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http://dx.doi.org/10.4161/cc.26077 | DOI Listing |
Eur J Med Chem
December 2025
National Facility for Protein Science in Shanghai, Shanghai Advanced Research Institute, Chinese Academy of Sciences, Shanghai, 201210, People's Republic of China. Electronic address:
Pin1 is a phosphorylation-dependent peptidyl-prolyl isomerase that specifically recognizes and catalyzes the cis-trans isomerization of pSer/Thr-Pro motifs. It plays a pivotal role in cell cycle regulation, signal transduction, and tumorigenesis. Due to its overexpression in many cancer types, Pin1 has emerged as a promising target for the development of anticancer drugs.
View Article and Find Full Text PDFBiochim Biophys Acta Mol Cell Res
August 2025
Department of Biomedical Chemistry, Graduate School of Biomedical and Health Sciences, Hiroshima University, Hiroshima 734-8553, Japan. Electronic address:
Breast cancer is the most common tumor in women, and approximately 70 % of cases are diagnosed to be estrogen receptor α (ERα)-positive. Estradiol (E2)-ERα signaling is undoubtedly involved in the development of breast cancer, and the upregulation of this pathway is linked to tamoxifen resistance. However, ERα regulation is complex, and the underlying mechanisms have not been comprehensively elucidated.
View Article and Find Full Text PDFNat Commun
August 2025
Zhejiang Key Laboratory of Pancreatic Disease, The First Affiliated Hospital, Zhejiang Key Laboratory of Frontier Medical Research on Cancer Metabolism, and Institute of Translational Medicine, Zhejiang University School of Medicine, Hangzhou, Zhejiang, China.
Hypoxia frequently occurs during rapid tumour growth. However, how tumour cells adapt to hypoxic stress by remodeling central cellular pathways remains largely unclear. Here, we show that hypoxia induces casein kinase 2 (CK2)-mediated glucokinase (GCK) S398 phosphorylation, which exposes its nuclear localization signal (NLS) for importin α1 binding and nuclear translocation.
View Article and Find Full Text PDFBioorg Chem
August 2025
University of Hradec Kralove, Faculty of Science, Department of Chemistry, Rokitanskeho 62, 500 03 Hradec Kralove, Czech Republic. Electronic address:
Cyclophilin D (CypD) is a mitochondrial enzyme and the key regulator of mitochondrial permeability transition pore (mPTP). Inhibition of CypD/mPTP holds promise as a therapeutic strategy for treatment of variety of diseases including ischemia-reperfusion injury, or neurodegeneration. Compounds based on the N-4-aminobenzyl-N'-(2-(2-phenylpyrrolidin)-2-oxoethyl)urea structural scaffold present the most potent class of small-molecule CypD inhibitors identified to date.
View Article and Find Full Text PDFProteomics
July 2025
Department of Biochemistry, Schulich School of Medicine & Dentistry, Western University, London, Ontario, Canada.
Peptidyl-prolyl isomerase, NIMA-interacting protein 1-(Pin1) catalyses the cis-trans interconversion of the inflexible bond between serine or threonine residues and proline at the +1 position (pSer/pThr-Pro). Although initially discovered as an essential regulator of cell division, Pin1 has since been identified as a regulator of many biological processes and is associated with numerous malignancies and neurodegenerative disorders. Pin1 has been shown to influence phosphorylation by modulating phosphatase accessibility.
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