G protein-coupled receptors : one of the most important drug discovery targets
Author
Source
Journal of King Abdulaziz University : Medical Sciences
Issue
Vol. 25, Issue 2 (30 Jun. 2018), pp.27-35, 9 p.
Publisher
King Abdulaziz University Scientific Publishing Center
Publication Date
2018-06-30
Country of Publication
Saudi Arabia
No. of Pages
9
Main Subjects
Abstract EN
G protein-coupled receptors are considered the most widely investigated drug discovery targets.
They are the largest family of receptors with almost 800 genes in humans.
Diff erent types of ligands can activate these receptors, such as catecholamines, nucleotides, lipids, and gut microbiota, where some ligands could be bitopic.
Nevertheless, some receptors have internal ligands bound to them.
Activated G protein-coupled receptors have complex signaling pathways that are involved in almost all bodily functions.
Furthermore, they constitute a large percentage of Food and Drug Administration marketed drugs and global share of drugs, in addition to a great proportion of drugs currently in clinical trials targeting these receptors.
The approved G protein-coupled receptors targeted drugs and potential drugs are involved in the management of many diseases including cancer, infl ammatory diseases, diabetes mellitus, hypertension, obesity, pain, and diseases of the central nervous system.
On the other hand, only 10% of G protein-coupled receptors are targeted.
Diff erent pharmacological approaches have been considered in drug discovery of these receptors including polypharmacology, allosteric modulators, biased agonism, tethered agonism, and pharmacogenomics.
Advances in the technologies are promising to help in the discovery of new targets.
Thus, the aim of this review is to discuss the importance of G protein-coupled receptors as drug discovery targets.
American Psychological Association (APA)
Andijani, Yusra Salih H.. 2018. G protein-coupled receptors : one of the most important drug discovery targets. Journal of King Abdulaziz University : Medical Sciences،Vol. 25, no. 2, pp.27-35.
https://search.emarefa.net/detail/BIM-887724
Modern Language Association (MLA)
Andijani, Yusra Salih H.. G protein-coupled receptors : one of the most important drug discovery targets. Journal of King Abdulaziz University : Medical Sciences Vol. 25, no. 2 (2018), pp.27-35.
https://search.emarefa.net/detail/BIM-887724
American Medical Association (AMA)
Andijani, Yusra Salih H.. G protein-coupled receptors : one of the most important drug discovery targets. Journal of King Abdulaziz University : Medical Sciences. 2018. Vol. 25, no. 2, pp.27-35.
https://search.emarefa.net/detail/BIM-887724
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references : p. 32-34
Record ID
BIM-887724