Zobrazeno 1 - 6
of 6
pro vyhledávání: '"Kumar Emayan"'
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:
Jeremy Fournier, Karen Chen, Artur K. Mailyan, Jeffrey J. Jackson, Brad O. Buckman, Kumar Emayan, Shendong Yuan, Ravi Rajagopalan, Shawn Misialek, Marc Adler, Michael Blaesse, Andreas Griessner, Armen Zakarian
Publikováno v:
Organic letters. 21(2)
A total synthesis of N-desmethyl thalassospiramide C, a unique strained macrocyclic proteobacterial depsipeptide, enabled a detailed crystallographic study of its covalent complex with cathepsin K, a member of a medicinally important family of cystei
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::224f7ef009372f080fe122a19b962fd5
https://pubmed.ncbi.nlm.nih.gov/30628449
https://pubmed.ncbi.nlm.nih.gov/30628449
Autor:
Mariko Nagashima, Kumar Emayan, Imadul Islam, William P. Dole, Lei Zhao, Shendong Yuan, Yi-Xin Wang, Ronald Vergona, Kohichi Kawai, Mark E. Sullivan, Brad O. Buckman, John Morser, Junko Hosoya, Jon Vincelette, Valdeci da Cunha
Publikováno v:
Thrombosis and Haemostasis. 97:54-61
SummaryWe have discovered a novel small-molecule TAFIa inhibitor, BX 528, which is potent, highly selective against other carboxypeptidases and safe. The present study was to determine if BX 528 can enhance exogenous and endogenous thrombolysis in fo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fece7848f9ffa2d997c6d326fb212d58
https://doi.org/10.1160/th06-09-0552
https://doi.org/10.1160/th06-09-0552
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:
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
Autor:
Ronald Vergona, John Morser, Jon Vincelette, Mariko Nagashima, Lei Zhao, Judi Bryant, Kumar Emayan, Wei-Wei Li, Shendong Yuan, Paul Hrvatin, Babu Subramanyam, Drew Sukovich, Imadul Islam, Brad O. Buckman, David R. Light, Yi-Xin Wang
Publikováno v:
Thrombosis and haemostasis. 97(1)
SummaryWe have discovered a novel small-molecule (3-phosphinoylpropionic acid) inhibitor of activated thrombin activatable fibrinolysis inhibitor (TAFIa), BX 528, which had an IC50 of 2 nM in an enzymatic assay and 50 nM in an in-vitro clot lysis ass
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0fb4909cf9deb49e412f2c270a27e4f5
https://pubmed.ncbi.nlm.nih.gov/17200770
https://pubmed.ncbi.nlm.nih.gov/17200770