring substitutions to successfu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5a48ede5c43b6a64048edfaea1a77596
https://doi.org/10.1021/acs.jmedchem.7b01806
https://doi.org/10.1021/acs.jmedchem.7b01806
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:
Bruce W. Shaw, Yuke Zhang, Kenneth C. Cassidy, Robert M. Christie, Prabhakar Kondaji Jadhav, Jim D. Durbin, Gary G. Deng, Matthew Allen Schiffler, Kostas Gavardinas, Richard A. Brier, Keyun Qing, Donald P. Matthews, Michael A. Staszak, William F. Matter, Yong Wang, Kim Euibong Jemes, D. Scott Coffey
Publikováno v:
ACS Medicinal Chemistry Letters. 5:1138-1142
Cathepsin S (Cat S) plays an important role in many pathological conditions, including abdominal aortic aneurysm (AAA). Inhibition of Cat S may provide a new treatment for AAA. To date, several classes of Cat S inhibitors have been reported, many of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6393a9fc5f96e20e55b6bf40e534a7b3
https://doi.org/10.1021/ml500283g
https://doi.org/10.1021/ml500283g
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
Autor:
Stephanie L. Stout, Patrick C. May, Brian Morgan Watson, Pablo Garcia Losada, Valentine J. Klimkowski, Brian Michael Mathes, David E. Timm, Dustin J. Mergott, Scott A. Monk, Leonard L. Winneroski, Leonard N. Boggs, James P. Beck, James E. Audia, Matthew Allen Schiffler, Richard A. Brier, Anthony R. Borders, Jon A. Erickson, Robert D. Boyer, Kevin John Hudziak
Publikováno v:
Bioorganicmedicinal chemistry. 23(13)
The BACE1 enzyme is a key target for Alzheimer’s disease. During our BACE1 research efforts, fragment screening revealed that bicyclic thiazine 3 had low millimolar activity against BACE1. Analysis of the co-crystal structure of 3 suggested that po
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::01477228c3c9d6ec449c18a60008a90e
https://pubmed.ncbi.nlm.nih.gov/26001341
https://pubmed.ncbi.nlm.nih.gov/26001341
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