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2010•Current Enzyme InhibitionRequires access

Small Molecule Inhibitors of Peptidylprolyl cis/trans Isomerase

Tadashi Mori, Takafumi Uchida

Open publisher page 6 citations

Abstract

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. Keywords: Peptidyl-prolyl cis/trans isomerases, cyclophilin, FK-506 binding protein, Pin1, small molecule inhibitors

About this research paper

What this paper is about

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. Keywords: Peptidyl-prolyl cis/trans isomerases, cyclophilin, FK-506 binding protein, Pin1, small molecule inhibitors

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Available abstract

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. Keywords: Peptidyl-prolyl cis/trans isomerases, cyclophilin, FK-506 binding protein, Pin1, small molecule inhibitors

Key concepts: FKBP, PIN1, Peptidylprolyl isomerase, Cyclophilin, Isomerase, Cis-trans-Isomerases, Prolyl isomerase, Cyclophilin A

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