Unlocking the potential of chemical probes for methyl-lysine reader proteins

Identification of a Fragment-like Small Molecule Ligand for the Methyl-lysine Binding Protein, 53BP1

(2015) Michael T. Perfetti et al.   ACS Chemical Biology

The promise and peril of chemical probes

(2015) Cheryl H Arrowsmith et al.   Nature Chemical Biology

The cellular thermal shift assay for evaluating drug target interactions in cells

(2014) Rozbeh Jafari et al.   Nature Protocols

Selective Inhibition of Tumor Oncogenes by Disruption of Super-Enhancers

(2013) Jakob Lovén et al.   CELL

Small-Molecule Ligands of Methyl-Lysine Binding Proteins: Optimization of Selectivity for L3MBTL3

(2013) Lindsey I. James et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain

(2013) Lindsey I James et al.   Nature Chemical Biology

Target validation using chemical probes

(2013) Mark E Bunnage et al.   Nature Chemical Biology

Epigenetics: Core misconcept

(2013) M. Ptashne   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Epigenetic protein families: a new frontier for drug discovery

(2012) Cheryl H. Arrowsmith et al.   NATURE REVIEWS DRUG DISCOVERY

BET Bromodomain Inhibition as a Therapeutic Strategy to Target c-Myc

(2011) Jake E. Delmore et al.   CELL

Small-Molecule Ligands of Methyl-Lysine Binding Proteins

(2011) J. Martin Herold et al.   JOURNAL OF MEDICINAL CHEMISTRY

Biophysical Probes Reveal a “Compromise” Nature of the Methyl-lysine Binding Pocket in L3MBTL1

(2011) Cen Gao et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Targeting MYC dependence in cancer by inhibiting BET bromodomains

(2011) J. A. Mertz et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Probing the Probes: Fitness Factors For Small Molecule Tools

(2010) Paul Workman et al.   CHEMISTRY & BIOLOGY

Targeting epigenetic enzymes for drug discovery

(2010) Robert A Copeland et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Suppression of inflammation by a synthetic histone mimic

(2010) Edwige Nicodeme et al.   NATURE

Selective inhibition of BET bromodomains

(2010) Panagis Filippakopoulos et al.   NATURE

The art of the chemical probe

(2010) Stephen V Frye   Nature Chemical Biology