In structural and cAMP assay analysis of cyclic and linear MSH analogues, a lysine residue at the C-terminus of the His-Phe-Arg-Trp core sequence was an important determinant of receptor selectivity.
In plain wordsIn lab tests, one lysine in the core of MSH analogues helped decide which melanocortin receptor they favour.
- Peptide
- Melanotan I (afamelanotide)
- Outcome
- Not applicableDeterminant of receptor selectivity in melanocortin analogues
- Study
n: not reported in source
- Outcome group
- Receptor activity and mechanism · Pharmacology
Source sentences
Using data from c-AMP assays in combination with structural analysis of melanocortin receptor/ligand models, we conclude that a lysine residue at the C-terminus of the His-Phe-Arg-Trp core sequence of melanocortin hormone is an important determinant for receptor selectivity in the both cyclic and linear MSH analogues.
1 context sentence(design, population, supporting numbers)
To enable the design of a selective drug candidate, the solution structures of four peptidyl analogues of the melanocyte stimulating hormones, NDP-MSH, NDP-MSH(4-10) and two cyclic forms ([C5,C10]NDP-MSH(5-10), [C5,C10]NDP-MSH(5-11)), were characterized by two-dimensional nuclear magnetic resonance…
In this study, Melanotan I (afamelanotide) was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Melanotan I (afamelanotide).