Zobrazeno 1 - 10
of 49
pro vyhledávání: '"Gerald W. Shipps"'
Autor:
Hong Lan, Cliff C. Cheng, Timothy J. Kowalski, Ling Pang, Lixin Shan, Cheng-Chi Chuang, James Jackson, Alberto Rojas-Triana, Loretta Bober, Li Liu, Johannes Voigt, Peter Orth, Xianshu Yang, Jr. Gerald W. Shipps, Joseph A. Hedrick
Publikováno v:
Journal of Lipid Research, Vol 52, Iss 4, Pp 646-656 (2011)
Fatty acid binding protein-4 (FABP4) and FABP5 are two closely related FA binding proteins expressed primarily in adipose tissue and/or macrophages. The small-molecule FABP4 inhibitor BMS309403 was previously reported to improve insulin sensitivity i
Externí odkaz:
https://doaj.org/article/4b996eda763348e98189f8126dd31a7e
Autor:
Craig R. Gibeau, Yao Ma, Gerald W. Shipps, Tian Yuan, Brian R. Lahue, Corey Strickland, Stephane L. Bogen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:2735-2738
Led by the structural information of the screening hit with mDM2 protein, a structure modification of Leu26 moiety of the novel p53–hDM2 inhibitors was conducted. A structure–activity relationship study of 4-substituted piperidines revealed compo
Autor:
Yaolin Wang, Yao Ma, Philip Lipari, Stephane L. Bogen, Cynthia Seidel-Dugan, Yinghui Lin, Asra Mirza, Craig R. Gibeau, Doll Ronald J, Corey Strickland, Giovanna Scapin, Winifred W. Prosise, Diane Rindgen, Paul Reichert, Xiaoying Wang, Ming Liu, Brian R. Lahue, Daniel J. Hicklin, Gerald W. Shipps, Tian Yuan, Elise Seigel, Suxing Liu, W. Robert Bishop, Weidong Pan, Amin A. Nomeir, Latha G. Nair
Publikováno v:
ACS Medicinal Chemistry Letters. 7:324-329
A new subseries of substituted piperidines as p53-HDM2 inhibitors exemplified by 21 has been developed from the initial lead 1. Research focused on optimization of a crucial HDM2 Trp23-ligand interaction led to the identification of 2-(trifluoromethy
Autor:
Liang Zhu, Weihong Jin, Xin Yao, Hong Mei, Abdul Basit Alhassan, William T. Windsor, Donna Carr, Li Xiao, Sunil Paliwal, Neng-Yang Shih, Sun Robert, Gerald W. Shipps, Sobhana Babu Boga, Yang Nan, Joseph Kelly, Alexei V. Buevich, Brian Long, Paul Kirschmeier, Bradley Sherborne, Kiran Muppalla, Stuart Black, Hon-Chung Tsui, Doll Ronald J, Hugh Y. Zhu, Stacey A. Taylor, Subrahmanyam Gudipati, Gongjie Liu, Alan B. Cooper, Li-Kang Zhang, Kathleen Cox, Robert Bishop, David Hesk, Yongqi Deng, Alan Hruza, Mehul D. Patel, Xiaolei Gao, Priya Dayananth, Tong Wang, Desai Jagdish A, Wang James J-S, Ahmed A. Samatar
[Image: see text] The emergence and evolution of new immunological cancer therapies has sparked a rapidly growing interest in discovering novel pathways to treat cancer. Toward this aim, a novel series of pyrrolidine derivatives (compound 5) were ide
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ab2250ac0d2e55d7a37e61d512ca2156
https://europepmc.org/articles/PMC6047169/
https://europepmc.org/articles/PMC6047169/
Autor:
Nicolas Bruneau-Latour, Gerald W. Shipps, Chantal Grand-Maître, Martin Dery, Vibha Oza, Michael A. Luther, Lea Constantineau-Forget, Stephane Ciblat, Michael A. Patane, Jedd Levine, Edith Bellavance, Matthew J. Kostura, Alan B. Cooper, Arshad Siddiqui
Publikováno v:
Bioorganicmedicinal chemistry letters. 28(5)
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
Autor:
Arshad Siddiqui, Chantal Grand-Maître, Alan B. Cooper, Martin Dery, Edith Bellavance, Stephane Ciblat, Michael A. Luther, Matthew J. Kostura, Nicolas Bruneau-Latour, Vibha Oza, Michael A. Patane, Gerald W. Shipps, Lea Constantineau-Forget, Jedd Levine
Publikováno v:
Bioorganicmedicinal chemistry letters. 27(18)
A class of substituted 1-thiazol-2-yl-N-3-methyl-1H-pyrozole-5-carboxylic acid derivatives was found to have potent anti-proliferative activity against a broad range of tumor cell lines. A compound from this class (14) was profiled across a broad pan
Autor:
Gerald W. Shipps, Doll Ronald J, Yao Ma, Latha G. Nair, Stephane L. Bogen, Brian R. Lahue, Weidong Pan, Yaolin Wang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:1983-1986
The discovery of 3,3-disubstituted piperidine 1 as novel p53–HDM2 inhibitors prompted us to implement subsequent SAR follow up directed towards piperidine core modifications. Conformational restrictions and further functionalization of the piperidi
Autor:
Gerald W. Shipps, Brian R. Lahue, Yaolin Wang, Yao Ma, Timothy J. Guzi, Craig R. Gibeau, Zhuyan Guo, Stephane L. Bogen
Publikováno v:
ACS Medicinal Chemistry Letters. 5:572-575
Introduction of an aliphatic side chain to a key position of a novel piperidine-based HDM2 inhibitor scaffold resulted in significant potency gains, enabling further series progression.
Autor:
Manami Shizuka, Margarita Kirova-Snover, Yao Ma, Yaolin Wang, Weidong Pan, Mark A. Miccoy, Brian R. Lahue, Matthew E. Voss, Stephane L. Bogen, Timothy J. Guzi, Latha G. Nair, Yuan Liu, Graig R. Gibeau, Gerald W. Shipps, Tian Yuan, W. Brent Clayton
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:1026-1030
The present invention provides a compound of Formula I (The formula should be inserted here) as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also