Comparative analysis for optimal LSD1 inhibitors evaluation techniques:pros and cons

Qiange Yin; Congcong Ma; Xiaoying Zhao; Panjie Wang; Dandan Shen; Chenchen Ren; Baojin Wang; Feiyan Li; Yan Yang; Hui-Min Liu; Li Yang; Yi-Chao Zheng

doi:10.1016/j.jpha.2025.101430

Article Contents

Article Navigation > Journal of Pharmaceutical Analysis > 2025 > Accepted Manu

Qiange Yin, Congcong Ma, Xiaoying Zhao, Panjie Wang, Dandan Shen, Chenchen Ren, Baojin Wang, Feiyan Li, Yan Yang, Hui-Min Liu, Li Yang, Yi-Chao Zheng. Comparative analysis for optimal LSD1 inhibitors evaluation techniques:pros and cons[J]. Journal of Pharmaceutical Analysis. doi: 10.1016/j.jpha.2025.101430

Citation:

Qiange Yin, Congcong Ma, Xiaoying Zhao, Panjie Wang, Dandan Shen, Chenchen Ren, Baojin Wang, Feiyan Li, Yan Yang, Hui-Min Liu, Li Yang, Yi-Chao Zheng. Comparative analysis for optimal LSD1 inhibitors evaluation techniques:pros and cons[J]. Journal of Pharmaceutical Analysis. doi: 10.1016/j.jpha.2025.101430

Citation:

Qiange Yin, Congcong Ma, Xiaoying Zhao, Panjie Wang, Dandan Shen, Chenchen Ren, Baojin Wang, Feiyan Li, Yan Yang, Hui-Min Liu, Li Yang, Yi-Chao Zheng. Comparative analysis for optimal LSD1 inhibitors evaluation techniques:pros and cons[J]. Journal of Pharmaceutical Analysis. doi: 10.1016/j.jpha.2025.101430

PDF( 3328 KB)

Comparative analysis for optimal LSD1 inhibitors evaluation techniques:pros and cons

doi: 10.1016/j.jpha.2025.101430

a. State Key Laboratory of Metabolic Dysregulation & Prevention and Treatment of Esophageal Cancer, Key Laboratory of Advanced Drug Preparation Technologies, Ministry of Education of China, Key Laboratory of Henan Province for Small Molecule Drug Discovery and Application, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, Henan, China;
b. Department of Obstetrics and Gynecology, The Third Affiliated Hospital of Zhengzhou University, Zhengzhou, Henan, China;
c. Department of Biochemistry and Molecular Biology, School of Basic Medical Sciences, Xinxiang Medical University, Xinxiang, China

Funds:

This work was supported by National Natural Science Foundation of China (No. 22477114)

Basic Research of the Key Project of the High Education from the Education Department of Henan Province (No.22ZX008, China)

the Young Top Talent Program from Henan Association for Science and Technology

D of Key Project of Henan Province (No. 241111312500, China)

the Young and Middle-aged Health Science and Technology Innovation Talent Project of Henan Province (No. YXKC2022019, China)

Natural Science Foundation of Henan Province (No. 252300420519, China).

Received Date: Apr. 20, 2025
Accepted Date: Aug. 09, 2025
Rev Recd Date: Jul. 29, 2025

Abstract

Abstract

Aberrant expression of lysine-specific demethylase 1 (LSD1) has been consistently implicated in a broad spectrum of malignancies, underscoring its relevance as a therapeutic target. Despite growing interest, the development of LSD1 inhibitors continues to face significant challenges, in part due to the enzyme’s dual role in catalysis and as a scaffolding protein within chromatin-remodeling complexes. Recent insights into the non-enzymatic functions of LSD1 have shifted the focus toward disrupting its protein–protein interactions, particularly with chromatin-modifying enzymes, as a complementary or alternative therapeutic strategy. In light of the limited systematic evaluation of available technologies, this work provides a critical overview and comparative analysis of current screening platforms and binding affinity assays, with particular attention to approaches capable of identifying LSD1 scaffold inhibitors. These efforts aim to accelerate the discovery of next-generation LSD1-targeted therapies with improved translational potential in oncology.
- LSD1,
- LSD1 inhibitors screening,
- LSD1 scaffold inhibitors