Zobrazeno 1 - 7
of 7
pro vyhledávání: '"Hillary L. Sturgis"'
Autor:
Wen-I Wu, Walter C Voegtli, Hillary L Sturgis, Faith P Dizon, Guy P A Vigers, Barbara J Brandhuber
Publikováno v:
PLoS ONE, Vol 5, Iss 9, p e12913 (2010)
AKT1 (NP_005154.2) is a member of the serine/threonine AGC protein kinase family involved in cellular metabolism, growth, proliferation and survival. The three human AKT isozymes are highly homologous multi-domain proteins with both overlapping and d
Externí odkaz:
https://doaj.org/article/deb7442d250247b78775ee4e8843f54a
Autor:
Kevin Ronald Condroski, Susan P. Rhodes, Maralee McVean, Walter C. Voegtli, Christopher F. Kraser, Walter E. DeWolf, Lance A. Williams, Deborah Anderson, Hillary L. Sturgis, Boyd Steven A, Ronald Jay Hinklin, Jonathan B. Houze, Brian R. Baer, Thomas Daniel Aicher
Publikováno v:
Journal of Medicinal Chemistry. 57:8180-8186
Glucokinase (GK) is the rate-limiting step for insulin release from the pancreas in response to high levels of glucose. Flux through GK also contributes to reducing hepatic glucose output. Since many individuals with type 2 diabetes appear to have an
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:
Steve Wenglowsky, Hillary L. Sturgis, Walter C. Voegtli, Joachim Rudolph, David A. Moreno, Susan L. Gloor, Tyler Risom, Ellen R. Laird, Li Ren
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(19)
Cell potent inhibitors of B-Raf V600E that bind to the kinase in the DFG-out conformation are reported. These compounds utilize the hinge-binding group and lipophilic linker from a previously disclosed series of B-Raf V600E inhibitors that bind to th
Autor:
Jonas Grina, David A. Moreno, Alexandre J. Buckmelter, Ellen R. Laird, Steve Wenglowsky, Li Ren, Jeongbeob Seo, Bainian Feng, Simon Mathieu, Stefan Gradl, Joachim Rudolph, Susan L. Gloor, Paul Lunghofer, Brad Newhouse, Walter C. Voegtli, Kateri A. Ahrendt, Joshua D. Hansen, Tyler Risom, Zhaoyang Wen, Hillary L. Sturgis
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(18)
Structure–activity relationships around a novel series of B-RafV600E inhibitors are reported. The enzymatic and cellular potencies of inhibitors derived from two related hinge-binding groups were compared and3-methoxypyrazolopyridine proved to be s
Autor:
Kim Malesky, Victoria Dinkel, Bruno Alicke, Hillary L. Sturgis, Simon Mathieu, Ignacio Aliagas, Sumeet Rana, Kyung Song, Brandon S. Willis, Bonnie Liu, Nikole Randolph, Yingqing Ran, Scott Savage, Wendy B. Young, Edna F. Choo, Ellen R. Laird, Steve Wenglowsky, Stephen E. Gould, Bainian Feng, Michael Shrag, Joachim Rudolph, Li Ren, Kateri A. Ahrendt, Nicholas J. Raddatz, Walter C. Voegtli, Tyler Risom, LeAnn T. Selby, Jonas Grina, Zhaoyang Wen, Susan L. Gloor, Janet Gunzner-Toste, Wen-I Wu, Alexandre J. Buckmelter, Brad Newhouse, Richard Woessner, Stefan Gross, Joshua D. Hansen, Georgia Hatzivassiliou
Publikováno v:
ACS medicinal chemistry letters. 2(5)
The V600E mutation of B-Raf kinase results in constitutive activation of the MAPK signaling pathway and is present in approximately 7% of all cancers. Using structure-based design, a novel series of pyrazolopyridine inhibitors of B-Raf(V600E) was dev
Autor:
Lu, Min1, Li, Pingping1, Bandyopadhyay, Gautam1, Lagakos, William1, DeWolf Jr, Walter E.2, Alford, Taylor2, Chicarelli, Mark Joseph2, Williams, Lance2, Anderson, Deborah A.2, Baer, Brian R.2, McVean, Maralee2, Conn, Marion3, Véniant, Murielle M.4, Coward, Peter3 pcoward@amgen.com
Publikováno v:
PLoS ONE. Feb2014, Vol. 9 Issue 2, p1-10. 10p.