Characteristics of parathyroid hormone-1 receptor agonists and antagonists.
Future Med Chem
; 11(8): 817-831, 2019 04.
Article
in En
| MEDLINE
| ID: mdl-30998079
ABSTRACT
Aim:
Parathyroid hormone-1 receptor (PTH1R) is a member of B G protein-coupled receptors. The agonistic activation of the PTH1R results in the production and secretion of osteoclast-stimulating cytokines while antagonists may be used to treat bone metastases, hypercalcemia, cachexia and hyperparathyroidism.Results:
We built pharmacophore models and investigated the characteristics of PTH1R agonists and antagonists. The agonist model consists of three hydrophobic points, one hydrogen bond acceptor and one positive ionizable point. The antagonist model consists of one hydrogen bond donor and three hydrophobic points.Conclusion:
The features of the two models are similar, but the hydrogen bond acceptor, which is the main difference between PTH1R agonists and antagonists, suggests it may be essential for the agonist.Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Drug Design
/
Receptor, Parathyroid Hormone, Type 1
Type of study:
Prognostic_studies
Limits:
Animals
/
Humans
Language:
En
Journal:
Future Med Chem
Year:
2019
Document type:
Article