Biased Ligands. Better Drugs.

Biased Ligand Publications

Poster - TRV250 preclinical studies

TRV250: a novel biased ligand at the delta receptor for the potential treatment of migraine

Poster - TRV734 Phase 1 clinical studies

TRV734, a G Protein-biased Ligand of the µ-opioid Receptor, Demonstrates Oral Bioavailability, Displays Predictable Pharmacokinetics and Pharmacodynamics, and Provides Analgesia in Healthy Adults

Poster - TRV734 Phase 1 formulation study

Formulation and Food Effect Studies of TRV734, an Oral, G Protein-biased Ligand of the µ-opioid Receptor

Review - Biased Ligand research

Biased ligands: pathway validation for novel GPCR therapeutics. Current Opinions in Pharmacology 2014 16: 108-115.

Poster - TRV734 - An orally available mu-opioid receptor biased ligand is analgesic with reduced constipation in rodents

This poster introduces TRV734, a G protein-biased mu-opioid receptor ligand that is analgesic with improved gastrointestinal effects compared to morphine and oxycodone in rodents. TRV734 displays promising pharmacokinetics in non-human primates; together these data suggest that oral TRV734 may deliver powerful analgesia with better tolerability than currently used oral opioids for acute and chronic pain.

Article - Signalling bias in new drug discovery: detection, quantification and therapeutic impact

Nat Rev Drug Discov. 2013 Mar;12(3):205-16

Article - Discovery of β-arrestin-biased dopamine D2 ligands for probing signal transduction pathways essential for antipsychotic efficacy

Proc Natl Acad Sci U S A. 2011 Nov 8;108(45):18488-93

Review - Introduction to Novel Aspects of Cardiovascular GPCR Signaling

AHA Journals Free Article

Article - Structural Features for Functional Selectivity at Serotonin Receptors

Science. 2013 Mar 21 (online)

Article - The quantification of ligand bias, a collaboration with R. Lefkowitz

Quantifying ligand bias at seven-transmembrane receptors. Mol Pharmacol. 2011 Sep. PubMed Central PMCID: PMC3164332

Article - A review of biased ligands

β-arrestin-biased ligands at seven-transmembrane receptors. Trends Pharmacol Sci. 2007 Aug

Article - A comprehensive review of β-arrestin functions

β-arrestins and cell signaling. Annu Rev Physiol. 2007

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