Design and Synthesis of Hsp90 Inhibitors with B-Raf and PDHK1 Multi-Target Activity.

ABSTRACT: The design of multi-target ligands has become an innovative approach for the identification of effective therapeutic treatments against complex diseases, such as cancer. Recent studies have demonstrated that the combined inhibition of Hsp90 and B-Raf provides synergistic effects against several types of cancers. Moreover, it has been reported that PDHK1, which presents an ATP-binding pocket similar to that of Hsp90, plays an important role in tumor initiation, maintenance and progression, participating also to the senescence process induced by B-Raf oncogenic proteins. Based on these premises, the simultaneous inhibition of these targets may provide several benefits for the treatment of cancer. In this work, we set up a design strategy including the assembly and integration of molecular fr

SUBMITTER: Pinzi L 

PROVIDER: S-EPMC8634768 | biostudies-literature | 2021 Dec

REPOSITORIES: biostudies-literature