FIELD: pharmaceuticals.
SUBSTANCE: group of inventions relates to derivatives of peptide nucleic acids (PNA) targeting human matrix metalloproteinase-1 (MMP-1) pre-mRNA and their use for the treatment of skin aging conditions associated with human MMP-1 protein. A PNA derivative of formula I or a pharmaceutically acceptable salt thereof for inducing exon skipping in human MMP-1 pre-mRNA are proposed. A PNA derivative has at least a 14-dimensional complementary overlap with a 16-dimensional pre-mRNA sequence [(5'→ 3') CAUAUAUGGUGAGUAU] in human MMP-1 pre-mRNA. Also a pharmaceutical composition and a cosmetic composition for reducing skin aging associated with human MMP-1, and a method of reducing skin aging are proposed.
EFFECT: PNA derivative has good cellular or membrane permeability, can be locally administered as a "naked" oligonucleotide to induce MMP-1 "exon 5" skipping in the skin, improve skin condition and prevent its aging.
6 cl, 13 dwg, 8 ex
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Authors
Dates
2023-08-28—Published
2019-05-03—Filed