Discovery of AG-270, a First-in-Class Oral MAT2A Inhibitor for the Treatment of Tumors with Homozygous MTAP Deletion

MAT2A inhibition blocks the growth of MTAP-deleted cancer cells by reducing PRMT5-dependent mRNA splicing and inducing DNA damage

(2021) Peter Kalev et al.   CANCER CELL

Anti-tumor Activity of the Type I PRMT Inhibitor, GSK3368715, Synergizes with PRMT5 Inhibition through MTAP Loss

(2019) Andrew Fedoriw et al.   CANCER CELL

Targeting S-adenosylmethionine biosynthesis with a novel allosteric inhibitor of Mat2A

(2017) Casey L Quinlan et al.   Nature Chemical Biology

Intramolecular Hydrogen Bond Expectations in Medicinal Chemistry

(2017) Fabrizio Giordanetto et al.   ACS Medicinal Chemistry Letters

Crystallography captures catalytic steps in human methionine adenosyltransferase enzymes

(2016) Ben Murray et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Disordered methionine metabolism in MTAP/CDKN2A-deleted cancers leads to dependence on PRMT5

(2016) Konstantinos J. Mavrakis et al.   SCIENCE

MTAPdeletion confers enhanced dependency on the PRMT5 arginine methyltransferase in cancer cells

(2016) Gregory V. Kryukov et al.   SCIENCE

MTAP Deletions in Cancer Create Vulnerability to Targeting of the MAT2A/PRMT5/RIOK1 Axis

(2016) Katya Marjon et al.   Cell Reports

Arginine methyltransferase PRMT5 is essential for sustaining normal adult hematopoiesis

(2015) Fan Liu et al.   JOURNAL OF CLINICAL INVESTIGATION

A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models

(2015) Elayne Chan-Penebre et al.   Nature Chemical Biology

2′,6′-Dihalostyrylanilines, Pyridines, and Pyrimidines for the Inhibition of the Catalytic Subunit of Methionine S-Adenosyltransferase-2

(2014) Vitaliy M. Sviripa et al.   JOURNAL OF MEDICINAL CHEMISTRY

Insight intoS-adenosylmethionine biosynthesis from the crystal structures of the human methionine adenosyltransferase catalytic and regulatory subunits

(2013) Naeem Shafqat et al.   BIOCHEMICAL JOURNAL

Regulation of constitutive and alternative splicing by PRMT5 reveals a role for Mdm4 pre-mRNA in sensing defects in the spliceosomal machinery

(2013) M. Bezzi et al.   GENES & DEVELOPMENT

Amplified and Homozygously Deleted Genes in Glioblastoma: Impact on Gene Expression Levels

(2012) Inês Crespo et al.   PLoS One

REFMAC5 for the refinement of macromolecular crystal structures

(2011) Garib N. Murshudov et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Screening a fragment cocktail library using ultrafiltration

(2011) Sayaka Shibata et al.   ANALYTICAL AND BIOANALYTICAL CHEMISTRY

XDS

(2010) Wolfgang Kabsch   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Features and development ofCoot

(2010) P. Emsley et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

PHENIX: a comprehensive Python-based system for macromolecular structure solution

(2010) Paul D. Adams et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Prmt5 is essential for early mouse development and acts in the cytoplasm to maintain ES cell pluripotency

(2010) W.-W. Tee et al.   GENES & DEVELOPMENT

Intramolecular Hydrogen Bonding in Medicinal Chemistry

(2010) Bernd Kuhn et al.   JOURNAL OF MEDICINAL CHEMISTRY

electronic Ligand Builder and Optimization Workbench(eLBOW): a tool for ligand coordinate and restraint generation

(2009) Nigel W. Moriarty et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY