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Literature summary for 5.2.1.8 extracted from

  • Liu, T.; Liu, Y.; Kao, H.Y.; Pei, D.
    Membrane permeable cyclic peptidyl inhibitors against human peptidylprolyl isomerase Pin1 (2010), J. Med. Chem., 53, 2494-2501.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 5.2.1.8

Cloned(Commentary)

Cloned (Comment) Organism
expression of MBP-Pin1 fusion protein in Escherichia coli strain BL21(DE3) Homo sapiens

Protein Variants

Protein Variants Comment Organism
S16A/Y23A the mutations of Pin1 protein do not affect the structure of Pin1 but abolishes the ability of the WW domain to bind pSer/pThr-Pro ligands Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
cyclo(Arg-Arg-Arg-D-pThr-Pip-Nal-Arg-Arg-Gln)
-
 Homo sapiens
cyclo(Arg-Arg-Arg-D-Thr-Pip-Nal-Arg-Arg-Gln)
-
 Homo sapiens
cyclo(D-Ala-Gln-Glu-Mpa-Mal-Ile-Gln)
-
 Homo sapiens
cyclo(D-Ala-Gly-D-pThr-Pip-Nal-Orn-Gln)
-
 Homo sapiens
cyclo(D-Ala-Ile-D-pSer-Pro-Nal-Orn-Gln)
-
 Homo sapiens
cyclo(D-Ala-Sar-D-pThr-Pip-Nal-Tyr-Gln)
-
 Homo sapiens
cyclo(D-Ala-Sar-D-pThr-Pip-Nal-Tyr-Gln)-Lys-SH
-
 Homo sapiens
cyclo(D-Arg-D-Arg-D-pThr-Pip-Nal-Arg-D-Arg-D-Arg-D-Arg-Gln)
-
 Homo sapiens
cyclo(D-Arg-D-Arg-D-pThr-Pip-Nal-Arg-Gln)
-
 Homo sapiens
cyclo(D-Arg-D-Arg-D-Thr-Pip-Nal-Arg-D-Arg-D-Arg-D-Arg-Gln)
-
 Homo sapiens
cyclo(D-Arg-D-Arg-D-Thr-Pip-Nal-Arg-Gln)
-
 Homo sapiens
additional information the OBOC peptide library screening for and selection of selected inhibitors containing a consensus motif of D-pThr-L-piperidine-2-carboxylic acid-L-2-naphthylalanine using inactive enzyme mutant S16A/Y23A, interaction analysis by Isothermal titration calorimetry, overview. A second generation of cell permeable Pin1 inhibitors, that have have antiproliferative activity against the cancer cells, is designed by replacing the noncritical residues within the cyclic peptide ring with arginine residues. Effects of inhibitor peptides in vivo on cancer cells, e.g. HeLa cells, overview Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Homo sapiens promyelocytic leukemia protein, PML, and silencing mediator for retinoic acid and thyroid hormone receptor, SMRT, are Pin1 substrates ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
recombinant MBP-Pin1 fusion protein from Escherichia coli strain BL21(DE3) by amylose affinity chromatography Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
breast cancer cell
-
 Homo sapiens
-
BT-474 cell
-
 Homo sapiens
-
HeLa cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information promyelocytic leukemia protein, PML, and silencing mediator for retinoic acid and thyroid hormone receptor, SMRT, are Pin1 substrates Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
peptidylprolyl isomerase
-
 Homo sapiens
Pin1
-
 Homo sapiens
PPIase
-
 Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.8
-
 assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000032
-
-
 Homo sapiens cyclo(D-Ala-Sar-D-pThr-Pip-Nal-Tyr-Gln)-Lys-SH
0.000043
-
-
 Homo sapiens cyclo(D-Ala-Gly-D-pThr-Pip-Nal-Orn-Gln)
0.00022
-
-
 Homo sapiens cyclo(D-Arg-D-Arg-D-pThr-Pip-Nal-Arg-Gln)
0.00031
-
-
 Homo sapiens cyclo(D-Ala-Sar-D-pThr-Pip-Nal-Tyr-Gln)
0.0011
-
-
 Homo sapiens cyclo(D-Ala-Ile-D-pSer-Pro-Nal-Orn-Gln)
0.0011
-
-
 Homo sapiens cyclo(Arg-Arg-Arg-D-pThr-Pip-Nal-Arg-Arg-Gln)
0.0025
-
-
 Homo sapiens cyclo(D-Arg-D-Arg-D-pThr-Pip-Nal-Arg-D-Arg-D-Arg-D-Arg-Gln)
0.063
-
-
 Homo sapiens cyclo(D-Ala-Gln-Glu-Mpa-Mal-Ile-Gln)
0.3
-
 above Homo sapiens cyclo(D-Arg-D-Arg-D-Thr-Pip-Nal-Arg-Gln)
0.3
-
 above Homo sapiens cyclo(D-Arg-D-Arg-D-Thr-Pip-Nal-Arg-D-Arg-D-Arg-D-Arg-Gln)
0.3
-
 above Homo sapiens cyclo(Arg-Arg-Arg-D-Thr-Pip-Nal-Arg-Arg-Gln)

General Information

General Information Comment Organism
physiological function Pin1 regulates the function and/or stability of phosphoproteins by altering the conformation of specific pSer/pThr-Pro peptide bonds Homo sapiens