BCL2 G quadruplex-binding small molecules: Current status and prospects for the development of next-generation anticancer therapeutics |
| |
Institution: | 1. Amity Institute of Molecular Medicine and Stem Cell Research, Amity University, Noida, UP, 201303, India;2. IOM-CNR National Research Council, Via Pascoli, Perugia I-06123, Italy;3. Department of Physics and Geology, University of Perugia, via Pascoli, 06123, Italy;4. Drug Discovery Unit, Jubilant Biosys Ltd, Sector 58, Noida, UP 201301, India |
| |
Abstract: | B cell lymphoma 2 (BCL2) overexpression in a range of human tumors is often related to chemotherapy resistance and poor prognosis. GC-rich regions upstream of the P1 promoter in human BCL2 can form G-quadruplex (G4) structures through the stacking of four Hoogsteen-paired guanine bases. Stabilizing the G4 fold implies the inhibition of BCL2 expression and, thus, small molecules that selectively bind to the G4 are promising anticancer candidates. In this review, we discuss the structural aspects, binding affinity, selectivity, and biological activity of well-characterized BCL2 G4 binding ligands in vitro and in vivo. We also explore future directions in the research and development of G4-based anticancer therapeutics. |
| |
Keywords: | BLC2 G quadruplex Drug discovery Small molecules Anticancer therapeutics Targeted cancer therapy |
本文献已被 ScienceDirect 等数据库收录! |
|