The β-arrestin-Biased Ligand TRV120023 Inhibits Angiotensin II-Induced Cardiac Hypertrophy While Preserving Enhanced Myofilament Response to Calcium
TRV027, a β-arrestin biased ligand at the angiotensin 2 type 1 receptor, produces rapid, reversible changes in hemodynamics in patients with stable systolic heart failure. Presented at 2013 American College of Cardiology meeting
GPCR biased ligands as novel heart failure therapeutics. Article in Press. Available online March 15th 2013
First human dosing experience with TRV027, a novel therapy for acute heart failure. Presented at 2012 Heart Failure of America Society meeting
β-Arrestin-biased AT1R stimulation promotes cell survival during acute cardiac injury. Am J Physiol Heart Circ Physiol 303:H1001-H1010, 2012. First published 10 August 2012
Cardiorenal Actions of TRV120027, a Novel, β-Arrestin-Biased Ligand at the Angiotensin II Type I Receptor, in Healthy and Heart Failure Canines: A Novel Therapeutic Strategy for Acute Heart Failure. Circ Heart Fail. 2011 Aug. PubMed PMID: 21835984.
Biased ligands for better cardiovascular drugs:dissecting G protein-coupled receptor pharmacology. Circ Res. 2011 Jul. PubMed PMID: 21737816.
Selectively engaging Beta-arrestins at the angiotensin II type 1 receptor reduces blood pressure and increases cardiac performance. J Pharmacol Exp Ther 2010 Dec.
TRV120027, a Beta-arrestin biased ligand at the angiotensin II type 1 receptor, produces unique pharmacology and is a novel potential therapy for heart failure. Presented at the 2010 Heart Failure of Society of America meeting
Cardiorenal Actions of TRV120027, a Novel, Beta-Arrestin-Biased Ligand at the Angiotensin II Type I Receptor, in Healthy and Heart Failure Canines: A Novel Therapeutic Strategy for Acute Heart Failure
A G Protein-Biased Ligand at the mu opioid Receptor is Potently Analgesic with Reduced Gastrointestinal and Respiratory Dysfunction Compared with Morphine. J Pharmacol Exp Ther 344:708-717, March 2013.
First human dosing experience with TRV130, a G protein biased ligand at the mu opioid receptor. Presented at 2013 American Academy of Neurology meeting
A G protein biased mu opioid receptor ligand elicits potent analgesia but reduced constipation & respiratory depression compared to morphine in rodents. Presented at the 2012 American Association of Pain Medicine Meeting
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.
Nat Rev Drug Discov. 2013 Mar;12(3):205-16
Proc Natl Acad Sci U S A. 2011 Nov 8;108(45):18488-93
AHA Journals Free Article
Science. 2013 Mar 21 (online)
Quantifying ligand bias at seven-transmembrane receptors. Mol Pharmacol. 2011 Sep. PubMed Central PMCID: PMC3164332
β-arrestin-biased ligands at seven-transmembrane receptors. Trends Pharmacol Sci. 2007 Aug
β-arrestins and cell signaling. Annu Rev Physiol. 2007
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