At the S58C and R165Q/W hMC4R variants, MTII potency was reduced only 2-9-fold compared with the wild-type receptor.
In plain wordsIn cells, MTII lost only 2 to 9 times of its potency at two variant receptors, compared with the normal receptor.
- Peptide
- Melanotan II
- Outcome
- DecreaseMTII potency at S58C and R165Q/W hMC4R polymorphisms versus wild type
- Study
n: not reported in source
cells expressing 40 human MC4R polymorphic receptors- Comparator
- Wild-type hMC4R
- Outcome group
- Receptor activity and mechanism · Pharmacology
- Studied dose
- Dose not stated
Measurements
- Potency reduction vs wild type
- 2 to 9 fold
- MTII at S58C and R165Q/W hMC4R
Source sentences
The S58C and R165Q/W hMC4Rs possessed significantly reduced endogenous agonist potency (15- to 90-fold), but the synthetic ligands NDP-MSH and MTII possessed only 2-9-fold reduced potency as compared to the wild-type receptor, suggesting their potential as therapeutic ligands to treat individuals wi…