Melanotan I

Zhang M, Chen M, Ge Y, Gunning W, Gong R

FASEB journal : official publication of the Federation of American Societies for Experimental Biology

In an active-immunization mouse model of THSD7A-associated membranous nephropathy, the melanocortin agonist NDP-MSH (Melanotan I) reduced proteinuria, glomerular immune deposits, and circulating autoantibody levels; in B cells isolated from these mice, NDP-MSH directly suppressed plasma-cell differentiation and antibody production via the MITF/IRF4 signaling axis.

Li J, Wang J, Long X, Lin J, Su M, Ding C, et al.

Journal of materials chemistry. B

In cultured RSC96 Schwann cells and a rat sciatic nerve defect model, NDP-MSH (Melanotan I) delivered via a biodegradable nerve conduit reduced markers of oxidative stress (reactive oxygen species, LDH release) and apoptosis, and shifted the post-injury immune microenvironment toward an M2-enriched profile, consistent with melanocortin-receptor-mediated antioxidant and pro-survival signaling in peripheral nerve tissue.

Yang Yk, Dickinson C, Haskell-Luevano C, Gantz I

The Journal of biological chemistry

Using site-directed mutagenesis of the cloned human melanocortin-1 receptor expressed in mammalian cells, this study identified specific acidic (Glu94, Asp117, Asp121) and aromatic (Phe175, Phe196, Phe257) receptor residues required for binding and activation by the superpotent alpha-MSH analog NDP-MSH (Melanotan I), mapping the molecular basis of the ligand-receptor interaction.

Jiang J, Sharma SD, Hruby VJ, Bentley DL, Fink JL, Hadley ME

Pigment cell research

Using NDP-MSH (Melanotan I) conjugated to latex microspheres and scanning electron microscopy, researchers visualized melanocortin receptor binding on cultured human epidermal melanocytes and keratinocytes, and confirmed binding specificity through competitive-blocking and control-ligand experiments, establishing melanocortin receptor expression as a characteristic marker of these skin cell types in vitro.

Haskell-Luevano C, Miwa H, Dickinson C, Hruby VJ, Yamada T, Gantz I

Biochemical and biophysical research communications

In mouse L cells transfected with the cloned human peripheral melanocortin receptor (hMC1R), this foundational pharmacology study measured receptor-binding affinity and cAMP-stimulating potency of alpha-MSH and its superpotent analog MT-I ([Nle4,D-Phe7]alpha-MSH, Melanotan I), finding MT-I bound with higher affinity and stimulated cAMP production more potently than native alpha-MSH in this receptor assay.