Zobrazeno 1 - 10
of 35
pro vyhledávání: '"Thomas S, Rush"'
Autor:
Matthias Zentgraf, Elizabeth Krutoholow, Thomas S. Rush, Chris Luebkemann, Kimito Funatsu, Gisbert Schneider, Jeff Blaney, Alleyn T. Plowright, Norman Sieroka, John Edward Hill, Petra Schneider, Jennifer Listgarten, José S. Duca, Robert Alan Goodnow, Johanna M. Jansen, Jasmin Fisher, Matthias Kohler, W. Patrick Walters
Publikováno v:
Nature Reviews Drug Discovery. 19:353-364
Artificial intelligence (AI) tools are increasingly being applied in drug discovery. While some protagonists point to vast opportunities potentially offered by such tools, others remain sceptical, waiting for a clear impact to be shown in drug discov
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::53001ef1a373cf62d629543029f92869
https://doi.org/10.1038/s41573-019-0050-3
https://doi.org/10.1038/s41573-019-0050-3
Autor:
James M. Brase, Thomas S. Rush, Brian J. Bennion, Kevin McLoughlin, Thomas D. Sweitzer, Margaret J. Tse, Jonathan E. Allen, Stacie Calad-Thomson, Claire G. Jeong, Amanda Minnich
Drug-induced liver injury (DILI) is the most common cause of acute liver failure and a frequent reason for withdrawal of candidate drugs during preclinical and clinical testing. An important type of DILI is cholestatic liver injury, caused by buildup
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b1d12110e0bc5b0a03cb79780f563a04
http://arxiv.org/abs/2002.12541
http://arxiv.org/abs/2002.12541
Autor:
Petra, Schneider, W Patrick, Walters, Alleyn T, Plowright, Norman, Sieroka, Jennifer, Listgarten, Robert A, Goodnow, Jasmin, Fisher, Johanna M, Jansen, José S, Duca, Thomas S, Rush, Matthias, Zentgraf, John Edward, Hill, Elizabeth, Krutoholow, Matthias, Kohler, Jeff, Blaney, Kimito, Funatsu, Chris, Luebkemann, Gisbert, Schneider
Publikováno v:
Nature reviews. Drug discovery. 19(5)
Artificial intelligence (AI) tools are increasingly being applied in drug discovery. While some protagonists point to vast opportunities potentially offered by such tools, others remain sceptical, waiting for a clear impact to be shown in drug discov
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::3b4340fe33dcb827c37bc8bd01eead2f
https://pubmed.ncbi.nlm.nih.gov/31801986
https://pubmed.ncbi.nlm.nih.gov/31801986
Autor:
Thomas S. Rush, Hussein Tawbi, Yongqi Deng, Wen-Jen Hwu, Paul Kirschmeier, Ryan J. Sullivan, Joseph Rubino, Ahmed A. Samatar, Lidia Robert, Gerald W. Shipps, Keith T. Flaherty, Donna Carr, Peter C.C. Fong, Antoni Ribas, Patrick Chun, Brian Long, Eric H. Rubin, Priya Dayananth, Ramesh K. Ramanathan, Ronnie Shapira-Frommer, Stergios J. Moschos, Blanca Homet Moreno, W. Robert Bishop, Alan B. Cooper, James E. Schiller, Alex A. Adjei, Nathan R. Miselis, Da Zhang
Publikováno v:
JCI Insight, Vol 3, Iss 4 (2018)
JCI insight, vol 3, iss 4
JCI insight, vol 3, iss 4
BACKGROUND. Constitutive activation of ERK1/2 occurs in various cancers, and its reactivation is a well-described resistance mechanism to MAPK inhibitors. ERK inhibitors may overcome the limitations of MAPK inhibitor blockade. The dual mechanism inhi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0f1125084220541ce8d767feec5c05a4
https://doaj.org/article/675b9e9f9e9e4e0f87e9c28de4f3db4b
https://doaj.org/article/675b9e9f9e9e4e0f87e9c28de4f3db4b
Autor:
Michael Weber, Joon Jung, Dongyu Sun, Alan B. Northrup, Ilona Kariv, Zangwei Xu, Thomas S. Rush, Ekaterina V. Bobkova
Publikováno v:
Combinatorial Chemistry & High Throughput Screening. 13:16-26
A dynamic, focused screening strategy that utilized a limited but diversified set of target-specific compounds was explored as an efficient means for the identification of inhibitors of the protein kinase PDK1. Approximately 21,500 compounds, includi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4da68acd8fb4546d1f86086d9e29b205
