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GSK525762A

Known as: IBET compound, GSK 525762A, I-BET762 
A small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family of bromodomain-containing proteins with potential antineoplastic… 
National Institutes of Health

Related topics

Related topics

2 relations

Broader (1)

Benzodiazepines
NCIt Antineoplastic Agent Terminology

Papers overview

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2018
2018
Structure-based optimization of a series of selective BET inhibitors containing aniline or indoline groups.
2018
2018
A phase Ib open-label, dose escalation and expansion study to investigate the safety, pharmacokinetics, pharmacodynamics and clinical activity of GSK525762 in combination with abiraterone or…
TPS391Background: Metastatic castrate-resistant prostate cancer (mCRPC) remains an incurable illness as resistance develops after… 
2018
2018
Abstract OT3-06-07: A phase I/II dose escalation and expansion study to investigate the safety, pharmacokinetics, pharmacodynamics and clinical activity of GSK525762 in combination with fulvestrant…
Background: Advanced or metastatic ER+BC (estrogen receptor positive breast cancer) is an incurable illness that will prove fatal… 
2017
2017
A phase I/II dose escalation and expansion study to investigate the safety, pharmacokinetics, pharmacodynamics and clinical activity of GSK525762 in combination with fulvestrant in subjects with ER…
TPS1114Background: Advanced or metastatic ER+BC (estrogen receptor positive breast cancer) is an incurable illness that will… 
2017
2017
Abstract CT104: A first-in-human phase I dose escalation study of BET inhibitor GSK2820151 in patients with advanced or recurrent solid tumors cancers
Background The Bromodomain (BRD) Extra Terminal (BET) family of proteins (BRD2, 3, 4 and T) contain bromodomains that recognize… 
2016
2016
Abstract CT014: GSK525762, a selective bromodomain (BRD) and extra terminal protein (BET) inhibitor: results from part 1 of a phase I/II open-label single-agent study in patients with NUT midline…
Background: GSK525762 is a potent, selective pan-BET inhibitor that abrogates binding of BET family proteins (BRD2, BRD3, BRD4… 
2016
2016
A Phase I/II Open-Label, Dose Escalation Study to Investigate the Safety, Pharmacokinetics, Pharmacodynamics and Clinical Activity of GSK525762 in Subjects with Relapsed, Refractory Hematologic…
Background: Bromodomains (BRDs) are domains found in a variety of proteins that recognize and bind to acetylated lysine residues… 
2016
2016
Structure-Activity Relationship Study of N(6)-Benzoyladenine-Type BRD4 Inhibitors and Their Effects on Cell Differentiation and TNF-α Production.
Bromodomains are epigenetic 'readers' of histone acetylation. The first potent bromodomain and extra-terminal domain (BET… 
Review
2016
Review
2016
Abstract 4693: Mechanism-based combination strategies for BET inhibitors in NUT midline carcinoma
NUT midline carcinoma (NMC) is a highly aggressive squamous cell cancer that responds poorly to standard chemotherapuetic… 
2014
2014
BETting on a new prostate cancer treatment
The bromodomain and extraterminal domain (BET)-containing proteins are a class of epigenetic regulators known as “chromatin… 
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