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BET Bromodomains 2/3/4 Inhibitor MK-8628

Known as: MK-8628 
A synthetic, small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family of bromodomain-containing proteins 2, 3 and 4 with potential… 
National Institutes of Health

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Related topics

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OTX015

Papers overview

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2019
2019
Synergistic activity of BET inhibitor MK-8628 and PLK inhibitor Volasertib in preclinical models of medulloblastoma.
2019
2019
BET Bromodomain Inhibition Suppresses Human T Cell Function
Bromodomain and extraterminal domain (BET) proteins help direct the differentiation of helper T cell subsets, but their role in… 
2019
2019
An Open-Label Phase I/IIa Study to Evaluate the Safety and Efficacy of CCS1477, a First in Clinic Inhibitor of the p300/CPB Bromodomains, As Monotherapy in Patients with Advanced Haematological…
Background CCS1477 is a first in class potent, selective and orally bioavailable inhibitor of the bromodomains of p300 and CBP… 
2018
2018
Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor.
As regulators of transcription, epigenetic proteins that interpret post-translational modifications to N-terminal histone tails… 
2017
2017
Benzoisoquinolinediones as Potent and Selective Inhibitors of BRPF2 and TAF1/TAF1L Bromodomains
Bromodomains (BD) are readers of lysine acetylation marks present in numerous proteins associated with chromatin. Here we… 
Highly Cited
2016
Highly Cited
2016
The bromodomain inhibitor OTX015 (MK-8628) exerts anti-tumor activity in triple-negative breast cancer models as single agent and in combination with everolimus
Triple-negative breast cancer (TNBC) is an aggressive and heterogeneous subgroup of breast tumors clinically defined by the lack… 
2016
2016
OTX015 (MK-8628), a novel BET inhibitor, exhibits antitumor activity in non-small cell and small cell lung cancer models harboring different oncogenic mutations
Inhibitors targeting epigenetic control points of oncogenes offer a potential mean of blocking tumor progression in small cell… 
2016
2016
Bromodomain inhibitor OTX015 (MK-8628) combined with targeted agents shows strong in vivo antitumor activity in lymphoma
The bromodomain inhibitor OTX015 (MK-8628) has shown anti-lymphoma activity as a single agent in both the preclinical and… 
2016
2016
Dose optimization of MK-8628 (OTX015), a small molecule inhibitor of bromodomain and extra-terminal (BET) proteins, in patients (pts) with recurrent glioblastoma (GB).
e14123Background: Bromodomains (BRD) bind to acetylated lysine residues on histone tails and are directly involved in remodeling… 
2016
2016
P08.63 Dose optimization of MK-8628 (OTX015), a small molecule inhibitor of bromodomain and extra-terminal (BET) proteins, in patients with recurrent glioblastoma
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