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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…
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National Institutes of Health
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1 relation
OTX015
Papers overview
Semantic Scholar uses AI to extract papers important to this topic.
2019
2019
BET Bromodomain Inhibition Suppresses Human T Cell Function
Peter Georgiev
,
Yun Wang
,
+5 authors
S. Shumway
ImmunoHorizons
2019
Corpus ID: 198983948
Bromodomain and extraterminal domain (BET) proteins help direct the differentiation of helper T cell subsets, but their role in…
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2019
2019
Synergistic activity of BET inhibitor MK-8628 and PLK inhibitor Volasertib in preclinical models of medulloblastoma.
Youjia Han
,
S. Lindner
,
+11 authors
Anton G. Henssen
Cancer Letters
2019
Corpus ID: 58573942
2018
2018
Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor.
Anand Divakaran
,
S. Talluri
,
+10 authors
W. Pomerantz
Journal of Medicinal Chemistry
2018
Corpus ID: 52824898
As regulators of transcription, epigenetic proteins that interpret post-translational modifications to N-terminal histone tails…
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2017
2017
Benzoisoquinolinediones as Potent and Selective Inhibitors of BRPF2 and TAF1/TAF1L Bromodomains
Léa Bouché
,
Clara D. Christ
,
+18 authors
B. Haendler
Journal of Medicinal Chemistry
2017
Corpus ID: 28443890
Bromodomains (BD) are readers of lysine acetylation marks present in numerous proteins associated with chromatin. Here we…
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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
R. Vazquez
,
M. Riveiro
,
+12 authors
M. D’Incalci
OncoTarget
2016
Corpus ID: 3674573
Triple-negative breast cancer (TNBC) is an aggressive and heterogeneous subgroup of breast tumors clinically defined by the lack…
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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
Caroline Berenguer‐Daizé
,
Lucile Astorgues-Xerri
,
+9 authors
L. Ouafik
International Journal of Cancer
2016
Corpus ID: 426576
Bromodomain and extraterminal (BET) bromodomain (BRD) proteins are epigenetic readers that bind to acetylated lysine residues on…
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Highly Cited
2016
Highly Cited
2016
Phase I Population Pharmacokinetic Assessment of the Oral Bromodomain Inhibitor OTX015 in Patients with Haematologic Malignancies
Elodie Odore
,
F. Lokiec
,
+11 authors
K. Rezaï
Clinical Pharmacokinetics
2016
Corpus ID: 207485266
Background and ObjectivesOTX015 (MK-8628) is a novel inhibitor of the bromodomain and extraterminal (BET)-bromodomain (BRD…
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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).
A. Hottinger
,
M. Sanson
,
+9 authors
O. Chinot
2016
Corpus ID: 80155634
e14123Background: Bromodomains (BRD) bind to acetylated lysine residues on histone tails and are directly involved in remodeling…
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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
M. Riveiro
,
Lucile Astorgues-Xerri
,
+12 authors
F. Bertoni
OncoTarget
2016
Corpus ID: 3642051
Inhibitors targeting epigenetic control points of oncogenes offer a potential mean of blocking tumor progression in small cell…
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2016
2016
Bromodomain inhibitor OTX015 (MK-8628) combined with targeted agents shows strong in vivo antitumor activity in lymphoma
E. Gaudio
,
C. Tarantelli
,
+10 authors
F. Bertoni
OncoTarget
2016
Corpus ID: 3502337
The bromodomain inhibitor OTX015 (MK-8628) has shown anti-lymphoma activity as a single agent in both the preclinical and…
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