A protein tertiary structure mimetic modulator of the Hippo signalling pathway.

ABSTRACT: Transcription factors are key protein effectors in the regulation of gene transcription, and in many cases their activity is regulated via a complex network of protein-protein interactions (PPI). The chemical modulation of transcription factor activity is a long-standing goal in drug discovery but hampered by the difficulties associated with the targeting of PPIs, in particular when extended and flat protein interfaces are involved. Peptidomimetics have been applied to inhibit PPIs, however with variable success, as for certain interfaces the mimicry of a single secondary structure element is insufficient to obtain high binding affinities. Here, we describe the design and characterization of a stabilized protein tertiary structure that acts as an inhibitor of the interaction between the tr

SUBMITTER: Adihou H 

PROVIDER: S-EPMC7591920 | biostudies-literature | 2020 Oct

REPOSITORIES: biostudies-literature