2. Academic Validation
  3. Biological Function of Pin1 in Vivo and Its Inhibitors for Preclinical Study: Early Development, Current Strategies, and Future Directions

Biological Function of Pin1 in Vivo and Its Inhibitors for Preclinical Study: Early Development, Current Strategies, and Future Directions

  • J Med Chem. 2023 Jul 27;66(14):9251-9277. doi: 10.1021/acs.jmedchem.3c00390.
Siyu He 1,  Linjie Li 2,  Rui Jin 2,  Xiaojie Lu 2 3 4
Affiliations

Affiliations

  • 1 School of Life Sciences, Shanghai University, Shanghai 200444, P. R. China.
  • 2 State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, P. R. China.
  • 3 School of Chinese Materia Medica, Nanjing University of Chinese Medicine, Nanjing 210023, P. R. China.
  • 4 University of Chinese Academy of Sciences, Beijing 100049, P. R. China.
PMID: 37438908 DOI: 10.1021/acs.jmedchem.3c00390
Abstract

Peptidyl-prolyl cis/trans isomerase family (PPIase) is structurally divided into three subfamilies, cyclophilins (Cyps), FK506-binding proteins (FKBPs), and parvulins. PIN1 belongs to the parvulin family and is the only enzyme capable of isomerizing the phosphorylated Ser/Thr-Pro motif (p-Ser/Thr-Pro) in its interacting proteins. Due to its multibiological functions in vivo, including folding, intracellular signaling, transcription, cell cycle progression, and Apoptosis, PIN1 is extensively studied as a promising drug target for various human diseases, especially Cancer. In this Perspective, we summarized the literature covering diverse classes of PIN1 inhibitors and the inhibition mechanism, aiming to provide insights for the design of potent PIN1 inhibitors and suggest alternative strategies for developing potent PIN1 inhibitors.

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