Small molecule inhibitors of peptidylprolyl cis/trans isomerase

Tadashi Mori, Takafumi Uchida

    Research output: Contribution to journalReview articlepeer-review

    5 Citations (Scopus)


    We would like to review the recent study of the inhibitors for peptidyl-prolyl cis/trans isomerase (PPIase), such as cyclophilin (Cyp), FK506- binding protein (FKBP) and Pin1. The inhibitors of Cyp and FKBP, CsA and FK506 respectively are well known potent immunosuppressive drugs. However, they cause a variety of side- effects. Therefore efforts are under way to identify PPIase inhibitors with less side- effects. In this review, efforts of discovering small molecule inhibitors are emphasized. While Cyp and FKBP inhibitors have been explored fairly thoroughly, the number of efforts to screen inhibitors of Pin1 is still limited so far. We think that the inhibitor of Pin1 has high potential as a drug.

    Original languageEnglish
    Pages (from-to)46-53
    Number of pages8
    JournalCurrent Enzyme Inhibition
    Issue number1
    Publication statusPublished - 2010 Feb 1


    • Cyclophilin
    • FK-506 binding protein
    • Peptidyl-prolyl cis/trans isomerases
    • Pin1
    • Small molecule inhibitors

    ASJC Scopus subject areas

    • Biochemistry
    • Molecular Medicine
    • Drug Discovery


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