Zobrazeno 1 - 10
of 39
pro vyhledávání: '"Charles A. Omer"'
Autor:
Terry MacIntyre, Brian Aquila, Edward J. Hennessy, Naomi Laing, Vibha Oza, David Whitston, Victor Kamhi, Jamal Carlos Saeh, Lillian Castriotta, Li Sha, Troy Patterson, Christopher Huntington, Danyang Li, Haiyun Wang, Charles A. Omer, Alexander Hird, Melissa Vasbinder, Donald J. Cook, Michael T. Rooney, Galina Repik, Maureen Hattersley, Ammar Adam
Publikováno v:
Journal of Medicinal Chemistry. 56:9897-9919
A series of dimeric compounds based on the AVPI motif of Smac were designed and prepared as antagonists of the inhibitor of apoptosis proteins (IAPs). Optimization of cellular potency, physical properties, and pharmacokinetic parameters led to the id
Autor:
Naomi Laing, Nicholas A. Larsen, Jamal Carlos Saeh, Charles A. Omer, Haiyun Wang, Andrew D. Ferguson, Terry MacIntyre, Brian Aquila, Edward J. Hennessy, Li Sha
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:1690-1694
A series of structurally unique Smac mimetics that act as antagonists of inhibitor of apoptosis proteins (IAPs) has been discovered. While most previously described Smac mimetics contain the proline ring (or a similar cyclic motif) found in Smac, a k
Autor:
Kevin Webster, Zhong Ying Liu, Patrick A. Zweidler-McKay, Haiyun Wang, Charles A. Omer, Jeffrey L. Brown, Peter E. Zage, Lizhi Zeng, Terry MacIntyre, Ethan Hoffmann, Dave Whitston, Tao Wang, Kenneth S. Thress
Publikováno v:
Molecular Cancer Therapeutics. 8:1818-1827
Tropomyosin-related kinases (TrkA, TrkB, and TrkC) are receptor tyrosine kinases that, along with their ligands, the neurotrophins, are involved in neuronal cell growth, development, and survival. The Trk-neurotrophin pathway may also play a role in
Autor:
Carrie L. Balliet, Srinivasu Poondru, Charles A. Omer, Davies Audrey, Thomas Gero, Scott David, Donald J. Cook, Maria-Elena Theoclitou, Boris Tyurin, Michael Zinda
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:697-700
3-amido-4-anilinoquinolines are potent and highly selective inhibitors of CSF-1R. Their synthesis and SAR is reported, along with initial efforts to optimize the physical properties and PK through modifications at the quinoline 6- and 7-positions.
Autor:
Lisa Drew, Les A. Dakin, Boris Tyurin, Kirsten Bell, Maureen Hattersley, Scott David, Xiaolan Zheng, Cheryl Campbell, Thomas Gero, Donald J. Cook, Charles A. Omer, David J. Del Valle
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:701-705
The optimization of compounds from the 3-amido-4-anilinoquinolines series of CSF-1R kinase inhibitors is described. The series has excellent activity and kinase selectivity. Excellent physical properties and rodent PK profiles were achieved through t
Autor:
J. Christopher Culberson, Steven M. Pitzenberger, Charles A. Omer, Michael J. Bogusky, Scott D. Mosser, Kenneth S. Koblan, S. Jane Desolms, E A Giuliani
Publikováno v:
Protein Science. 4:681-688
Farnesyl-protein transferase (FPTase) catalyzes the posttranslational farnesylation of the cysteine residue located in the carboxyl-terminal tetrapeptide of the Ras oncoprotein. Prenylation of this residue is essential for the membrane association an
Autor:
Charles A. Omer, Tracy L. Deegan, Minwei Ye, Les A. Dakin, Paul Lyne, Maureen Hattersley, Donald J. Cook, Xiaolan Zheng, Stephanos Ioannidis, Brian Aquila, Geraldine Bebernitz, Scott David
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:4794-4797
The bisamide class of kinase inhibitors was identified as being active against CSF-1R. The synthesis and SAR of pyridyl and thiazolyl bisamides are reported, along with the pharmacokinetic properties and in vivo activity of selected examples.
Autor:
Theresa M. Williams, A. David Rodrigues, Douglas C. Beshore, Carolyn A. Buser, Joseph P. Davide, Michelle Ellis-Hutchings, Steven N. Gallicchio, J. Christopher Culberson, Samuel L. Graham, George D. Hartman, Marc Abrams, David C. Heimbrook, and Eileen S. Walsh, Carl F. Homnick, Kenneth S. Koblan, Joel R. Huff, Robert B. Lobell, Joseph J. Lynch, Christine Fernandes, Patricia A. Miller, Jackson B. Gibbs, Charles A. Omer, Kelem Kassahun, Nancy E. Kohl, Ian M. Bell
Publikováno v:
Journal of Medicinal Chemistry. 44:2933-2949
The synthesis, structure-activity relationships, and biological properties of a novel series of imidazole-containing inhibitors of farnesyltransferase are described. Starting from a 3-aminopyrrolidinone core, a systematic series of modifications prov
Publikováno v:
Biochemical and Biophysical Research Communications. 256:584-590
The N-termini of members of the T-cell factor (Tcf) and lymphocyte-enhancement factor (Lef) protein families bind to beta-catenin, forming bipartite transcription factors which regulate expression of genes involved in organismal development and the g
Autor:
Charles A. Omer, Donald N. Cook, Jeffrey W. Johannes, Lisa Drew, Timothy Pontz, Minwei Ye, Paul Lyne, Benjamin Fauber, Brian Aquila, Edward J. Hennessy, Martin Augustin, Haixia Wang, Sangeetha Palakurthi, Steve C. Glossop, Huawei Chen, Stephen Lee, Mario Mörtl, Melissa Vasbinder, Michael Grondine, Tony Cheung, Li Sha, Allan Wu, Jon Read, Minhui Shen, Stefan Steinbacher
Publikováno v:
Journal of medicinal chemistry. 56(5)
B-Raf represents an attractive target for anticancer therapy and the development of small molecule B-Raf inhibitors has delivered new therapies for metastatic melanoma patients. We have discovered a novel class of small molecules that inhibit mutant