Identification and Development of BRD9 Chemical Probes

被引：5

作者：

Colarusso, Ester ^{[1
]}

Chini, Maria Giovanna ^{[2
]}

Bifulco, Giuseppe ^{[1
]}

Lauro, Gianluigi ^{[1
]}

Giordano, Assunta ^{[3
]}

机构：

[1] Univ Salerno, Dept Pharm, Via Giovanni Paolo II 132, I-84084 Fisciano, Salerno, Italy

[2] Univ Molise, Dept Biosci & Terr, Contrada Fonte Lappone, I-86090 Pesche, Isernia, Italy

[3] Consiglio Nazl Ric CNR, Inst Biomol Chem ICB, Via Campi Flegrei 34, I-80078 Pozzuoli, Napoli, Italy

来源：

PHARMACEUTICALS | 2024年 / 17卷 / 03期

关键词：

BRD9; inhibitors; small molecules; PROTACs; leukemia; drug discovery; PROTEIN-DEGRADATION; BROMODOMAIN; INHIBITORS; DISCOVERY; DESIGN; RECOGNITION; COMPLEX; H3K14;

D O I：

10.3390/ph17030392

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The development of BRD9 inhibitors involves the design and synthesis of molecules that can specifically bind the BRD9 protein, interfering with the function of the chromatin-remodeling complex ncBAF, with the main advantage of modulating gene expression and controlling cellular processes. Here, we summarize the work conducted over the past 10 years to find new BRD9 binders, with an emphasis on their structure-activity relationships, efficacies, and selectivities in preliminary studies. BRD9 is expressed in a variety of cancer forms, hence, its inhibition holds particular significance in cancer research. However, it is crucial to note that the expanding research in the field, particularly in the development of new degraders, may uncover new therapeutic potentials.

引用

页数：31

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