Zobrazeno 1 - 10
of 16
pro vyhledávání: '"Judi Bryant"'
Autor:
John Morser, Imadul Islam, Cornell Mallari, Elena Ho, Marc Adler, Kumar Emayan, Gary Phillips, Shendong Yuan, Marc Whitlow, Christopher W. West, David R. Light, Giovanna Gualtieri, Drew Sukovich, Ulrich Bothe, Zheng Chang, Kieu Chu, Judi Bryant, Deborah Chen, Caralee Schaefer, Brad O. Buckman
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:3372-3375
We report here the design and synthesis of a novel series of benzylamines that are potent and selective inhibitors of uPA with promising oral availability in rat. Further evaluation of one representative (ZK824859) of the new structural class showed
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::09b761e7a2ae7d063c07c5d293801b02
https://doi.org/10.1016/j.bmcl.2018.09.001
https://doi.org/10.1016/j.bmcl.2018.09.001
Autor:
Shendong Yuan, Robert G. Wei, Andrea DiMella, Michael Snider, Dewan Zheng, Babu Subramanyam, Imadul Islam, Raju Mohan, Michael M. Morrissey, Brad O. Buckman, Laura Dunning, Wei Xu, Jih-Lie Tseng, Judi Bryant
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:1459-1463
A hit to lead process to identify reversible, orally available ADP receptor (P2Y12) antagonists lead compounds is described. High throughput screening afforded 1. Optimization of 1, using parallel synthesis methods, a methyl scan to identify promisin
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::5836598e30c5acf87af4514146955b74
https://doi.org/10.1016/j.bmcl.2018.03.090
https://doi.org/10.1016/j.bmcl.2018.03.090
Autor:
Shendong Yuan, Mark E. Sullivan, Judi Bryant, Serene Alexander, Brad O. Buckman, Mike Snider, Babu Subramanyam, Yi-Xin Wang, Joseph Post, Imadul Islam, Lorraine Kent, Jih-Lie Tseng, John Morser, Sabine Schirm
Publikováno v:
Thrombosis Research. 122:523-532
ADP plays a key role in platelet aggregation which has led to the development of antiplatelet drugs that target the P2Y12 receptor. The aim of this study was to characterize the effects of two novel P2Y12 receptor antagonists, BX 667 and its active m
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::06449e5dacf1d2aa304fd696e5b41090
https://doi.org/10.1016/j.thromres.2008.03.026
https://doi.org/10.1016/j.thromres.2008.03.026
Autor:
Richard I. Feldman, Gary Phillips, Marc Adler, Daguang Zhu, Elena Ho, Wheeseong Lee, Mark A. Polokoff, Hongyi Yu, Dao Lentz, Marc Whitlow, Arnaiz Damian O, Kochanny Monica, Babu Subramanyam, Imadul Islam, James M. Wu, Judi Bryant, Yuo-Ling Chou
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:3814-3818
HTS screening identified 1 with micromolar inhibitory activity against PDK1. Optimization of 1 afforded 4i (BX-517) which has single-digit nanomolar activity against PDK1 and excellent selectivity against PKA.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ca9b5b6c85e996a38c96e34d7d0210bc
https://doi.org/10.1016/j.bmcl.2007.04.071
https://doi.org/10.1016/j.bmcl.2007.04.071
Autor:
Dao Lentz, Marc Whitlow, Zheng Chang, Harald Dinter, Mike Ferrer, Silke Finster, Marc Adler, Daguang Zhu, Sandra L. Biroc, Richard I. Feldman, Bruno Alicke, Monica Kochanny, Judi Bryant, Brad O. Buckman, Mark A. Polokoff, Arnaiz Damian O, James M. Wu, Shendong Yuan
Publikováno v:
Journal of Biological Chemistry. 280:19867-19874
The phosphoinositide 3-kinase/3-phosphoinositide-dependent kinase 1 (PDK1)/Akt signaling pathway plays a key role in cancer cell growth, survival, and tumor angiogenesis and represents a promising target for anticancer drugs. Here, we describe three
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a5088ddc20f2394f04c36606bd1d432b
https://doi.org/10.1074/jbc.m501367200
https://doi.org/10.1074/jbc.m501367200
Autor:
