Abstract
Pin1 is the only known peptidyl-prolyl cis–trans isomerase (PPIase) that specifically recognizes and isomerizes the phosphorylated Serine/Threonine-Proline (pSer/Thr-Pro) motif. The Pin1-mediated structural transformation posttranslationally regulates the biofunctions of multiple proteins. Pin1 is involved in many cellular processes, the aberrance of which lead to both degenerative and neoplastic diseases. Pin1 is highly expressed in the majority of cancers and its deficiency significantly suppresses cancer progression. According to the ground-breaking summaries by Hanahan D and Weinberg RA, the hallmarks of cancer comprise ten biological capabilities. Multiple researches illuminated that Pin1 contributes to these aberrant behaviors of cancer via promoting various cancer-driving pathways. This review summarized the detailed mechanisms of Pin1 in different cancer capabilities and certain Pin1-targeted small-molecule compounds that exhibit anticancer activities, expecting to facilitate anticancer therapies by targeting Pin1.
Highlights
Proline (Pro)-directed Serine/Threonine (Ser/Thr) phosphorylation is a common modification of numerous signaling pathways
Their work showed that this novel formulation exhibits long-term inhibition of Pin[1] and is more efficient than the traditional all trans retinoic acid (ATRA) to suppress hepatocellular carcinoma (HCC) cell growth[223]
After decades of research, we are uncovering the secret of cancer
Summary
Proline (Pro)-directed Serine/Threonine (Ser/Thr) phosphorylation is a common modification of numerous signaling pathways. Research indicated that Pin[1] increases the transcriptional activity[48], ERE binding affinity[49], and inhibits the E3 ligase E6AP-induced degradation of ERα in breast cancer[50]. Research illuminated that Pin[1] promotes CDK-induced phosphorylation[76] and inhibits PP2A-mediated dephosphorylation[77] of pRb that subsequently activate E2F and trigger cells into S phase. Pin[1] enhances the E3 adapter KLHL20-induced ubiquitination of PML to promote the proliferation and angiogenesis of prostate cancer[79].
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