Search

Your search keyword '"Mark W. Holladay"' showing total 2 results
Start Over Author "Mark W. Holladay" Publication Year Range Last 10 years
2 results on '"Mark W. Holladay"'

1. Supplementary Data 1 from CEP-32496: A Novel Orally Active BRAFV600E Inhibitor with Selective Cellular and In Vivo Antitumor Activity

Author

Mark W. Holladay, Shripad S. Bhagwat, Michael Williams, Bruce D. Dorsey, Raffaella Faraoni, Julius L. Apuy, Mark A. Ator, Darren E. Insko, Mehran Yazdanian, Dana Gitnick, Mangeng Cheng, Ronald R. Nepomuceno, Kathryn Hunter, Merryl D. Cramer, Hugh Zhao, Michael F. Gardner, Pawel Dobrzanski, Ruwanthi N. Gunawardane, Susan Jones-Bolin, Martin W. Rowbottom, Robert C. Armstrong, Bruce Ruggeri, and Joyce James

Abstract

PDF file - 74K, CEP-32496 Supplemental Data.

Published
2023

2. Discovery and optimization of a highly efficacious class of 5-aryl-2-aminopyridines as FMS-like tyrosine kinase 3 (FLT3) inhibitors

Author

Barbara Belli, Alan Dao, Robert C. Armstrong, Michael F. Gardner, Darren E. Insko, Sunny Abraham, Ron R. Nepomuceno, Gang Liu, Mark W. Holladay, Dana Gitnick, Daniel Brigham, Patrick P. Zarrinkar, Shimin Xu, Xing Liu, Allison M. Rooks, and Ron Christopher

Subjects
Clinical Biochemistry, Pharmaceutical Science, Aminopyridines, Antineoplastic Agents, Pharmacology, Biochemistry, chemistry.chemical_compound, In vivo, Drug Discovery, Humans, Molecular Biology, Tumor xenograft, Quizartinib, Cell Proliferation, CYP3A4, Dose-Response Relationship, Drug, Aryl, Organic Chemistry, Xenograft Model Antitumor Assays, chemistry, fms-Like Tyrosine Kinase 3, Tyrosine Kinase 3, Fms-Like Tyrosine Kinase 3, Molecular Medicine
Abstract

Based on a putative binding mode of quizartinib (AC220, 1), a potent FMS-like tyrosine kinase 3 (FLT3) inhibitor in Phase III clinical development, we have designed de novo a simpler aminopyridine-based hinge binding motif. Further optimization focusing on maximizing in vivo efficacy and minimizing CYP3A4 time-dependent inhibition resulted in a highly efficacious compound (6s) in tumor xenograft model for further preclinical development.

Published
2015

Catalog

Books, media, physical & digital resources
See catalog results