https://doi.org/10.2174/138620710790218186
https://doi.org/10.2174/138620710790218186
Autor:
Ilona Kariv, Alan B. Northrup, Dongyu Sun, Thomas S. Rush, Kumiko Nagashima, Ekaterina V. Bobkova, Zangwei Xu, Jannik N. Andersen
Publikováno v:
SLAS Discovery. 14:1257-1262
The PI3K/Akt signaling pathway plays a key role in cancer cell growth, survival, and tumor angiogenesis. 3-Phosphoinositide-dependent protein kinase 1 (PDK1) is a Ser/Thr protein kinase, which catalyzes the phosphorylation of a conserved residue in t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4c64b6ee859c214267787fe54e109207
https://doi.org/10.1177/1087057109349356
https://doi.org/10.1177/1087057109349356
Autor:
Jennifer R. Thomason, Phaik-Eng Sum, Elisabeth A. Morris, Erica Reifenberg, Tam Steve Yik-Kai, Yonghan Hu, Manas K. Majumdar, Thomas S. Rush, Katy E. Georgiadis, Leila Abrous, Jason Shaoyun Xiang, Manus Ipek, Joshua James Sabatini
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:311-316
Aggrecanases are recently discovered enzymes that cleave aggrecan, a key component of cartilage. Aggrecanase inhibitors may provide a unique means to halt the progression of cartilage destruction in osteoarthritis. The synthesis and evaluation of bip
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::09e990d97f59210a9bc14ea6a6dd2edb
https://doi.org/10.1016/j.bmcl.2005.10.001
https://doi.org/10.1016/j.bmcl.2005.10.001
Autor:
Wei Li, Qin Wang, Jason Shaoyun Xiang, Jeremy I. Levin, Leif M. Laakso, Xuemei Du, Thomas S. Rush, Jennifer R. Thomason, Manus Ipek, Tam Steve Yik-Kai, Yonghan Hu, Jerauld S. Skotnicki, Jean Schmid, Martin J. DiGrandi, Jianchang Li
Publikováno v:
Bioorganic & Medicinal Chemistry. 13:6629-6644
Modification of alpha-biphenylsulfonamidocarboxylic acids led to potent and selective MMP-13 inhibitors. Compound 16 showed 100% oral bioavailability in rats and demonstrated50% inhibition of bovine cartilage degradation at 10 ng/mL.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::22d053419b0d61b6ff86d04a32ae1868
https://doi.org/10.1016/j.bmc.2005.07.076
https://doi.org/10.1016/j.bmc.2005.07.076
Autor:
Xuemei Du, Thomas S. Rush, Tam Steve Yik-Kai, Yonghan Hu, Dianne DeVincentis, Jennifer R. Thomason, Kristina Cunningham, Jason Shaoyun Xiang, Jeremy I. Levin, Jianchang Li, Elisabeth A. Morris, Wei Li, Jerauld S. Skotnicki, Priya S. Chockalingam
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:4961-4966
The structure-based design and synthesis of a series of novel biphenyl sulfonamide carboxylic acids as potent MMP-13 inhibitors with selectivity over MMP-1, MMP-2, MMP-3, MMP-7, MMP-8, MMP-9, MMP-14, Aggrecanase 1, and TACE are described.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5b44ddefc7ea6586738dcff00b25091c
https://doi.org/10.1016/j.bmcl.2005.08.001
https://doi.org/10.1016/j.bmcl.2005.08.001
Autor:
Lee D, Jennings, Kenneth W, Foreman, Thomas S, Rush, Desiree H H, Tsao, Lidia, Mosyak, Scott L, Kincaid, Mohani N, Sukhdeo, Alan G, Sutherland, Weidong, Ding, Cynthia Hess, Kenny, Chantel L, Sabus, Hanlan, Liu, Elizabeth G, Dushin, Soraya L, Moghazeh, Pornpen, Labthavikul, Peter J, Petersen, Margareta, Tuckman, Steven A, Haney, Alexey V, Ruzin
Publikováno v:
Bioorganic & Medicinal Chemistry. 12:5115-5131
The ZipA–FtsZ protein–protein interaction is a potential target for antibacterial therapy. The design and parallel synthesis of a combinatorial library of small molecules, which target the FtsZ binding area on ZipA are described. Compounds were d
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::41000540d428bfc3965e4aaf6d9608f0
https://doi.org/10.1016/j.bmc.2004.07.031
https://doi.org/10.1016/j.bmc.2004.07.031