Cargando…

BET inhibitor OTX015 targets BRD2 and BRD4 and decreases c-MYC in acute leukemia cells

The bromodomain (BRD) and extraterminal (BET) proteins including BRD2, BRD3 and BRD4 have been identified as key targets for leukemia maintenance. A novel oral inhibitor of BRD2/3/4, the thienotriazolodiazepine compound OTX015, suitable for human use, is available. Here we report its biological effe...

Descripción completa

Detalles Bibliográficos
Autores principales:	Coudé, Marie-Magdelaine, Braun, Thorsten, Berrou, Jeannig, Dupont, Mélanie, Bertrand, Sibyl, Masse, Aline, Raffoux, Emmanuel, Itzykson, Raphaël, Delord, Marc, Riveiro, Maria E., Herait, Patrice, Baruchel, André, Dombret, Hervé, Gardin, Claude
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	Impact Journals LLC 2015
Materias:	Research Paper
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4627339/ https://www.ncbi.nlm.nih.gov/pubmed/25989842

Ejemplares similares

Biological Effects of BET Inhibition by OTX015 (MK-8628) and JQ1 in NPM1-Mutated (NPM1c) Acute Myeloid Leukemia (AML)
por: Djamai, Hanane, et al.
Publicado: (2021)

BRD3 and BRD4 BET Bromodomain Proteins Differentially Regulate Skeletal Myogenesis
por: Roberts, Thomas C., et al.
Publicado: (2017)

BET Bromodomain Proteins Brd2, Brd3 and Brd4 Selectively Regulate Metabolic Pathways in the Pancreatic β-Cell
por: Deeney, Jude T., et al.
Publicado: (2016)

Dissecting the Role of BET Bromodomain Proteins BRD2 and BRD4 in Human NK Cell Function
por: Cribbs, Adam P., et al.
Publicado: (2021)

The BET inhibitor OTX015 reactivates latent HIV-1 through P-TEFb
por: Lu, Panpan, et al.
Publicado: (2016)

BRD9 regulates interferon-stimulated genes during macrophage activation via cooperation with BET protein BRD4
por: Ahmed, Nasiha S., et al.
Publicado: (2021)

BRD4: A BET(ter) target for the treatment of AML?
por: Valent, Peter, et al.
Publicado: (2014)

MYC protein stability is negatively regulated by BRD4
por: Devaiah, Ballachanda N., et al.
Publicado: (2020)

The BET Inhibitor OTX015 Exhibits In Vitro and In Vivo Antitumor Activity in Pediatric Ependymoma Stem Cell Models
por: Servidei, Tiziana, et al.
Publicado: (2021)

Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4
por: Zengerle, Michael, et al.
Publicado: (2015)

Zebrafish brd2a and brd2b are paralogous members of the bromodomain-ET (BET) family of transcriptional coregulators that show structural and expression divergence
por: DiBenedetto, Angela J, et al.
Publicado: (2008)

BET protein Brd4 activates transcription in neurons and BET inhibitor Jq1 blocks memory in mice
por: Korb, Erica, et al.
Publicado: (2015)

Preparation data of the bromodomains BRD3(1), BRD3(2), BRD4(1), and BRPF1B and crystallization of BRD4(1)-inhibitor complexes
por: Hügle, Martin, et al.
Publicado: (2016)

Transcriptional regulation of BRD7 expression by Sp1 and c-Myc
por: Liu, Huaying, et al.
Publicado: (2008)

The BET/BRD inhibitor JQ1 improves brain plasticity in WT and APP mice
por: Benito, E, et al.
Publicado: (2017)

Resistance to BET inhibitors in lung adenocarcinoma is mediated by casein kinase phosphorylation of BRD4
por: Calder, Jack, et al.
Publicado: (2021)

Phosphorylation-dependent BRD4 dimerization and implications for therapeutic inhibition of BET family proteins
por: Malvezzi, Francesca, et al.
Publicado: (2021)

Bromodomain-containing subunits BRD1, BRD2, and BRD13 are required for proper functioning of SWI/SNF complexes in Arabidopsis
por: Jarończyk, Kamila, et al.
Publicado: (2021)

Preclinical Evaluation of a Novel Small Molecule Inhibitor of LIM Kinases (LIMK) CEL_Amide in Philadelphia-Chromosome Positive (BCR::ABL+) Acute Lymphoblastic Leukemia (ALL)
por: Berrou, Jeannig, et al.
Publicado: (2022)

