Matrix metalloproteinases (MMPs) are a group of enzymes well-known for degrading most types of extracellular matrix (ECM) proteins. This leads to skin wrinkling and other signs of aging.
As such, MMPs have been the target of various anti-aging efforts in the cosmetics industry; not unlike the work in a new patent from LVMH Recherche and the Paris-based Institut National de la Santé et de la Recherche Médicale (INSERM).
According to these inventors, when keratinocytes in the epidermis are exposed to UV or other inflammation triggers, they express the specific MMP known as MMP-9. Yet, while other MMP inhibitors are known, they show some side effects in skin and demonstrate potential cytotoxicity.
The aim of the present invention was therefore to solve these issues and propose a solution for regulating the degradation of ECM components via MMP-9, in order to control skin remodeling and reduce aging-related changes in skin appearance. A specific aptamer was identified that hits this mark.
Aptamers inhibiting the enzymatic activity of the MMP-9 protein
U.S. Patent 9902961
Assignee: LVMH Recherche and Institut National de la Santé et de la Recherche Médicale (INSERM)
Publication date: Feb. 27, 2018
The present invention relates to a DNA aptamer—i.e., an oligonucleotide or peptide with a specific molecular target—having a G-quadruplex structure that can penetrate skin cells to inhibit the enzymatic activity of MMP-9 protein. Dermatological and cosmetic uses of the aptamer also are described.
According to the patent, these inventors used a library of phosphotriester oligonucleotide sequences having the same composition as natural DNA to systematically identify, isolate and characterize sequences that could interact with metalloproteinase-9. These aptamers were then tested for their ability to inhibit MMP-9 on synthetic substrates, in cells and on a skin model.