BioCentury | Jun 6, 2020
Translation in Brief

Engineered bacteria for targeted bacterial killing; plus Cas12a base editors, base editing to restore hearing and more

Targeted delivery of antibacterial toxins University of Washington researchers have co-opted a bacterial secretion system to enable killing of select bacterial species. They d escribed in Cell Host & Microbe how they programmed bacteria with...
BioCentury | Feb 7, 2020
Translation in Brief

Gilead’s remdesivir vs. 2019-nCov in cells; plus Syndax, Syntrix and Max Planck

...Syntrix found that even at supratherapeutic concentrations, desmetramadol -- a MOR agonist -- avoids the ARRB2...
...p ublished in Nature Communications in January. Targets APOE4 - Apolipoprotein E (APOE) epsilon 4 ARRB2...
BioCentury | Oct 13, 2018
Product Development

Trevena goes for MOR than morphine

FDA’s Anesthetic and Analgesic Drug Products Advisory Committee meeting on pain candidate oliceridine from Trevena Inc. gave the agency little reason to reverse its skepticism about the molecule’s benefits and risks. But it did leave...
BioCentury | Feb 16, 2018
Preclinical News

Improved dopamine receptor agonists for Parkinson’s

A study published in Nature Communications showed that non-catechol dopamine D1 receptor agonists reduced receptor desensitization, suggesting the compounds could help treat Parkinson's disease better than available dopamine replacement therapies. Marketed D1 receptor selective agonists...
BioCentury | Jan 17, 2018
Distillery Techniques

Drug platforms

...identified hydrophobic interactions with residues W287 and Y312 that mediate the induction of arrestin β2 (ARRB2...
...cell lines of the designed KOR agonists, yielded a compound that decreased activation of the ARRB2...
BioCentury | Jan 9, 2018
Preclinical News

Selective kappa opioid receptor agonist could dial out side effects

...effect liabilities such as dysphoria, sedation and hallucination, which are caused by induction of arrestin beta 2 (ARRB2...
...and active states and define residues that mediate specific features of its activity, such as ARRB2...
...with additional patents expected in the "near future." Jennie Walters University of North Carolina at Chapel Hill Arrestin beta 2 (ARRB2) Kappa...
BioCentury | Jan 3, 2017
Distillery Therapeutics

Neurology; dermatology

...KOR agonists. A previously reported triazole-based, biased KOR agonist activated KOR-dependent G-protein signaling and KOR-dependent ARRB2...
...I testing to treat uremic pruritus. TARGET/MARKER/PATHWAY: κ opioid receptor (KOR; OPRK1); arrestin β 2 (ARRB2...
BioCentury | Nov 15, 2016
Distillery Techniques

Chemistry

...compounds Aripiprazole-based biased agonists at the dopamine D2 receptor that activate GNAI1 but not arrestin beta 2 (ARRB2...
...and neurodegenerative diseases. Chemical synthesis and testing in cell-based assays of GNAI1-induced cAMP accumulation and ARRB2...
...email: bryan_roth@med.unc.edu Selina Koch Icahn School of Medicine at Mount Sinai University of North Carolina at Chapel Hill Arrestin beta 2 (ARRB2) Dopamine...
BioCentury | Sep 15, 2016
Targets & Mechanisms

KOR-recting MS

...by activation of the G protein GNAI1 , and dysphoria via activation of the β-arrestin, ARRB2...
...Francisco, Calif. University of North Carolina at Chapel Hill, Chapel Hill, N.C. Targets and Compounds ARRB2...
BioCentury | Sep 1, 2016
Distillery Therapeutics

Therapeutics: µ opioid receptor (MOR; OPRM1); G protein α inhibiting activity polypeptide 1 (GNAI1)

...with an EC50 of 4.6 nM and producing no detectable activation of arrestin β2 ( ARRB2...
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