Zobrazeno 1 - 10
of 44
pro vyhledávání: '"Karen, Lackey"'
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:66-70
A series of novel, potent 4-aminothienopyridine B-Raf kinase inhibitors was designed and synthesized using knowledge-based design. Compounds 5f, and 6k exhibited not only excellent potency in both enzyme assay (IC50 = 5.1, 16.6 nM) and cellular assay
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a749ac8970b90d3c5dd7e232e9811237
https://doi.org/10.1016/j.bmcl.2012.11.020
https://doi.org/10.1016/j.bmcl.2012.11.020
Autor:
David H. Drewry, Eidarus Salah, Joel Morris, John P. Overington, Jowita Mikolajczyk, Francis Atkinson, Alexander Tropsha, Karen Lackey, Jonathan M. Elkins, Kamal R. Abdul Azeez, Mark Kunkel, Nikolai Sepetov, Daniel J. Price, Xi Ping Huang, Eric C. Polley, Timothy M. Willson, Beverly A. Teicher, Vita Fedele, Susanne Müller, Ayman Al Haj Zen, William J. Zuercher, Eugene N. Muratov, Sergei Romanov, Paul Bamborough, Bryan L. Roth, Stefan Knapp, Denis Fourches, M. Szklarz
Despite the success of protein kinase inhibitors as approved therapeutics, drug discovery has focused on a small subset of kinase targets. Here we provide a thorough characterization of the Published Kinase Inhibitor Set (PKIS), a set of 367 small-mo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ef3b54fff9b892e25076832396fb828f
Autor:
Karen Lackey, Bruce Roth
Edited by two renowned medicinal chemists who have pioneered the development of personalized therapies in their respective fields, this authoritative analysis of what is already possible is the first of its kind, and the only one to focus on drug dev
Autor:
Ronda G. Davis-Ward, Felix Deanda, Octerloney B. McDonald, Robert N. Hunter, Patrick R. Maloney, Edgar R. Wood, Vicente Samano, Karen Lackey
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:5378-5383
The synthesis of several novel aza-stilbene derivatives was carried out. The compounds were tested for their c-RAF enzyme inhibition. Compound 27 possesses significant potency against c-RAF and demonstrates selectivity over other protein kinases. A h
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f1af6b219f0fd17fd42af625350f538e
https://doi.org/10.1016/j.bmcl.2006.07.063
https://doi.org/10.1016/j.bmcl.2006.07.063
Autor:
Kimberly G. Petrov, Ann Louise Walker, Yu Guo, Malcolm Clive Carter, David W. Rusnak, Scott Howard Dickerson, Robert A. Mook, Cassandra A. Gauthier, Edgar R. Wood, Karen Lackey, G. Stuart Cockerill, Yue-Mei Zhang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:4686-4691
Synthetic modifications on a 6-furanylquinazoline scaffold to optimize the dual ErbB-1/ErbB-2 tyrosine kinase inhibition afforded consistent SAR whereby a 4-(3-fluorobenzyloxy)-3-haloanilino provided the best enzyme potency and cellular selectivity.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fb0e36c5b474465ea5bf127c87c05182
https://doi.org/10.1016/j.bmcl.2006.05.090
https://doi.org/10.1016/j.bmcl.2006.05.090
Autor:
Anne T. Truesdale, Octerloney B. McDonald, Byron Ellis, Christopher Pennisi, Edgar R. Wood, David W. Rusnak, Karen Lackey, Scott Howard Dickerson, Krystal J. Alligood, Tona M. Gilmer, Derek Yuan, Lisa M. Shewchuk, Anne M. Hassell, Earnest Horne
Publikováno v:
Cancer Research. 64:6652-6659
GW572016 (Lapatinib) is a tyrosine kinase inhibitor in clinical development for cancer that is a potent dual inhibitor of epidermal growth factor receptor (EGFR, ErbB-1) and ErbB-2. We determined the crystal structure of EGFR bound to GW572016. The c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::6c95f3a757694358225cd7c815d1bea3
https://doi.org/10.1158/0008-5472.can-04-1168
https://doi.org/10.1158/0008-5472.can-04-1168
Autor:
Christine R. Hoffman, Karen Lackey, Krystal J. Alligood, Mary B. Moyer, Sue H. Kadwell, Earnest Horne, Perry Scott Brignola, Wilson B. Knight, Kevin Blackburn, J. Darren Stuart, Edgar R. Wood, H. Luke Carter
Publikováno v:
Journal of Biological Chemistry. 277:1576-1585
Epidermal growth factor receptor (EGFR), ErbB-2, and ErbB-4 are members of the type 1 receptor tyrosine kinase family. Overexpression of these receptors, especially ErbB-2 and EGFR, has been implicated in multiple forms of cancer. Inhibitors of EGFR
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::61284b3bec4306cfdbc8d396eae850e9
https://doi.org/10.1074/jbc.m105907200
https://doi.org/10.1074/jbc.m105907200
Autor:
Renae M. Crosby, Christopher Mohr, Daniel D. Sternbach, Steven R. Jordan, Krystal J. Alligood, Paul L. Feldman, Paul S. Charifson, George F. Dorsey, Conrad W. Hummel, Judd Berman, Lisa M. Shewchuk, Gregory J. Pacofsky, Marc Rodriguez, Tona M. Gilmer, Karen Lackey
Publikováno v:
Journal of Medicinal Chemistry. 41:1894-1908
The design, synthesis, and evaluation of dipeptide analogues as ligands for the pp60c-src SH2 domain are described. The critical binding interactions between Ac-Tyr-Glu-N(n-C5H11)2 (2) and the protein are established and form the basis for our struct
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::345090efdacd7e7720467d586c6bb6b8
https://doi.org/10.1021/jm970853a
https://doi.org/10.1021/jm970853a
Autor:
Bruce D. Roth, Karen Lackey
Publikováno v:
Methods and Principles in Medicinal Chemistry ISBN: 9783527677252
Medicinal Chemistry Approaches to Personalized Medicine
Medicinal Chemistry Approaches to Personalized Medicine
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::688eafca926d667e886885fe3eaafa50
https://doi.org/10.1002/9783527677252
https://doi.org/10.1002/9783527677252
Autor:
Bruce D. Roth, Karen Lackey
Publikováno v:
Medicinal Chemistry Approaches to Personalized Medicine
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::4b44b5e048ba7a06a416da8575f260d3
https://doi.org/10.1002/9783527677252.ch01
https://doi.org/10.1002/9783527677252.ch01