BioCentury | Jun 18, 2019
Distillery Therapeutics

APLN17 analog identified for abdominal aortic aneurysm

...an APLN17 analog that bound its receptor, APLNR, and activated forms of the G proteins GNAI1...
...failure. TARGET/MARKER/PATHWAY: Apelin (APLN); apelin receptor (APLNR; APJ); G protein α inhibiting activity polypeptide 1 (GNAI1...
BioCentury | Oct 13, 2018
Product Development

Trevena goes for MOR than morphine

...more strongly than the other. MOR-induced activation of G protein α inhibiting activity polypeptide 1 (GNAI1...
...at least one study in the literature suggests it only subtly biases MOR signaling toward GNAI1...
...2017 Cell paper from The Scripps Research Institute found that oliceridine isn’t strongly biased to GNAI1...
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

...GNAI1 signaling in psychiatric and neurodegenerative diseases. Chemical synthesis and testing in cell-based assays of GNAI1-induced...
...cAMP accumulation and ARRB2 recruitment of aripiprazole-based D2 receptor agonists identified five compounds that activated GNAI1...
...at the dopamine D2 receptor for probing receptor-induced G protein α inhibiting activity polypeptide 1 (GNAI1...
BioCentury | Sep 15, 2016
Targets & Mechanisms

KOR-recting MS

...mu receptors, kappas cause analgesia and other desired effects by activation of the G protein GNAI1...
...Targets and Compounds ARRB2 - Arrestin β2 DOR ( OPRD1 ) - Opioid receptor δ1 GNAI1...
BioCentury | Sep 1, 2016
Distillery Therapeutics

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

...that bound MOR with a Ki of 1.1 nM and showed biased downstream signaling, activating GNAI1...
...Story). TARGET/MARKER/PATHWAY: μ opioid receptor (MOR; OPRM1 ); G protein α inhibiting activity polypeptide 1 (GNAI1...
BioCentury | Sep 1, 2016
Targets & Mechanisms

Biased against pain

...demonstrated it has orders of magnitude greater potency at signaling via the receptor's G protein, GNAI1...
...to Roth, the field has converged on the notion in the last 15 years that GNAI1...
...can bind the mu receptor and trigger a shift toward a conformation capable of activating GNAI1...
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 hemorrhage in thrombocytopenia patients. In a mouse model of thrombocytopenia, antibody-mediated granulocyte depletion prior to immune-mediated blood vessel injury...
BioCentury | Jan 5, 2012
Distillery Therapeutics

Indication: Musculoskeletal disease

Indication Target/marker/pathway Summary Licensing status Publication and contact information Musculoskeletal disease Muscular atrophy G protein alpha inhibiting activity polypeptide 2 (GNAI2) Mouse and tissue culture studies suggest increasing GNAI2 signaling could help promote muscle repair...
Items per page:
1 - 10 of 11