pelabresib and Leukemia--Myeloid--Acute

pelabresib has been researched along with Leukemia--Myeloid--Acute* in 1 studies

Other Studies

1 other study(ies) available for pelabresib and Leukemia--Myeloid--Acute

Article	Year
Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials. Journal of medicinal chemistry, 2016, Feb-25, Volume: 59, Issue:4 In recent years, inhibition of the interaction between the bromodomain and extra-terminal domain (BET) family of chromatin adaptors and acetyl-lysine residues on chromatin has emerged as a promising approach to regulate the expression of important disease-relevant genes, including MYC, BCL-2, and NF-κB. Here we describe the identification and characterization of a potent and selective benzoisoxazoloazepine BET bromodomain inhibitor that attenuates BET-dependent gene expression in vivo, demonstrates antitumor efficacy in an MV-4-11 mouse xenograft model, and is currently undergoing human clinical trials for hematological malignancies (CPI-0610). Topics: Animals; Antineoplastic Agents; Azepines; Cell Cycle Proteins; Cell Line, Tumor; Clinical Trials as Topic; Dogs; Gene Expression Regulation, Neoplastic; Genes, myc; Humans; Leukemia, Myeloid, Acute; Mice; Nuclear Proteins; Proto-Oncogene Proteins c-myc; Rats; Transcription Factors; Xenograft Model Antitumor Assays	2016

Article

Year

Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials.

Journal of medicinal chemistry, 2016, Feb-25, Volume: 59, Issue:4

In recent years, inhibition of the interaction between the bromodomain and extra-terminal domain (BET) family of chromatin adaptors and acetyl-lysine residues on chromatin has emerged as a promising approach to regulate the expression of important disease-relevant genes, including MYC, BCL-2, and NF-κB. Here we describe the identification and characterization of a potent and selective benzoisoxazoloazepine BET bromodomain inhibitor that attenuates BET-dependent gene expression in vivo, demonstrates antitumor efficacy in an MV-4-11 mouse xenograft model, and is currently undergoing human clinical trials for hematological malignancies (CPI-0610).

Topics: Animals; Antineoplastic Agents; Azepines; Cell Cycle Proteins; Cell Line, Tumor; Clinical Trials as Topic; Dogs; Gene Expression Regulation, Neoplastic; Genes, myc; Humans; Leukemia, Myeloid, Acute; Mice; Nuclear Proteins; Proto-Oncogene Proteins c-myc; Rats; Transcription Factors; Xenograft Model Antitumor Assays

2016