Inducible In Vivo Silencing of Brd4 Identifies Potential Toxicities of Sustained BET Protein Inhibition
por: Bolden, Jessica E., et al.
Publicado: (2014)

The BET Family Member BRD4 Interacts with OCT4 and Regulates Pluripotency Gene Expression
por: Wu, Tao, et al.
Publicado: (2015)

The BET bromodomain inhibitor, JQ1, facilitates c-FLIP degradation and enhances TRAIL-induced apoptosis independent of BRD4 and c-Myc inhibition
por: Yao, Weilong, et al.
Publicado: (2015)

OTX015 (MK-8628), a novel BET inhibitor, exhibits antitumor activity in non-small cell and small cell lung cancer models harboring different oncogenic mutations
por: Riveiro, Maria E., et al.
Publicado: (2016)

The MDM2 inhibitor CGM097 combined with the BET inhibitor OTX015 induces cell death and inhibits tumor growth in models of neuroblastoma
por: Maser, Tyler, et al.
Publicado: (2020)

CLRM-04. PHASE I/II SAFETY AND EFFICACY STUDY OF BET BROMODOMAIN INHIBITOR OTX-015 WITH OLAPARIB AND LOMUSTINE IN PATIENTS WITH RECURRENT GLIOBLASTOMA
por: Lam, Fred
Publicado: (2021)

BET bromodomain-mediated interaction between ERG and BRD4 promotes prostate cancer cell invasion
por: Blee, Alexandra M., et al.
Publicado: (2016)

BET Family Protein BRD4: An Emerging Actor in NFκB Signaling in Inflammation and Cancer
por: Hajmirza, Azadeh, et al.
Publicado: (2018)

Prostate cancer-associated SPOP mutations confer resistance to BET inhibitors through stabilization of BRD4
por: Dai, Xiangpeng, et al.
Publicado: (2017)

Stromal induction of BRD4 phosphorylation Results in Chromatin Remodeling and BET inhibitor Resistance in Colorectal Cancer
por: Wang, Wenyu, et al.
Publicado: (2021)

Retinoblastoma protein as an intrinsic BRD4 inhibitor modulates small molecule BET inhibitor sensitivity in cancer
por: Ding, Donglin, et al.
Publicado: (2022)

tBRD-1 and tBRD-2 regulate expression of genes necessary for spermatid differentiation
por: Theofel, Ina, et al.
Publicado: (2017)

Increased expression of BRD4 isoforms long (BRD4-L) and short (BRD4-S) promotes chemotherapy resistance in high-grade serous ovarian carcinoma
por: Drumond-Bock, Ana Luiza, et al.
Publicado: (2023)

Bromodomain inhibitor OTX015 (MK-8628) combined with targeted agents shows strong in vivo antitumor activity in lymphoma
por: Gaudio, Eugenio, et al.
Publicado: (2016)

A Novel BRD Family PROTAC Inhibitor dBET1 Exerts Great Anti-Cancer Effects by Targeting c-MYC in Acute Myeloid Leukemia Cells
por: Zhang, Kunlong, et al.
Publicado: (2022)

I-BET151 suppresses osteoclast formation and inflammatory cytokines secretion by targetting BRD4 in multiple myeloma
por: Guo, Ning-Hong, et al.
Publicado: (2019)

Targeting BRD/BET proteins inhibits adaptive kinome upregulation and enhances the effects of BRAF/MEK inhibitors in melanoma
por: Tiago, Manoela, et al.
Publicado: (2020)

The BRD4 Inhibitor dBET57 Exerts Anticancer Effects by Targeting Superenhancer-Related Genes in Neuroblastoma
por: Jia, Si-Qi, et al.
Publicado: (2022)

Comprehensive analysis of the prognosis and immune infiltrates for the BET protein family reveals the significance of BRD4 in glioblastoma multiforme
por: Ye, Yintao, et al.
Publicado: (2023)

Targeting BRD9 by I-BRD9 efficiently inhibits growth of acute myeloid leukemia cells
por: Zhou, Lixin, et al.
Publicado: (2021)

Methylation of BRD4 by PRMT1 regulates BRD4 phosphorylation and promotes ovarian cancer invasion
por: Liu, Yi, et al.
Publicado: (2023)

Cannot write session to /tmp/vufind_sessions/sess_pe8nv8kd8g56ott7ku2cu5jnvj