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  • [Pin1: a multi-talented peptidyl prolyl cis-trans isomerase and a promising therapeutic target for human cancers].

[Pin1: a multi-talented peptidyl prolyl cis-trans isomerase and a promising therapeutic target for human cancers].

Medecine sciences : M/S (2014-09-02)
Justine Marsolier, Jonathan B Weitzman
摘要

Post-translational modifications are critical to modulate protein function. A post-translational mechanism, peptidyl prolyl cis-trans isomerisation, plays a key role in protein regulation. Pin1 is a ubiquitous peptidyl prolyl cis-trans isomerase conserved from Archae to Human. This enzyme binds and isomerizes phospho-serine/threonine-proline motifs. This process can induce conformational change in protein targets and modulates their activity, cellular localization, phosphorylation state, stability and/or protein-protein interactions. Pin1 activity regulates proteins involved in cell proliferation, pluripotency or cellular invasion. Pin1 is overexpressed in several human cancers and contributes to tumorigenesis. Its inactivation constitutes a promising therapeutic strategy.