MeCP2 small molecule inhibitor

MeCP2 (methyl-CpG-binding protein 2) small molecule inhibitors represent a class of preclinical therapeutic agents designed to target and inhibit MeCP2, a chromatin-associated protein that binds to methylated CpG dinucleotides to regulate gene transcription and chromatin architecture. While MeCP2 mutations are primarily associated with Rett syndrome, MeCP2 overexpression has been identified as an oncogenic driver and a mediator of therapeutic resistance in several cancers, including lung cancer and triple-negative breast cancer. By inhibiting MeCP2, these small molecules aim to disrupt its interaction with chromatin, thereby restoring the expression of tumor suppressor genes, enhancing DNA damage repair sensitivity, and activating the cGAS-STING pathway to promote antitumor immunity. Consequently, MeCP2 small molecule inhibitors are being investigated as potential anticancer therapies and radiosensitizers.

Other names

MECP2 inhibitorMECP-2 inhibitorMECP 2 inhibitorMECP2 small molecule inhibitorMECP-2 small molecule inhibitorMECP 2 small molecule inhibitormethyl-CpG-binding protein 2 inhibitor