Zobrazeno 1 - 10
of 19
pro vyhledávání: '"Walter C Voegtli"'
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:
Scott Alan Pratt, Patrice Lee, Thomas Daniel Aicher, John Fischer, Kevin Ronald Condroski, Brian R. Baer, Boyd Steven A, Mark D. Chicarelli, Walter C. Voegtli, Walter E. DeWolf, Francis X. Sullivan, Eli M. Wallace, Nickolas A. Neitzel, Lance A. Williams, Ronald Jay Hinklin, Turner Timothy M, Ajay Singh, Gary P. Hingorani, Michele Frank
Publikováno v:
Bioorganicmedicinal chemistry. 28(1)
Glucose flux through glucokinase (GK) controls insulin release from the pancreas in response to high levels of glucose. Flux through GK is also responsible for reducing hepatic glucose output. Since many individuals with type 2 diabetes appear to hav
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:
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:
Ajay Singh, Lee Wai-Man, Kevin Ronald Condroski, Patrice Lee, Thomas Daniel Aicher, Laurie Thomas, Ronald Jay Hinklin, Boyd Steven A, Mark Joseph Chicarelli, Walter E. DeWolf, Lance Williams, Walter C. Voegtli
Publikováno v:
Journal of Medicinal Chemistry. 56:7669-7678
Glucose flux through glucokinase (GK) controls insulin release from the pancreas in response to high glucose concentrations. Glucose flux through GK also contributes to reducing hepatic glucose output. Because many individuals with type 2 diabetes ap
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
Autor:
Bryson Rast, Alexandre J. Buckmelter, Li Ren, Walter C. Voegtli, Greg Miknis, Robert J. Ely, Tony Morales, Guy Vigers, Nikole Randolph, Ellen R. Laird, Michele Callejo, Joseph P. Lyssikatos, Sarah Galbraith, Matthew Martinson, Stephen T. Schlachter, Barbara J. Brandhuber, Steve Wenglowsky
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:1243-1247
The development of inhibitors of B-Raf(V600E) serine-threonine kinase is described. Various head-groups were examined to optimize inhibitor activity and ADME properties. Several of the head-groups explored, including naphthol, phenol and hydroxyamidi
Autor:
Deborah L. Perlstein, Amy C. Rosenzweig, Walter C. Voegtli, Jie Ge, Monika Sommerhalter, JoAnne Stubbe
Publikováno v:
Biochemistry. 43:7736-7742
Class I ribonucleotide reductases (RNRs) catalyze the reduction of ribonucleotides to deoxyribonucleotides. Eukaryotic RNRs comprise two subunits, the R1 subunit, which contains substrate and allosteric effector binding sites, and the R2 subunit, whi
Autor:
Lana Saleh, Amy C. Rosenzweig, Walter C. Voegtli, Jeffrey Baldwin, J. Martin Bollinger, Monika Sommerhalter
Publikováno v:
Journal of the American Chemical Society. 125:15822-15830
The R2 subunit of Escherichia coli ribonucleotide reductase contains a dinuclear iron center that generates a catalytically essential stable tyrosyl radical by one electron oxidation of a nearby tyrosine residue. After acquisition of Fe(II) ions by t