The pharmacology and function of receptors for short-chain fatty acids [PDF]
, 2015 Despite some blockbuster G protein–coupled receptor (GPCR) drugs, only a small fraction (∼15%) of the more than 390 nonodorant GPCRs have been successfully targeted by the pharmaceutical industry.
Bolognini, Daniele +3 more
core +1 more source
G protein-coupled receptors not currently in the spotlight: free fatty acid receptor 2 and GPR35 [PDF]
, 2017 It is widely appreciated that G protein-coupled receptors have been the most successfully exploited class of targets for the development of small molecule medicines. Despite this, to date, less than 15% of the non-olfactory G protein-coupled receptors in
Milligan, Graeme
core +1 more source
Monoclonal anti-β1-adrenergic receptor antibodies activate G protein signaling in the absence of β-arrestin recruitment [PDF]
, 2013 Thermostabilized G protein-coupled receptors used as antigens for in vivo immunization have resulted in the generation of functional agonistic anti-β1-adrenergic (β1AR) receptor monoclonal antibodies (mAbs).
Ali Jazayeri +18 more
core +2 more sources
Extracellular loops 2 and 3 of the calcitonin receptor selectively modify agonist binding and efficacy. [PDF]
, 2018 Class B peptide hormone GPCRs are targets for the treatment of major chronic disease. Peptide ligands of these receptors display biased agonism and this may provide future therapeutic advantage.
Andreassen +70 more
core +1 more source
Journal of Pharmacological Sciences, 2013 .: β-Arrestin-biased agonists are a new class of drugs with promising therapeutic effects. The molecular mechanisms of β-arrestin-biased agonists are still not completely identified.
Islam A.A.E-H. Ibrahim +2 more
doaj +1 more source
7‑hydroxymitragynine is an active metabolite of mitragynine and a key mediator of its analgesic effects [PDF]
, 2019 Mitragynina speciosa, more commonly known as kratom, is a plant native to Southeast Asia, the leaves of which have been used traditionally as a stimulant, analgesic, and treatment for opioid addiction.
Ansonoff, Michael +12 more
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Cell Reports, 2019 Summary: Desensitization, signaling, and trafficking of G-protein-coupled receptors (GPCRs) are critically regulated by multifunctional adaptor proteins, β-arrestins (βarrs).
Eshan Ghosh +18 more
doaj +1 more source
Agonist Effects of Propranolol on Non-Tumor Human Breast Cells
Cells, 2020 The β-blocker propranolol (PROP) has been proposed as a repurposed treatment for breast cancer. The similarity of action between β-agonists and antagonists found on breast cells encouraged us to compare PROP and isoproterenol (ISO, agonist) signaling ...
Lucía Gargiulo +7 more
doaj +1 more source
A Single Dose-Escalation Study to Evaluate the Safety and Pharmacokinetics of Orally Administered Des-Aspartate Angiotensin I in Healthy Subjects [PDF]
, 2016 Des-aspartate-angiotensin I (DAA-I) is an endogenous angiotensin peptide and a prototype angiotensin receptor agonist (ARA). It acts on the angiotensin AT(1) receptor and antagonises the deleterious actions of angiotensin II.
Balram Chowbay +4 more
core +1 more source
Arrestin-biased AT1R agonism induces acute catecholamine secretion through TRPC3 coupling
Nature Communications, 2017 Angiotensin II type 1 receptor (AT1R)-mediated acute catecholamine release is modulated by β-arrestin. Here the authors show that β-arrestin-1 recruits the Ca2+channel TRPC3 and the PLCγ to the AT1R-β-arrestin complex, triggering G protein-independent ...
Chun-Hua Liu +26 more
doaj +1 more source