Fragment-Based Design of a Potent MAT2a Inhibitor and <i>in Vivo</i> Evaluation in an MTAP Null Xenograft Model
Claudia De Fusco, Marianne Schimpl, Ulf Börjesson, Tony Cheung, Iain T. Collie, Laura Evans, Priyanka Narasimhan, Christopher J. Stubbs, Mercedes Vázquez–Chantada, David J. Wagner, Michael Grondine, Matthew G. Sanders, Sharon Tentarelli, E. Underwood, Argyrides Argyrou, James M. Smith, James T. Lynch, Elisabetta Chiarparin, Graeme R. Robb, Sharan K. Bagal, James S. Scott
Abstract
was able to induce antitumor response in an MTAP knockout HCT116 xenograft model.
Topics & Concepts
In vivoMethionine AdenosyltransferaseChemistryMethylationIn vitroMethionineMetaboliteCancer researchAllosteric regulationBiochemistryEnzymeGeneGeneticsBiologyAmino acidCancer-related gene regulationEpigenetics and DNA MethylationHistone Deacetylase Inhibitors Research