G protein-coupled estrogen receptor-1: homology modeling approaches and application in screening new GPER-1 modulators

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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.

Original languageEnglish
Pages (from-to)3325-3335
Number of pages11
JournalJournal of Biomolecular Structure and Dynamics
Issue number7
Publication statusPublished - 2022


  • estrogen
  • GPER-1
  • homology modeling
  • modulators
  • molecular docking

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