Targeting Pin1 for Modulation of Cell Motility and Cancer Therapy

Peptidyl-prolyl <i>cis-trans</i> isomerase NIMA-interacting 1 (Pin1) specifically binds and isomerizes the phosphorylated serine/threonine-proline (pSer/Thr-Pro) motif, which leads to changes in protein conformation and function. Pin1 is widely overexpressed in cancers and plays an impor...

Full description

Bibliographic Details
Main Authors: Hsiang-Hao Chuang, Yen-Yi Zhen, Yu-Chen Tsai, Cheng-Hao Chuang, Ming-Shyan Huang, Michael Hsiao, Chih-Jen Yang
Format: Article
Language:English
Published: MDPI AG 2021-03-01
Series:Biomedicines
Subjects:
Online Access:https://www.mdpi.com/2227-9059/9/4/359
_version_ 1797539389681696768
author Hsiang-Hao Chuang
Yen-Yi Zhen
Yu-Chen Tsai
Cheng-Hao Chuang
Ming-Shyan Huang
Michael Hsiao
Chih-Jen Yang
author_facet Hsiang-Hao Chuang
Yen-Yi Zhen
Yu-Chen Tsai
Cheng-Hao Chuang
Ming-Shyan Huang
Michael Hsiao
Chih-Jen Yang
author_sort Hsiang-Hao Chuang
collection DOAJ
description Peptidyl-prolyl <i>cis-trans</i> isomerase NIMA-interacting 1 (Pin1) specifically binds and isomerizes the phosphorylated serine/threonine-proline (pSer/Thr-Pro) motif, which leads to changes in protein conformation and function. Pin1 is widely overexpressed in cancers and plays an important role in tumorigenesis. Mounting evidence has revealed that targeting Pin1 is a potential therapeutic approach for various cancers by inhibiting cell proliferation, reducing metastasis, and maintaining genome stability. In this review, we summarize the underlying mechanisms of Pin1-mediated upregulation of oncogenes and downregulation of tumor suppressors in cancer development. Furthermore, we also discuss the multiple roles of Pin1 in cancer hallmarks and examine Pin1 as a desirable pharmaceutical target for cancer therapy. We also summarize the recent progress of Pin1-targeted small-molecule compounds for anticancer activity.
first_indexed 2024-03-10T12:45:22Z
format Article
id doaj.art-3e6de68364774303935ec9f5d90d6ff4
institution Directory Open Access Journal
issn 2227-9059
language English
last_indexed 2024-03-10T12:45:22Z
publishDate 2021-03-01
publisher MDPI AG
record_format Article
series Biomedicines
spelling doaj.art-3e6de68364774303935ec9f5d90d6ff42023-11-21T13:32:10ZengMDPI AGBiomedicines2227-90592021-03-019435910.3390/biomedicines9040359Targeting Pin1 for Modulation of Cell Motility and Cancer TherapyHsiang-Hao Chuang0Yen-Yi Zhen1Yu-Chen Tsai2Cheng-Hao Chuang3Ming-Shyan Huang4Michael Hsiao5Chih-Jen Yang6Division of Pulmonary and Critical Care Medicine, Department of Internal Medicine, Kaohsiung Medical University Hospital, Kaohsiung Medical University, Kaohsiung 80708, TaiwanDivision of Nephrology, Department of Internal Medicine, Kaohsiung Medical University Hospital, Kaohsiung Medical University, Kaohsiung 80708, TaiwanDivision of Pulmonary and Critical Care Medicine, Department of Internal Medicine, Kaohsiung Medical University Hospital, Kaohsiung Medical University, Kaohsiung 80708, TaiwanDivision of Pulmonary and Critical Care Medicine, Department of Internal Medicine, Kaohsiung Medical University Hospital, Kaohsiung Medical University, Kaohsiung 80708, TaiwanDepartment of Internal Medicine, E-Da Cancer Hospital, School of Medicine, I-Shou University, Kaohsiung 82445, TaiwanGenomics Research Center, Academia Sinica, Taipei 11529, TaiwanDivision of Pulmonary and Critical Care Medicine, Department of Internal Medicine, Kaohsiung Medical University Hospital, Kaohsiung Medical University, Kaohsiung 80708, TaiwanPeptidyl-prolyl <i>cis-trans</i> isomerase NIMA-interacting 1 (Pin1) specifically binds and isomerizes the phosphorylated serine/threonine-proline (pSer/Thr-Pro) motif, which leads to changes in protein conformation and function. Pin1 is widely overexpressed in cancers and plays an important role in tumorigenesis. Mounting evidence has revealed that targeting Pin1 is a potential therapeutic approach for various cancers by inhibiting cell proliferation, reducing metastasis, and maintaining genome stability. In this review, we summarize the underlying mechanisms of Pin1-mediated upregulation of oncogenes and downregulation of tumor suppressors in cancer development. Furthermore, we also discuss the multiple roles of Pin1 in cancer hallmarks and examine Pin1 as a desirable pharmaceutical target for cancer therapy. We also summarize the recent progress of Pin1-targeted small-molecule compounds for anticancer activity.https://www.mdpi.com/2227-9059/9/4/359Pin1<i>cis</i>-<i>trans</i> isomerizationtumorigenesiscell motilitymetastasiscancer therapeutics
spellingShingle Hsiang-Hao Chuang
Yen-Yi Zhen
Yu-Chen Tsai
Cheng-Hao Chuang
Ming-Shyan Huang
Michael Hsiao
Chih-Jen Yang
Targeting Pin1 for Modulation of Cell Motility and Cancer Therapy
Biomedicines
Pin1
<i>cis</i>-<i>trans</i> isomerization
tumorigenesis
cell motility
metastasis
cancer therapeutics
title Targeting Pin1 for Modulation of Cell Motility and Cancer Therapy
title_full Targeting Pin1 for Modulation of Cell Motility and Cancer Therapy
title_fullStr Targeting Pin1 for Modulation of Cell Motility and Cancer Therapy
title_full_unstemmed Targeting Pin1 for Modulation of Cell Motility and Cancer Therapy
title_short Targeting Pin1 for Modulation of Cell Motility and Cancer Therapy
title_sort targeting pin1 for modulation of cell motility and cancer therapy
topic Pin1
<i>cis</i>-<i>trans</i> isomerization
tumorigenesis
cell motility
metastasis
cancer therapeutics
url https://www.mdpi.com/2227-9059/9/4/359
work_keys_str_mv AT hsianghaochuang targetingpin1formodulationofcellmotilityandcancertherapy
AT yenyizhen targetingpin1formodulationofcellmotilityandcancertherapy
AT yuchentsai targetingpin1formodulationofcellmotilityandcancertherapy
AT chenghaochuang targetingpin1formodulationofcellmotilityandcancertherapy
AT mingshyanhuang targetingpin1formodulationofcellmotilityandcancertherapy
AT michaelhsiao targetingpin1formodulationofcellmotilityandcancertherapy
AT chihjenyang targetingpin1formodulationofcellmotilityandcancertherapy