- Guide to PHARMACOLOGY
Compound class: Peptide or derivative
Comment: MM07, is a cyclic peptide agonist of the apelin receptor that is more stable than the endogenous apelin peptide. It acts as a biased agonist at the apelin receptor, that can preferentially stimulate the G protein pathway. It was hypothesised that this biased action could translate to improved efficacy in vitro by selectively stimulating vasodilatation and inotropic actions, whilst avoiding activation of detrimental β-arrestin-dependent pathways.
We generated the HELM annotation and SMILES for MM07 using HELM Editor v1.4 (from Pistoia Alliance).
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Brame AL, Maguire JJ, Yang P, Dyson A, Torella R, Cheriyan J, Singer M, Glen RC, Wilkinson IB, Davenport AP. (2015)
Design, characterization, and first-in-human study of the vascular actions of a novel biased apelin receptor agonist.
Hypertension, 65 (4): 834-40. [PMID:25712721]
2. Yang P, Read C, Kuc RE, Nyimanu D, Williams TL, Crosby A, Buonincontri G, Southwood M, Sawiak SJ, Glen RC et al.. (2019)
A novel cyclic biased agonist of the apelin receptor, MM07, is disease modifying in the rat monocrotaline model of pulmonary arterial hypertension.
Br J Pharmacol, 176 (9): 1206-1221. [PMID:30710493]