Zobrazeno 1 - 10
of 106
pro vyhledávání: '"Robert M. Scarborough"'
Autor:
Yoshiyuki Toya, Masamichi Nakagome, James E. Tomlinson, Susumu Minamisawa, Takashi Tsunematsu, Kousaku Iwatsubo, Robert M. Scarborough, Yoshihiro Ishikawa, Daniel E. Levy, Satoshi Umemura
Publikováno v:
Journal of Biological Chemistry. 279:40938-40945
Adenylyl cyclase, a major target enzyme of beta-adrenergic receptor signals, is potently and directly inhibited by P-site inhibitors, classic inhibitors of this enzyme, when the enzyme catalytic activity is high. Unlike beta-adrenergic receptor antag
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::64b5d3c34a74f556fdba5fb23caa2a4a
https://doi.org/10.1074/jbc.m314238200
https://doi.org/10.1074/jbc.m314238200
Autor:
Athiwat Hutchaleelaha, Robert M. Scarborough, Penglie Zhang, Susan Edwards, Yanhong Wu, Uma Sinha, Zhaozhong J. Jia, John Woolfrey, Wenrong Huang, Stanley J. Hollennbach, Joseph L. Lambing, Ann E. Arfsten, Yonghong Song, Bing-Yan Zhu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:1229-1234
Using N,N-dialkylated benzamidines as the novel P4 motifs, we have designed and synthesized a class of 1-(2-naphthyl)-1H-pyrazole-5-carboxylamides as highly potent and selective fXa inhibitors with significantly improved hydrophilicity and in vitro a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2cf6e59bdd393461f089032d7d0bc858
https://doi.org/10.1016/j.bmcl.2003.12.054
https://doi.org/10.1016/j.bmcl.2003.12.054
Autor:
Yanhong Wu, Ann E. Arfsten, Bing-Yan Zhu, Uma Sinha, Lane A. Clizbe, Penglie Zhang, Robert M. Scarborough, Susan Edwards, Erick A. Goldman, Merlyn Alphonso, Athiwat Hutchaleelaha, Wenrong Huang, Zhaozhong J. Jia
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:1221-1227
A variety of P4 motifs have been examined to increase the binding affinity and in vitro anticoagulant potency of our biphenyl 1-(2-naphthyl)-1H-pyrazole-5-carboxylamide-based fXa inhibitors. Highly potent 2-naphthyl-P1 fXa inhibitors (K(i)or =2 nM) w
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5398c5f418fd911780f5cf7f3549d9f1
https://doi.org/10.1016/j.bmcl.2003.12.053
https://doi.org/10.1016/j.bmcl.2003.12.053
Autor:
Joseph L. Lambing, Ann E. Arfsten, Bing-Yan Zhu, Gary Park, Stanley J. Hollenbach, Athiwat Hutchaleelaha, Erick A. Goldman, Susan Edwards, Robert M. Scarborough, Jingmei Zuckett, Zhaozhong J. Jia, Bao Liang, Uma Sinha, Penglie Zhang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:983-987
Anthranilamides 4 and 5 were designed and synthesized as selective and orally bioavailable factor Xa inhibitors. Structural modifications aimed at lowering their lipophilicity were performed at the central phenyl ring and at the S4 binding biphenyl r
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::558e9732fd33fd36296be9a795c97db3
https://doi.org/10.1016/j.bmcl.2003.11.079
https://doi.org/10.1016/j.bmcl.2003.11.079
Autor:
Charles J Homcy, Diana B. Cherbavaz, James E. Tomlinson, David M. Sedlock, Robert M. Scarborough, Daniel E. Levy, Ming Bao
Publikováno v:
Journal of Medicinal Chemistry. 46:2177-2186
The adenylyl cyclases (ACs) are a family of intracellular enzymes associated with signal transduction by virtue of their ability to convert ATP to cAMP. The catalytic mechanism of this transformation proceeds through initial binding of ATP to the so-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::31173d1dac9adeec92bc4d65786e1ae6
https://doi.org/10.1021/jm0205604
https://doi.org/10.1021/jm0205604
Autor:
Robert M. Scarborough
Publikováno v:
Current Medicinal Chemistry-Cardiovascular & Hematological Agents. 1:73-82
Interest in the development of specific antagonists of the protease-activated receptors are significant, however, achieving such goals remain extremely challenging. Considerable efforts have been directed at developing specific antagonists of the fir
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::87c63738f64747f3201b3e79c2a1dc6f
https://doi.org/10.2174/1568016033356698
https://doi.org/10.2174/1568016033356698
Autor:
Hua Yang, Bing-Yan Zhu, Ting Su, Deborah Volkots, Paul W. Wong, Robert M. Scarborough, John R. Woolfrey, Uma Sinha, Suiko Dam
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:729-732
The structure-activity relationship of a novel series of substituted piperazinone-based factor Xa inhibitors is described. The most potent compound 34 displays IC(50) of 0.9 nM.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::246edc7a1c0e4f7efe3d517bb30d61ef
https://doi.org/10.1016/s0960-894x(02)01038-7
https://doi.org/10.1016/s0960-894x(02)01038-7
Autor:
Wenhao Li, Brian Huang, Willy Teng, Chhaya Bhakta, Uma Sinha, Lane A. Clizbe, Gary Park, Paul W. Wong, Yonghong Song, Bing-Yan Zhu, Robert M. Scarborough, Andrea Reed
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:2043-2046
To overcome the low bioavailability of our substituted acrylamide P1 benzamidine factor Xa inhibitors reported previously, neutral and less basic groups were used to replace the benzamidine. As a result, a series of P1 aminoisoquinoline substituted a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3012afd60d7c2309311fb94b54171650
https://doi.org/10.1016/s0960-894x(02)00304-9
https://doi.org/10.1016/s0960-894x(02)00304-9
Autor:
John Malinowski, John Woolfrey, Uma Sinha, Katherine Tran, Penglie Zhang, Paul W. Wong, Brian Huang, Gary Park, Jingmei Zuckett, Andrea Reed, Robert M. Scarborough, Stan Hollenbach, Bing-Yan Zhu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:1657-1661
Monoamidine FXa inhibitors 3 were designed and synthesized. SAR studies and molecular modeling led to the design of conformationally constrained diaryl ethers 4 and 5, as well as benzopyrrolidinone 7 as potent FXa inhibitors. The monoamidines show hi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::73fbaeed0975d6f76345655f58bb50df
https://doi.org/10.1016/s0960-894x(02)00234-2
https://doi.org/10.1016/s0960-894x(02)00234-2
Autor:
Nicole Duclos, Neill A. Giese, Keith Abe, Sonia M Amaral, Anjali Pandey, Christina L. Boulton, Carol M. Sullivan, Donna Neuberg, Robert M. Scarborough, Nathalie Lokker, D. Gary Gilliland, Jin-Chen Yu, Louise M Kelly, Mutiah Apatira, Stanley J. Hollenbach, Jason Li, Ifor R. Williams, David P. Curley
Publikováno v:
Cancer Cell. 1:421-432
Up to 30% of acute myelogenous leukemia (AML) patients harbor an activating internal tandem duplication (ITD) within the juxtamembrane domain of the FLT3 receptor, suggesting that it may be a target for kinase inhibitor therapy. For this purpose we h
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::44c51c7cd29183be5c9610a60f6ea335
https://doi.org/10.1016/s1535-6108(02)00070-3
https://doi.org/10.1016/s1535-6108(02)00070-3