Structure-based design of irreversible, tripeptidyl human rhinovirus 3C protease inhibitors containing N-methyl amino acids

Autor: Dragovich, Peter S, Webber, Stephen E, Prins, Thomas J, Zhou, Ru, Marakovits, Joseph T, Tikhe, Jayashree G, Fuhrman, Shella A, Patick, Amy K, Matthews, David A, Ford, Clifford E, Brown, Edward L, Binford, Susan L, Meador, James W, III, Ferre, Rose Ann, Worland, Stephen T

Publikováno v: In Bioorganic & Medicinal Chemistry Letters 1999 9(15):2189-2194

Novel Tricyclic Poly(ADP-ribose) Polymerase-1 Inhibitors with Potent Anticancer Chemopotentiating Activity: Design, Synthesis, and X-ray Cocrystal Structure

Autor: Huw D. Thomas, Anne Ekker, Stephen E. Webber, Christopher R. Calabrese, Nicola J. Curtin, Robert Almassy, Karen A. Maegley, Rena N. Mansour, Lan-Zhen Wang, Robert Arnold Kumpf, A. Hilary Calvert, Cathy Zhang, Scott E. Zook, Jianke Li, Bernard T. Golding, Tikhe Jayashree Girish, Xiao-Hong Yu, Suzanne Kyle, Zdenek Hostomsky, Theodore J. Boritzki, Thoresen Lars Henrik, David Richard Newell, Kanyin E. Zhang, Stacie S. Canan Koch, Roger John Griffin

Publikováno v: Journal of Medicinal Chemistry. 45:4961-4974

A series of novel compounds have been designed that are potent inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1), and the activity and physical properties have been characterized. The new structural classes, 3,4,5,6-tetrahydro-1H-azepino[5,4,3-cd]

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ec741e627bfb818de6119c89a2082ae7
https://doi.org/10.1021/jm020259n

Abstract PR-2: Discovery of p21-activated kinase inhibitor PF-03758309

Autor: Joseph K. T. Lee, Tikhe Jayashree Girish, Ya‐Li Deng, Joseph Piraino, Li Haitao, Djamal Bouzida, Eleanor Dagostino, Chuangxing Guo, Zhang Junhu, Hasam Younis, Kephart Susan Elizabeth, Brion W. Murray, Indrawan James Mcalpine, Jamie Christensen, Marakovits Joseph T, Tod Smeal, Eugenia Kraynov, Cho-Ming Loi, Lisa Guo, Dan Knighton, Catherine Johnson, Yang Anle, Dong Liming

Publikováno v: Molecular Cancer Therapeutics. 8:PR-2

The p21-activated kinase (PAK) family members are key effectors of Rho family GTPases, which act as regulatory switches that control such cellular processes as motility, proliferation, and cell survival. Some members of this family (such as Cdc42) ha

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::1b220446bd808e97bcb76e7a46d06a11
https://doi.org/10.1158/1535-7163.targ-09-pr-2

Discovery of Pyrroloaminopyrazolesas Novel PAK Inhibitors.

Autor: Guo, Chuangxing, McAlpine, Indrawan, Zhang, Junhu, Knighton, Daniel D., Kephart, Susan, Johnson, M. Catherine, Li, Haitao, Bouzida, Djamal, Yang, Anle, Dong, Liming, Marakovits, Joseph, Tikhe, Jayashree, Richardson, Paul, Guo, Lisa C., Kania, Robert, Edwards, Martin P., Kraynov, Eugenia, Christensen, James, Piraino, Joseph, Lee, Joseph

Publikováno v: Journal of Medicinal Chemistry; May2012, Vol. 55 Issue 10, p4728-4739, 12p

Design, synthesis, and evaluation of 3,4-dihydro-2H-[1,4]diazepino[6,7,1-hi]indol-1-ones as inhibitors of poly(ADP-ribose) polymerase.

Autor: Tikhe JG; Pfizer Global R&D--La Jolla Laboratories, 10770 Science Center Drive, San Diego, California 92121, USA. jayashree.tikhe@pfizer.com, Webber SE, Hostomsky Z, Maegley KA, Ekkers A, Li J, Yu XH, Almassy RJ, Kumpf RA, Boritzki TJ, Zhang C, Calabrese CR, Curtin NJ, Kyle S, Thomas HD, Wang LZ, Calvert AH, Golding BT, Griffin RJ, Newell DR

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2004 Oct 21; Vol. 47 (22), pp. 5467-81.