Zobrazeno 1 - 10
of 17
pro vyhledávání: '"Kateri A. Ahrendt"'
Autor:
Augustine N. Vu, Santana P. Garcia, Jenny H. Tran, Adrian A. Godoy, Joaquin M. Mesa, Cassidy M. DiTirro, Kinsey L. Kotsch, Sarah E. Sullivan, Vincent J. Tavalez, Kateri A. Ahrendt
Publikováno v:
Journal of Chemical Education. 100:914-920
Publikováno v:
Biochemistry. 53:202-213
Class II fructose 1,6-bisphosphate aldolase (FBA) is an enzyme critical for bacterial, fungal, and protozoan glycolysis/gluconeogenesis. Importantly, humans lack this type of aldolase, having instead a class I FBA that is structurally and mechanistic
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:
Ben Colson, David A. Moreno, Alisha Arrigo, Yingqing Ran, Kateri A. Ahrendt, Joachim Rudolph, Gregg Hastings, Susan L. Gloor, Steve Wenglowsky
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:912-915
A single crystal was obtained of a lead B-RafV600E inhibitor with low aqueous solubility. The X-ray crystal structure revealed hydrogen-bonded head-to-tail dimers formed by the pyrazolopyridine and sulfonamide groups of a pair of molecules. This obse
Publikováno v:
The Journal of Organic Chemistry. 70:6775-6781
A directed C-H bond activation approach to the synthesis of indans, tetralins, dihydrofurans, dihydroindoles, and other polycyclic aromatic compounds is presented. Cyclization of aromatic ketimines and aldimines containing alkenyl groups tethered at
Publikováno v:
Organic Letters. 5:1301-1303
[reaction: see text] A tetrahydrobis(benzofuran) mescaline analogue has been prepared in six steps and 38% overall yield from (4'-O-methyl)methyl gallate. The key step in this synthesis is a tandem cyclization reaction via directed C[bond]H activatio
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
Publikováno v:
ChemInform. 31
Publikováno v:
ChemInform. 33