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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… Expand
National Institutes of Health

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Related topics

1 relation
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.
Medulloblastoma is the most prevalent central nervous system tumor in children. Targeted treatment approaches for patients with… Expand
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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…
 
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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… Expand
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2017
2017
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… Expand
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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… Expand
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Highly Cited
2016
Highly Cited
2016
OTX015 (MK-8628), a novel BET inhibitor, displays in vitro and in vivo antitumor effects alone and in combination with conventional therapies in glioblastoma models.
Bromodomain and extraterminal (BET) bromodomain (BRD) proteins are epigenetic readers that bind to acetylated lysine residues on… Expand
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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… Expand
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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… Expand
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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… Expand
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2015
2015
Phase I Population Pharmacokinetic Assessment of the Oral Bromodomain Inhibitor OTX015 in Patients with Haematologic Malignancies
Background and ObjectivesOTX015 (MK-8628) is a novel inhibitor of the bromodomain and extraterminal (BET)-bromodomain (BRD… Expand
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