Targeting the cis-dimerization of LINGO-1 with low MW compounds affects its downstream signalling.

ABSTRACT:

Background and purpose

The transmembrane protein LINGO-1 is a negative regulator in the nervous system mainly affecting axonal regeneration, neuronal survival, oligodendrocyte differentiation and myelination. However, the molecular mechanisms regulating its functions are poorly understood. In the present study, we investigated the formation and the role of LINGO-1 cis-dimers in the regulation of its biological activity.

Experimental approach

LINGO-1 homodimers were identified in both HEK293 and SH-SY5Y cells using co-immunoprecipitation experiments and BRET saturation analysis. We performed a hypothesis-driven screen for identification of small-molecule protein-protein interaction modulators of LINGO-1 using a BRET-based assay, adapted for screening. The compound identified

SUBMITTER: Cobret L 

PROVIDER: S-EPMC4301693 | biostudies-literature | 2015 Feb

REPOSITORIES: biostudies-literature