A
Anne Marie Velasco
Researcher at Ambit Biosciences
Publications - 4
Citations - 2674
Anne Marie Velasco is an academic researcher from Ambit Biosciences. The author has contributed to research in topics: FLT3 Inhibitor & ABL. The author has an hindex of 4, co-authored 4 publications receiving 2553 citations.
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Journal ArticleDOI
A small molecule-kinase interaction map for clinical kinase inhibitors.
Miles A. Fabian,William H. Biggs,Daniel K. Treiber,Corey E. Atteridge,Mihai Azimioara,Mihai Azimioara,Michael G. Benedetti,Michael G. Benedetti,Todd A. Carter,Pietro Ciceri,Philip T. Edeen,Mark Floyd,Julia M. Ford,Margaret Galvin,Jay L Gerlach,Jay L Gerlach,Robert M. Grotzfeld,Sanna Herrgard,Darren E. Insko,Michael A Insko,Andiliy G. Lai,Jean-Michel Lélias,Shamal A. Mehta,Zdravko V. Milanov,Anne Marie Velasco,Lisa M. Wodicka,Hitesh K. Patel,Patrick P. Zarrinkar,David J. Lockhart +28 more
TL;DR: An efficient way to determine kinase inhibitor specificity by measuring binding of small molecules to the ATP site of kinases is described, which represents a systematic small molecule-protein interaction map for clinical compounds across a large number of related proteins.
Journal ArticleDOI
Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases
Todd A. Carter,Lisa Wodicka,Neil P. Shah,Anne Marie Velasco,Miles A. Fabian,Daniel K. Treiber,Zdravko V. Milanov,Corey E. Atteridge,William H. Biggs,Philip T. Edeen,Mark Floyd,Julia M. Ford,Robert M. Grotzfeld,Sanna Herrgard,Darren E. Insko,Shamal A. Mehta,Hitesh Patel,William Pao,Charles L. Sawyers,Harold E. Varmus,Patrick Parvis Zarrinkar,David J. Lockhart +21 more
TL;DR: The results highlight the strategy of screening existing clinical compounds against newly identified drug-resistant mutant variants to find compounds that may serve as starting points for the development of next-generation drugs, or that could be used directly to treat patients that have acquired resistance to first-generation targeted therapy.
Journal ArticleDOI
Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor.
Qi Chao,Kelly G. Sprankle,Robert M. Grotzfeld,Andiliy G. Lai,Todd A. Carter,Anne Marie Velasco,Ruwanthi N. Gunawardane,Merryl D. Cramer,Michael F. Gardner,Joyce James,Patrick P. Zarrinkar,Hitesh K. Patel,Shripad Bhagwat +12 more
TL;DR: Compound 7 (AC220) was identified from this series to be the most potent and selective FLT3 inhibitor with good pharmaceutical properties, excellent PK profile, and superior efficacy and tolerability in tumor xenograft models.
Journal ArticleDOI
Arylcarboxyamino-substituted diaryl ureas as potent and selective FLT3 inhibitors.
Hitesh K. Patel,Robert M. Grotzfeld,Andiliy G. Lai,Shamal A. Mehta,Zdravko V. Milanov,Qi Chao,Kelly G. Sprankle,Todd A. Carter,Anne Marie Velasco,Miles A. Fabian,Joyce James,Daniel K. Treiber,David J. Lockhart,Patrick P. Zarrinkar,Shripad Bhagwat +14 more
TL;DR: A series of diaryl ureas with an amide substitution at the 4-position was prepared and found to be potent and selective FLT3 inhibitors with good oral bioavailability and efficacy in a tumor xenograft model.