Current Trends in GPCR Allostery
| Autor: | Khuraijam Dhanachandra Singh, Sadashiva S. Karnik |
|---|---|
| Rok vydání: | 2021 |
| Předmět: |
0303 health sciences
Physiology Chemistry 030310 physiology Drug target Allosteric regulation Biophysics Endogeny Receptor signaling Cell Biology Ligands Receptors G-Protein-Coupled GPCR Signaling Food and drug administration 03 medical and health sciences Allosteric Regulation Receptor Neuroscience Signal Transduction 030304 developmental biology G protein-coupled receptor |
| Zdroj: | The Journal of Membrane Biology. 254:293-300 |
| ISSN: | 1432-1424 0022-2631 |
| Popis: | GPCRs remain the most important drug target comprising ~ 34% of the Food and Drug Administration (FDA)-approved drugs. In modern pharmacology of GPCRs, modulating receptor signaling based on requirement of a specific disorder is of immense interest. Classical drugs targeting orthosteric sites in GPCRs completely block the binding of endogenous ligand and consequently inhibit all important signals from a GPCR. Some of many signals elicited by the endogenous ligands may play vital role and inhibiting these may also cause severe side effects in the long run. However, allosteric drugs can modulate GPCR signaling without blocking the endogenous ligand binding. Therefore, allosteric drugs can maintain beneficial signaling of the receptor and prevent unwanted side effects. In this chapter, we will discuss GPCR crystal structures solved with allosteric ligands, advantages of allosteric drugs, and allosteric drugs which are in clinical use or trials. |
| Databáze: | OpenAIRE |
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