Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of MTAP-Deleted Cancers

PF-06939999, a potent and selective PRMT5 inhibitor, in patients with advanced or metastatic solid tumors: A phase 1 dose escalation study.

(2021) Jordi Rodon Ahnert et al.   JOURNAL OF CLINICAL ONCOLOGY

Discovery and Pharmacological Characterization of JNJ-64619178, a Novel Small-Molecule Inhibitor of PRMT5 with Potent Antitumor Activity

(2021) Dirk Brehmer et al.   MOLECULAR CANCER THERAPEUTICS

Fragments: where are we now?

(2020) James Osborne et al.   BIOCHEMICAL SOCIETY TRANSACTIONS

PRMT5 Is Required for T Cell Survival and Proliferation by Maintaining Cytokine Signaling

(2020) Yukinori Tanaka et al.   Frontiers in Immunology

438OMETEOR-1: A phase I study of GSK3326595, a first-in-class protein arginine methyltransferase 5 (PRMT5) inhibitor, in advanced solid tumours

(2019) L L Siu et al.   ANNALS OF ONCOLOGY

Oncogenic Signaling Pathways in The Cancer Genome Atlas

(2018) Francisco Sanchez-Vega et al.   CELL

Determination of Affinity and Residence Time of Potent Drug-Target Complexes by Label-free Biosensing

(2018) John G. Quinn et al.   JOURNAL OF MEDICINAL CHEMISTRY

LLY-283, a Potent and Selective Inhibitor of Arginine Methyltransferase 5, PRMT5, with Antitumor Activity

(2018) Zahid Q. Bonday et al.   ACS Medicinal Chemistry Letters

PRMT5 is essential for B cell development and germinal center dynamics

(2018) Ludivine C. Litzler et al.   Nature Communications

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

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

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

Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666

(2015) Kenneth W. Duncan et al.   ACS Medicinal Chemistry Letters

Prmt5 is required for germ cell survival during spermatogenesis in mice

(2015) Yanbo Wang et al.   Scientific Reports

Preparation and Reactions of Heteroarylmethylzinc Reagents

(2014) Nadja M. Barl et al.   ORGANIC LETTERS

Structure of the Arginine Methyltransferase PRMT5-MEP50 Reveals a Mechanism for Substrate Specificity

(2013) Meng-Chiao Ho et al.   PLoS One

Fragment-based lead discovery grows up

(2012) Monya Baker   NATURE REVIEWS DRUG DISCOVERY

Crystal structure of the human PRMT5:MEP50 complex

(2012) S. Antonysamy et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Revealing Atropisomer Axial Chirality in Drug Discovery

(2011) Steven R. LaPlante et al.   ChemMedChem

Fragment screening to predict druggability (ligandability) and lead discovery success

(2011) Fredrik N.B. Edfeldt et al.   DRUG DISCOVERY TODAY

Biosensor-based small molecule fragment screening with biolayer interferometry

(2011) Charles A. Wartchow et al.   JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN

Assessing Atropisomer Axial Chirality in Drug Discovery and Development

(2011) Steven R. LaPlante et al.   JOURNAL OF MEDICINAL CHEMISTRY

Protein Arginine Methyltransferase 5 Regulates ERK1/2 Signal Transduction Amplitude and Cell Fate Through CRAF

(2011) P. Andreu-Perez et al.   Science Signaling

Versatility of PRMT5-induced methylation in growth control and development

(2011) Vrajesh Karkhanis et al.   TRENDS IN BIOCHEMICAL SCIENCES

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

Using the Golden Triangle to optimize clearance and oral absorption

(2009) Ted W. Johnson et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Defining optimum lipophilicity and molecular weight ranges for drug candidates—Molecular weight dependent lower logD limits based on permeability

(2009) Michael J. Waring   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Protein Arginine Methylation in Mammals: Who, What, and Why

(2009) Mark T. Bedford et al.   MOLECULAR CELL

Physiochemical drug properties associated with in vivo toxicological outcomes

(2008) Jason D. Hughes et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS