Regulation of MALAT1 triple helix stability and in vitro degradation by diphenylfurans.

ABSTRACT: Small molecule-based modulation of a triple helix in the long non-coding RNA metastasis-associated lung adenocarcinoma transcript 1 (MALAT1) has been proposed as an attractive avenue for cancer treatment and a model system for understanding small molecule:RNA recognition. To elucidate fundamental recognition principles and structure-function relationships, we designed and synthesized nine novel analogs of a diphenylfuran-based small molecule DPFp8, a previously identified lead binder of MALAT1. We investigated the role of recognition modalities in binding and in silico studies along with the relationship between affinity, stability and in vitro enzymatic degradation of the triple helix. Specifically, molecular docking studies identified patterns driving affinity and selectivity, including

SUBMITTER: Donlic A 

PROVIDER: S-EPMC7430642 | biostudies-literature | 2020 Aug

REPOSITORIES: biostudies-literature