Target Information

Target General Infomation
Target ID
T16308
Former ID
TTDR00355
Target Name
Peptidyl-prolyl cis-trans isomerase NIMA-interacting 1
Gene Name
PIN1
Synonyms
PPIase Pin1; Peptidyl prolyl cis/trans isomerase Pin1; Prolyl isomerase Pin1; Rotamase Pin1; PIN1
Target Type
Research
Function
Essential PPIase that regulates mitosis presumably by interacting with NIMA and attenuating its mitosis-promoting activity. Displays a preference for an acidic residue N-terminal to the isomerized proline bond. Catalyzes pSer/Thr-Pro cis/trans isomerizations. Down-regulates kinase activity of BTK. Can transactivate multiple oncogenes and induce centrosome amplification, chromosome instability and cell transformation. Required for the efficient dephosphorylation and recycling of RAF1 after mitogen activation. Binds and targets PML and BCL6 for degradation in a phosphorylation-dependent manner.
BioChemical Class
Cis-trans-isomerases
Target Validation
T16308
UniProt ID
Q13526
EC Number
EC 5.2.1.8
Sequence
MADEEKLPPGWEKRMSRSSGRVYYFNHITNASQWERPSGNSSSGGKNGQGEPARVRCSHL
LVKHSQSRRPSSWRQEKITRTKEEALELINGYIQKIKSGEEDFESLASQFSDCSSAKARG
DLGAFSRGQMQKPFEDASFALRTGEMSGPVFTDSGIHIILRTE
Inhibitor (R)-2-(2-naphthamido)-3-m-tolylpropanoic acid Drug Info [530771]
(R)-2-(2-naphthamido)-3-p-tolylpropanoic acid Drug Info [530771]
(R)-2-(2-naphthamido)-5-phenylpent-4-ynoic acid Drug Info [530771]
(R)-3-(2-naphthamido)-4-m-tolylbutanoic acid Drug Info [530771]
(R,)-2-(2-naphthamido)-5-phenylpent-4-enoic acid Drug Info [530771]
3,6,9,12,15,18-HEXAOXAICOSANE Drug Info [551374]
Ac-Bth-Thr(PO3H2)-Pip-Nal-Gln-NH2 Drug Info [528104]
Ac-Phe-D-Thr(PO3H2)-Pip-Nal-Gln-NH2 Drug Info [528104]
Ac-Phe-Thr(PO3H2)-Pip-Nal-Gln-NH2 Drug Info [528104]
Beta-(2-Naphthyl)-Alanine Drug Info [551374]
Pathways
KEGG Pathway RIG-I-like receptor signaling pathway
Pathway Interaction Database p73 transcription factor network
C-MYC pathway
PDGFR-beta signaling pathway
p53 pathway
Reactome ISG15 antiviral mechanism
Negative regulators of RIG-I/MDA5 signaling
WikiPathways ISG15 antiviral mechanism
RIG-I/MDA5 mediated induction of IFN-alpha/beta pathways
References
Ref 528104J Med Chem. 2006 Apr 6;49(7):2147-50.Nanomolar inhibitors of the peptidyl prolyl cis/trans isomerase Pin1 from combinatorial peptide libraries.
Ref 530771Bioorg Med Chem Lett. 2010 Apr 1;20(7):2210-4. Epub 2010 Feb 14.Structure-based design of novel human Pin1 inhibitors (II).
Ref 551374The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.

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