Identification of small molecule inhibitors of the Lin28-mediated blockage of pre-let-7g processing.

ABSTRACT: The protein Lin28 and microRNA let-7 play critical roles in mammalian development and human disease. Lin28 inhibits let-7 biogenesis through direct interaction with let-7 precursors (pre-let-7). Accumulating evidence in vitro and in vivo suggests this interaction plays a dominant role in embryonic stem cell self-renewal and tumorigenesis. Thus the Lin28-let-7 interaction might be an attractive drug target, if not for the well-known difficulties in targeting protein-RNA interactions with drugs. The identification and development of suitable probe molecules to further elucidate therapeutic potential, as well as mechanistic details of this pathway will be valuable. We report the development and application of a biophysical high-throughput screening assay for the identification of small molecu

SUBMITTER: Lightfoot HL 

PROVIDER: S-EPMC5433426 | biostudies-literature | 2016 Nov

REPOSITORIES: biostudies-literature