Henrik Seidel, Stewart Leung, Dave Davey, Eric Lyons, Neil G. Miyamoto, April Holbrook, Hugh Salamon, Rebecca Pulk, Richard Horuk, Hong Tao Lu, John Parkinson, Stefan Jaroch, Caralee Schaefer, Markus Berger, Wei Wei Li, Vincent Evans, Daniela Schilling, Werner Skuballa, Babu Subramanyam, Susan Harvey, Cornell Mallari, Elena Ho, Joern Kraetzschmar, Christopher West, Gary Phillips, Michael Snider, Daniel Perez, Beverly King, Judi Bryant
Publikováno v:
SLAS Discovery. 10:168-181
Effector functions and proliferation of T helper (Th) cells are influenced by cytokines in the environment. Th1 cells respond to a synergistic effect of interleukin-12 (IL-12) and interleukin-18 (IL-18) to secrete interferon-gamma (IFN-gamma). In con
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e77054cfcd65440fde4eb19c4a1e47dc
https://doi.org/10.1177/1087057104272394
https://doi.org/10.1177/1087057104272394
Autor:
Stewart, Leung, April, Holbrook, Beverly, King, Hong-Tao, Lu, Vincent, Evans, Neil, Miyamoto, Cornell, Mallari, Susan, Harvey, Dave, Davey, Elena, Ho, Wei-Wei, Li, John, Parkinson, Richard, Horuk, Stefan, Jaroch, Markus, Berger, Werner, Skuballa, Christopher, West, Rebecca, Pulk, Gary, Phillips, Judi, Bryant, Babu, Subramanyam, Caralee, Schaefer, Hugh, Salamon, Eric, Lyons, Daniela, Schilling, Henrik, Seidel, Joern, Kraetzschmar, Michael, Snider, Daniel, Perez
Publikováno v:
SLAS Discovery. 10:157-167
Effector functions and proliferation of T helper (Th) cells are influenced by cytokines in the environment. Th1 cells respond to a synergistic effect of interleukin-12 (IL-12) and interleukin-18 (IL-18) to secrete interferon-gamma (IFN-gamma). In con
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d0f3098f1d6e20981b14ca8e12c2ed60
https://doi.org/10.1177/1087057104272295
https://doi.org/10.1177/1087057104272295
Autor:
Deborah Chen, Damian O. Arnaiz, Wei-Wei Li, Feldman Richard, James M. Wu, Marc Whitlow, Shendong Yuan, Mike Ferrer, Brad Buckman, Judi Bryant, Mark A. Polokoff, Daguang Zhu, Bob Mintzer, Zheng Chang, Kumar Emayan, Sandra L. Biroc, Harald Dinter, Xue Snow Ge, Jih-Lie Tseng, Marc Adler, Jian-Ming Gu, Takashi Sato, Jun Shen
Publikováno v:
Chemical biologydrug design. 74(1)
Heat-shock protein-90 is an attractive target for anticancer drugs, as heat-shock protein-90 blockers such as the ansamycin 17-(allylamino)-17-demethoxygeldanamycin greatly reduce the expression of many signaling molecules that are disregulated in ca
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8ba5a3e56f10ef89bd5c9c6bebd1899e
https://pubmed.ncbi.nlm.nih.gov/19519743
https://pubmed.ncbi.nlm.nih.gov/19519743
Autor:
Gary Phillips, Rebecca Pulk, Christopher W. West, Danny Arnaiz, Shendong Yuan, Kieu Chu, Marc Adler, David R. Light, Deborah Chen, Elena Ho, Giovanna Gualtieri, Marc Whitlow, Christoph Huwe, Judi Bryant, Drew Sukovich
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(19)
In this Letter we report the synthesis and evaluation of a series of non-amidine inhibitors of Urokinase Plasminogen Activator (uPA). Starting from compound 1, a significant change provided compounds in which the amidine, binding in the S1 pocket, wa
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::60747fc1bc1095b1d652f959205693a8
https://pubmed.ncbi.nlm.nih.gov/19703768
https://pubmed.ncbi.nlm.nih.gov/19703768
Autor:
Imadul Islam, Paul Hrvatin, Kieu Chu, Marc Whitlow, Brad O. Buckman, Marc Adler, Drew Sukovich, John Morser, Christopher West, Shendong Yuan, Judi Bryant, Zheng Chang, Kumar Emayan
Publikováno v:
Acta crystallographica. Section D, Biological crystallography. 64(Pt 2)
This article reports the crystal structures of inhibitors of the functional form of thrombin-activatable fibrinolysis inhibitor (TAFIa). In vivo experiments indicate that selective inhibitors of TAFIa would be useful in the treatment of heart attacks
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5377fbebefde91aec43492782d0f200a
https://pubmed.ncbi.nlm.nih.gov/18219114
https://pubmed.ncbi.nlm.nih.gov/18219114