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Title: Leveraging Structure-Based Drug Design to Identify Next-Generation MAT2A Inhibitors, Including Brain

Journal Article · · J. Med. Chem.

Research Organization:
Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Sponsoring Organization:
DOE - Office Of Science; INDUSTRY
OSTI ID:
1861844
Journal Information:
J. Med. Chem., Vol. 65, Issue (6)
Country of Publication:
United States
Language:
ENGLISH

References (25)

S-Adenosyl-l-methionine: Beyond the universal methyl group donor journal August 2006
PHENIX: a comprehensive Python-based system for macromolecular structure solution journal January 2010
MTAP Deletions in Cancer Create Vulnerability to Targeting of the MAT2A/PRMT5/RIOK1 Axis journal April 2016
MTAP deletion confers enhanced dependency on the PRMT5 arginine methyltransferase in cancer cells journal February 2016
Disordered methionine metabolism in MTAP/CDKN2A-deleted cancers leads to dependence on PRMT5 journal February 2016
Discovery of AG-270, a First-in-Class Oral MAT2A Inhibitor for the Treatment of Tumors with Homozygous MTAP Deletion journal April 2021
MAT2A Inhibition Blocks the Growth of MTAP-Deleted Cancer Cells by Reducing PRMT5-Dependent mRNA Splicing and Inducing DNA Damage journal February 2021
Fragment-Based Design of a Potent MAT2a Inhibitor and in Vivo Evaluation in an MTAP Null Xenograft Model journal April 2021
Targeting S-adenosylmethionine biosynthesis with a novel allosteric inhibitor of Mat2A journal May 2017
Principles and Applications of Halogen Bonding in Medicinal Chemistry and Chemical Biology journal January 2013
Predicting and Tuning Physicochemical Properties in Lead Optimization: Amine Basicities journal August 2007
A PXR reporter gene assay in a stable cell culture system: CYP3A4 and CYP2B6 induction by pesticides journal December 2004
In Vitro and in Vivo Induction of Cytochrome P450: A Survey of the Current Practices and Recommendations: A Pharmaceutical Research and Manufacturers of America Perspective journal April 2009
Identification of Clinically Used Drugs That Activate Pregnane X Receptors journal October 2010
Evaluation of pregnane X receptor (PXR)-mediated CYP3A4 drug-drug interactions in drug development journal January 2013
Identification and Optimization of Benzimidazole Sulfonamides as Orally Bioavailable Sphingosine 1-Phosphate Receptor 1 Antagonists with in Vivo Activity journal August 2015
Attenuating pregnane X receptor (PXR) activation: A molecular modelling approach journal February 2007
The ABCs of drug transport in intestine and liver: efflux proteins limiting drug absorption and bioavailability journal January 2004
Blood-brain barrier active efflux transporters: ATP-binding cassette gene family journal January 2005
Structure−Brain Exposure Relationships journal December 2006
The Irwin Test and Functional Observational Battery (FOB) for Assessing the Effects of Compounds on Behavior, Physiology, and Safety Pharmacology in Rodents journal September 2018
[20] Processing of X-ray diffraction data collected in oscillation mode book January 1997
XDS journal January 2010
Tools for ligand validation in Coot journal March 2017
REFMAC 5 for the refinement of macromolecular crystal structures journal March 2011