Discover Community Create You

Loading publication...

Noodle always counts identifier-free feature events for service operation. With your permission, Google Analytics can also estimate audience and engagement. Search text, publication identifiers, cookies, IP addresses and browser fingerprints are never included in Noodle's first-party event counters.

Privacy details

Article

GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1

5 Aug 2022

Abstract excerpt

Bromodomains are acetyllysine recognition domains present in a variety of human proteins. Bromodomains also bind small molecules that compete with acetyllysine, and therefore bromodomains have been targets for drug discovery efforts. Highly potent and selective ligands with good cellular permeability have been proposed as chemical probes for use in exploring the functions of many of the bromodomain proteins. We...

Read the complete abstract on PubMed

Topics

Share this publication in a Topic to start or enrich a Post.

Share to Chromatin Remodeling and Cancer
Share to Peptidase Inhibition and Analysis
Share to Protein Degradation and Inhibitors

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Source

Identifiers

PMID: 35930799
DOI: 10.1021/acs.jmedchem.2c00662

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 5 Sept 2026.

Related research

Semantic proximity does not establish scientific evidence.

Research trail→

Click a neighbor to travelStep 1 · 12 closest

GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1PMID 35930799Read ↗

Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain InhibitorsSemantic proximity Read ↗

Inhibition of bromodomain and extra-terminal proteins (BET) as a potential therapeutic approach in haematological malignancies: emerging preclinical and clinical evidenceSemantic proximity Read ↗

Rational Design and Development of Selective BRD7 Bromodomain Inhibitors and Their Activity in Prostate CancerSemantic proximity Read ↗

Targeting bromodomain-containing proteins: research advances of drug discoverySemantic proximity Read ↗

Chemical Epigenetics: The Impact of Chemical and Chemical Biology Techniques on Bromodomain Target ValidationSemantic proximity Read ↗

Design of a Biased Potent Small Molecule Inhibitor of the Bromodomain and PHD Finger-Containing (BRPF) Proteins Suitable for Cellular and in Vivo StudiesSemantic proximity Read ↗

Design and Synthesis of a Highly Selective and In Vivo-Capable Inhibitor of the Second Bromodomain of the Bromodomain and Extra Terminal Domain Family of ProteinsSemantic proximity Read ↗

Bromodomains as therapeutic targets in cancerSemantic proximity Read ↗

Clinical progress and pharmacology of small molecule bromodomain inhibitorsSemantic proximity Read ↗

A selective and orally bioavailable VHL-recruiting PROTAC achieves SMARCA2 degradation in vivoSemantic proximity Read ↗

Histone Recognition and Large-Scale Structural Analysis of the Human Bromodomain FamilySemantic proximity Read ↗

Pharmacological Targeting of BET Bromodomain Proteins in Acute Myeloid Leukemia and Malignant Lymphomas: From Molecular Characterization to Clinical ApplicationsSemantic proximity Read ↗

⌁Select a neighboring publication to make it the new centre.