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Targeting the anti-apoptotic Bcl-2 family proteins: machine learning virtual screening and biological evaluation of new small molecules

Elisabetta Valentini, Simona D’Aguanno, Marta Di Martile, Camilla Montesano, Virginia Ferraresi, Alexandros Patsilinakos, Manuela Sabatino, Lorenzo Antonini, Martina Chiacchiarini, Sérgio Valente, Antonello Mai, Gianni Colotti, Rino Ragno, Daniela Trisciuoglio, Donatella Del Bufalo

2022Theranostics50 citationsDOIOpen Access PDF

Abstract

Bcl-2 family anti-apoptotic proteins are overexpressed in several hematological and solid tumors, and contribute to tumor formation, progression, and resistance to therapy. They represent a promising therapeutic avenue to explore for cancer treatment. Venetoclax, a Bcl-2 inhibitor is currently used for hematological malignancies or is undergoing clinical trials for either hematological or solid tumors. Despite these progresses, ongoing efforts are focusing on the identification and development of new molecules targeting Bcl-2 protein and/or other family members.

Topics & Concepts

ApoptosisCancer researchVenetoclaxBcl-2 familyClonogenic assayIn vivoAutophagyVirtual screeningBiologyProgrammed cell deathChemistryImmunologyBioinformaticsBiochemistryDrug discoveryLeukemiaGeneticsChronic lymphocytic leukemiaCell death mechanisms and regulationAutophagy in Disease and TherapyRNA Interference and Gene Delivery
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