Pharmacological inhibition of KDM5A for cancer treatment

Lysine-specific demethylase 5A (KDM5A, also named RBP2 or JARID1A) is a demethylase that can remove methyl groups from histones H3K4me1/2/3. It is aberrantly expressed in many cancers, where it impedes differentiation and contributes to cancer cell proliferation, cell metastasis and invasiveness, drug resistance, and is associated with poor prognosis. Pharmacological inhibition of KDM5A has been reported to significantly attenuate tumor progression in vitro and in vivo in a range of solid tumors and acute myeloid leukemia. This review will present the structural aspects of KDM5A, its role in carcinogenesis, a comparison of currently available approaches for screening KDM5A inhibitors, a classification of KDM5A inhibitors, and its potential as a drug target in cancer therapy. (C) 2021 Elsevier Masson SAS. All rights reserved.

Automated summary

KDM5A, a demethylase that is aberrantly expressed in many cancers, plays a role in promoting cancer cell proliferation, metastasis, invasiveness, drug resistance, and poor prognosis. Pharmacological inhibition of KDM5A has been shown to significantly attenuate tumor progression and may serve as a potential drug target in cancer therapy.