G protein-coupled estrogen receptor-1: homology modeling approaches and application in screening new GPER-1 modulators.
J Biomol Struct Dyn
; 40(7): 3325-3335, 2022 04.
Article
in En
| MEDLINE
| ID: mdl-33164654
ABSTRACT
G protein-coupled receptors (GPCRs) belong to the largest family of protein targets comprising over 800 members in which at least 500 members are the therapeutic targets. Among the GPCRs, G protein-coupled estrogen receptor-1 (GPER-1) has shown to have the ability in estrogen signaling. As GPER-1 plays a critical role in several physiological responses, GPER-1 has been considered as a potential therapeutic target to treat estrogen-based cancers and other non-communicable diseases. However, the progress in the understanding of GPER-1 structure and function is relatively slow due to the availability of a only a few selective GPER-1 modulators. As with many GPCRs, the X-ray crystal structure of GPER-1 is yet to be resolved and thus has led the researchers to search for new GPER-1 modulators using homology models of GPER-1. In this review, we aim to summarize various approaches used in the generation of GPER-1 homology model and their applications that have resulted in new GPER-1 ligands.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Receptors, Estrogen
/
Receptors, G-Protein-Coupled
Type of study:
Diagnostic_studies
/
Screening_studies
Language:
En
Journal:
J Biomol Struct Dyn
Year:
2022
Document type:
Article
Affiliation country:
Malaysia