BioCentury | Jun 18, 2019
Distillery Therapeutics

APLN17 analog identified for abdominal aortic aneurysm

...analog that bound its receptor, APLNR, and activated forms of the G proteins GNAI1 and GNAI2...
...TARGET/MARKER/PATHWAY: Apelin (APLN); apelin receptor (APLNR; APJ); G protein α inhibiting activity polypeptide 1 (GNAI1); GNAI2...
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 | Jan 4, 2018
Translation in Brief

New Therapeutic Targets and Biomarkers: December 2017

New Therapeutic Targets and Biomarkers: December 2017 Select top therapeutic targets and biomarkers covered by BioCentury or added to the BCIQ database during December 2017. Therapeutic targets are defined as any protein, gene or other...
BioCentury | Dec 5, 2017
Distillery Techniques

Chemistry

TECHNOLOGY: Tool compounds A GNAI3-based inhibitor could help probe the role of GBA motif-containing proteins in cancer. The inhibitor, which competitively inhibits binding between wild-type GNAI3 and GBA motif proteins, is a GNAI3 variant containing...
BioCentury | Nov 15, 2016
Distillery Techniques

Chemistry

TECHNOLOGY: Tool compounds Aripiprazole-based biased agonists at the dopamine D2 receptor that activate GNAI1 but not arrestin beta 2 (ARRB2) could be useful as probes for D2 receptor-induced GNAI1 signaling in psychiatric and neurodegenerative diseases....
BioCentury | Sep 15, 2016
Targets & Mechanisms

KOR-recting MS

Although the failed Phase II multiple sclerosis trial of Biogen Inc. 's anti-LINGO mAb in June dealt a blow to myelin repair, a slew of compounds acting by different mechanisms lies behind it in clinical...
BioCentury | Sep 1, 2016
Distillery Therapeutics

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

Neurology INDICATION: Pain In vitro and mouse studies identified a biased agonist of MOR signaling that could help treat pain. In silico screening of a library of 3 million small molecules, each in 1.3 million...
BioCentury | Sep 1, 2016
Targets & Mechanisms

Biased against pain

In a departure from the rote tweaking of morphinan structures to find better and safer opioids, an academic collaboration has used a powerful, computer-based screen of more than 3 million molecules to identify a new...
BioCentury | Aug 27, 2015
Distillery Therapeutics

Therapeutics: G protein α inhibiting activity polypeptide 2 (GNAI2)

...Hematology INDICATION: Thrombocytopenia Mouse studies suggest inhibiting GNAI2 or other neutrophil extravasation factors could help prevent...
...treatment. In the mouse model, knockout of GNAI2 decreased lipopolysaccharide-induced lung hemorrhage compared with normal GNAI2...
...a therapeutic that specifically blocks neutrophil extravasation. TARGET/MARKER/PATHWAY: G protein α inhibiting activity polypeptide 2 (GNAI2...
BioCentury | Jan 5, 2012
Distillery Therapeutics

Indication: Musculoskeletal disease

...increasing GNAI2 signaling could help promote muscle repair and regeneration. In mice, a vector expressing Gnai2...
...and abundance compared with a control vector. In human skeletal muscle myotubules, a vector expressing GNAI2...
...whereas a control vector did not. Next steps could include identifying compounds that could increase GNAI2...
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