Colarusso Ester, Chini Maria Giovanna, Bifulco Giuseppe, Lauro Gianluigi, Giordano Assunta
Department of Pharmacy, University of Salerno, Via Giovanni Paolo II 132, 84084 Fisciano, Salerno, Italy.
Department of Biosciences and Territory, University of Molise, Contrada Fonte Lappone, 86090 Pesche, Isernia, Italy.
Pharmaceuticals (Basel). 2024 Mar 19;17(3):392. doi: 10.3390/ph17030392.
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.
BRD9抑制剂的研发涉及能够特异性结合BRD9蛋白的分子的设计与合成，这些分子会干扰染色质重塑复合物ncBAF的功能，其主要优势在于调节基因表达和控制细胞进程。在此，我们总结了过去10年为寻找新型BRD9结合剂所开展的工作，重点关注它们在初步研究中的构效关系、效力和选择性。BRD9在多种癌症类型中均有表达，因此，对其进行抑制在癌症研究中具有特殊意义。然而，必须注意的是，该领域不断扩展的研究，尤其是新型降解剂的研发，可能会揭示新的治疗潜力。
