Identification of Crocin I as a positive modulator of GSTP1 with potential relevance to prostate cancer.

Authors

Hao Qin, YuanYuan Wang, Yukai Yang, Haihong Fang, Yangbiao Li, Yuxiu Yang, Yinhua Xiong, Lin Zhang

Published in

Journal of enzyme inhibition and medicinal chemistry. Volume 41. Issue 1. Pages 2736806. Epub Sep 28, 2026.

Abstract

Glutathione S-transferase Pi 1 (GSTP1) is frequently silenced in prostate adenocarcinoma (PRAD), yet whether its residual catalytic activity can be chemically enhanced is largely unexplored. Here, we identify Crocin I as a positive modulator of GSTP1 through structure-based screening, biophysical characterisation, and biochemical validation. Bio-layer interferometry (BLI) supported a concentration-dependent association between Crocin I and GSTP1, and enzymatic assays demonstrated enhanced catalytic activity. Michaelis-Menten kinetics showed that Crocin I increased V_max without markedly altering the apparent K_m, consistent with apparent non-competitive activation of 1-chloro-2,4-dinitrobenzene conjugation under the tested conditions. Differential scanning fluorimetry showed that Crocin I altered GSTP1 thermal behaviour, with a comparable shift in the presence of the H-site inhibitor NBDHEX. Exploratory systems-level analyses further connected Crocin I-GSTP1 modulation with redox- and PRAD-associated networks. Together, these findings establish Crocin I as a previously unrecognised positive modulator of GSTP1 and provide a biochemical foundation for GSTP1-directed modulation in PRAD.

PMID:
42803268
Bibliographic data and abstract were imported from PubMed on 28 Sep 2026.

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