At the E61K, D90N, Y157S and C271R hMC4R variants, all agonist ligands examined, a set that includes MTII, were only partially efficacious in generating a maximal signaling response.
In plain wordsIn cells, at four altered MC4 receptors, all tested agonists, including Melanotan II, gave only a partial response.
- Peptide
- Melanotan II
- Outcome
- DecreaseMaximal signaling efficacy at E61K, D90N, Y157S and C271R hMC4R variants
- Study
humann: not reported in source
Cells expressing human MC4R polymorphisms- Outcome group
- Receptor activity and mechanism · Pharmacology
- Studied dose
- Dose not stated
Source sentences
At the E61K, D90N, Y157S, and C271R hMC4Rs, all agonist ligands examined were only partially efficacious in generating a maximal signaling response (partial agonists) and possessed significantly decreased endogenous agonist ligand potency.
2 context sentences(design, population, supporting numbers)
The goal of the current study is to perform a similar comprehensive side-by-side characterization of 30 additional human hMC4R with single nucleotide polymorphisms
and synthetic agonists [NDP-MSH, MTII,