Work

Design and Synthesis of Hydroxamate-Based Matrix Metalloproteinase-2 Inhibitors for Anti-Photoaging

Year: 2025

Type: article

Abstract: Matrix metalloproteinases-2 (MMP-2) is crucial for collagen degradation at the dermal-epidermal junction, contributing to skin aging and photoaging.This study presents a series of hydroxamatebased inhibitors selectively targeting MMP-2.Through structure-activity relationship analysis, we systematically modified the N-arylsulfonyl group and amino acid backbone to enhance MMP-2 selectivity.Compounds 1ad, 1af, and 4an showed strong MMP-2 inhibition, with 1ad demonstrating nanomolar-level selectivity.Zymogram assays revealed 30-60% MMP-2 activity reduction, while gene expression analysis confirmed post-transcriptional inhibition.These hydroxamate-based inhibitors are promising candidates for anti-photoaging applications, combining potent MMP-2 inhibition with simplified synthesis, supporting their potential for large-scale cosmetic formulations aimed at improving skin firmness and reducing wrinkles.

Source: Journal of Microbiology and Biotechnology

DOI: 10.4014/jmb.2412.12027

Authors: Jin Young Lee, Geunhyuk Jang, Yung Hyup Joo, Joonho Choi, Dong-Woo Lee, Jae Won Yoo

Institutions: Yonsei University, Amorepacific (South Korea)

Language: English

Topic: Protease and Inhibitor Mechanisms

Subfield: Cancer Research

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: bronze

Funders: Amorepacific Corporation, Ministry of Health and Welfare