A biased agonist at immunometabolic receptor GPR84 causes distinct functional effects in macrophages.
Sign Up to like & getrecommendations! Published in 2019 at "ACS chemical biology"
DOI: 10.1021/acschembio.9b00533
Abstract: GPR84 is an orphan G protein-coupled receptor which is expressed on immune cells and implicated in several inflammatory diseases. The validation of GPR84 as a therapeutic target is hindered by the narrow range of available… read more here.
Keywords: biased agonist; agonist immunometabolic; receptor gpr84; gpr84 ... See more keywords
Ang-(1-7) is an endogenous β-arrestin-biased agonist of the AT1 receptor with protective action in cardiac hypertrophy
Sign Up to like & getrecommendations! Published in 2017 at "Scientific Reports"
DOI: 10.1038/s41598-017-12074-3
Abstract: The renin-angiotensin system (RAS) plays a key role in the control of vasoconstriction as well as sodium and fluid retention mediated mainly by angiotensin (Ang) II acting at the AT1 receptor (AT1R). Ang-(1-7) is another… read more here.
Keywords: biased agonist; endogenous arrestin; hypertrophy; ang ... See more keywords
Cortical 5-hydroxytryptamine 1A receptor biased agonist, NLX-101, displays rapid-acting antidepressant-like properties in the rat chronic mild stress model
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Psychopharmacology"
DOI: 10.1177/0269881119860666
Abstract: Background: NLX-101 (also known as F15599) is a highly selective and efficacious ‘biased’ agonist at cortical 5-hydroxytryptamine 1A (5-HT1A) heteroreceptors. In rodents, it possesses marked antidepressant-like activity, potently and completely abolishing immobility in the forced… read more here.
Keywords: biased agonist; cortical hydroxytryptamine; model; rat chronic ... See more keywords
NKTR-214 (CD122-biased agonist) plus nivolumab in patients with advanced solid tumors: Preliminary phase 1/2 results of PIVOT.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of Clinical Oncology"
DOI: 10.1200/jco.2018.36.15_suppl.3006
Abstract: 3006Background: PIVOT is an ongoing, open-label, phase 1/2 study of NKTR-214 (214; CD122-biased agonist) plus PD-1 inhibitor nivolumab (N) in patients (pts) with advanced cancers (MEL, RCC, NSCLC, TNBC, and UC). 214 monotherapy increases newly… read more here.
Keywords: biased agonist; nktr 214; nivolumab patients; agonist plus ... See more keywords
Molecular Signaling Mechanisms for the Antidepressant Effects of NLX-101, a Selective Cortical 5-HT1A Receptor Biased Agonist
Sign Up to like & getrecommendations! Published in 2022 at "Pharmaceuticals"
DOI: 10.3390/ph15030337
Abstract: Depression is the most prevalent of the mental illnesses and serotonin (5-hydroxytryptamine, 5-HT) is considered to be the major neurotransmitter involved in its etiology and treatment. In this context, 5-HT1A receptors have attracted interest as… read more here.
Keywords: ht1a; signaling mechanisms; antidepressant effects; molecular signaling ... See more keywords