Zobrazeno 1 - 10
of 25
pro vyhledávání: '"Steve Wenglowsky"'
Autor:
Victoria Brown, Nealia House, Phil Ramsden, Karen Ho, Hsin-Jung Wu, Erik Wilker, Jian Guo, Maxine Chen, Douglas Wilson, Neil Bifulco, Steve Wenglowsky, Yoon Jong Choi, Kerrie Faia
Publikováno v:
Cancer Research. 83:P6-10
Cyclin-dependent kinase 4/6 (CDK4/6) inhibitors are standard of care in combination with endocrine therapy in advanced hormone receptor-positive (HR+), human epidermal growth factor receptor 2 negative (HER2-) breast cancer. Despite improved progress
Autor:
Victoria Brown, Phil Ramsden, Nealia House, Richard Vargas, Jian Guo, Ruduan Wang, Riadh Lobbardi, Maxine Chen, Douglas Wilson, Joseph Kim, Neil Bifulco, Michelle Maynard, Emanuele Perola, Dean Zhang, Steve Wenglowsky, Yoon Jong Choi
Publikováno v:
Cancer Research. 82:2306-2306
Background: Cyclin-dependent kinases (CDK) are a class of enzymes that, along with their regulatory cyclin binding partners, drive cell cycle progression. Cell cycle dysregulation is a hallmark of cancer and targeting its genetic drivers can confer t
Autor:
Emily Rozsahegyi, Ruduan Wang, Riadh Lobbardi, Grace O. Silva, Joseph L. Kim, Dean Zhang, Victoria Tzortziou Brown, Jian Guo, Richard Vargas, Megan A. Hatlen, Marion Dorsch, Doug Wilson, Yoon Jin Choi, Rich Woessner, Phil Ramsden, Neil Bifulco, Michelle Maynard, Faith Stevison, Emanuele Perola, Rob Meissner, Klaus P. Hoeflich, Yeon Seo Choi, Tim LaBranche, Steve Wenglowsky
Publikováno v:
Cancer Research. 81:1279-1279
Background: Cyclin dependent kinases (CDK) comprise a family of proteins which are activated upon cyclin binding to promote cell cycle progression. Historically, CDK family inhibitors have had limited utility in the clinic due to 1) toxicities associ
Autor:
Victoria Dinkel, Jonas Grina, David A. Moreno, Simon Mathieu, Joshua D. Hansen, Kevin Rasor, Gregg Hastings, Walter C. Voegtli, Guy Vigers, Sumeet Rana, Joachim Rudolph, Susan L. Gloor, Ellen R. Laird, Li Ren, Steve Wenglowsky, Brandon S. Willis, Hillary L. Sturgis
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:1923-1927
Herein we describe the design of a novel series of ATP competitive B-Raf inhibitors via structure-based methods. These 3-N-methylquinazoline-4(3H)-one based inhibitors exhibit both excellent cellular potency and striking B-Raf selectivity. Optimizati
Autor:
Alexandre J. Buckmelter, Kateri A. Ahrendt, Susan L. Gloor, Ellen R. Laird, Steve Wenglowsky, Nathalie Klopfenstein, Bainian Feng, Xianfeng Li, Jonas Grina, Li Ren, Brad Newhouse, Zhaoyang Wen, Walter C. Voegtli, Joachim Rudolph
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:5896-5899
This Letter details the synthesis and evaluation of imidazo[4,5-b]pyridines as inhibitors of B-Raf kinase. These compounds bind in a DFG-in, αC-helix out conformation of B-Raf, which is a binding mode associated with significant kinase selectivity.
Autor:
Joachim Rudolph, Jason Boggs, Yingqing Ran, Po-Chang Chiang, Edna F. Choo, Jonas Grina, Yong Cui, Steve Wenglowsky
Publikováno v:
International Journal of Pharmaceutics. 454:241-248
It is well acknowledged that oral bioavailability of a drug candidate is often influenced by factors such as the permeability, physico-chemical properties, and metabolism of the drug. Among the physico-chemical properties, solubility and dissolution
Autor:
Leonid Beigelman, Hailong Zhang, Benjamin T. Woodard, Christine Lemieux, Guy Vigers, Vlad Serebryany, Brad O. Buckman, Bin Wang, Scott D. Seiwert, Barbra J. Brandhuber, Steve Wenglowsky, Stengel Peter J, Andrews Steven W, Lawrence M. Blatt, Kennedy April L, Doherty George Andrew, John A. Josey, Joshua Ballard, Mary Geck Do, Madduru Machender R, Jiang Yutong, Kevin Ronald Condroski, Michael Lyon
Publikováno v:
Journal of Medicinal Chemistry. 57:1753-1769
HCV serine protease NS3 represents an attractive drug target because it is not only essential for viral replication but also implicated in the viral evasion of the host immune response pathway through direct cleavage of key proteins in the human inna
Autor:
Steve Wenglowsky
Publikováno v:
Expert Opinion on Therapeutic Patents. 23:281-298
Numerous heterocycles occur as recurring motifs in the design of kinase inhibitors. Pyrazolo[3,4-b]pyridine has proved particularly versatile due to its ability to interact with kinases via multiple binding modes. As such, this scaffold has been clai
Autor:
Janet Gunzner-Toste, Edna F. Choo, Bruno Alicke, Stephen E. Gould, Rebecca Pulk, Ellen R. Laird, Zhaoyang Wen, Li Ren, Jonas Grina, Jason Boggs, David A. Moreno, Joachim Rudolph, Alexandre J. Buckmelter, Simon Mathieu, Guiling Zhao, Stefan Gradl, Walter C. Voegtli, Yingqing Ran, Ignacio Aliagas, Joshua D. Hansen, Georgia Hatzivassiliou, Wendy Lee, Victoria Dinkel, Steve Wenglowsky, Gregg Hastings, Susan L. Gloor
Publikováno v:
Journal of Medicinal Chemistry. 55:2869-2881
Recent clinical data provided proof-of-concept for selective B-Raf inhibitors in treatment of B-Raf(V600E) mutant melanoma. Pyrazolopyridine-type B-Raf inhibitors previously described by the authors are potent and selective but exhibit low solubility