Label-free integrative pharmacology on-target of drugs at the β(2)-adrenergic receptor.

Scientific Reports
Ann M FerrieYe Fang

Abstract

We describe a label-free integrative pharmacology on-target (iPOT) method to assess the pharmacology of drugs at the β(2)-adrenergic receptor. This method combines dynamic mass redistribution (DMR) assays using an array of probe molecule-hijacked cells with similarity analysis. The whole cell DMR assays track cell system-based, ligand-directed, and kinetics-dependent biased activities of the drugs, and translates their on-target pharmacology into numerical descriptors which are subject to similarity analysis. We demonstrate that the approach establishes an effective link between the label-free pharmacology and in vivo therapeutic indications of drugs.

References

Dec 9, 1998·Proceedings of the National Academy of Sciences of the United States of America·M B EisenD Botstein
Oct 8, 1999·American Journal of Ophthalmology·S S HayrehM B Zimmerman
Feb 10, 2000·European Heart Journal·J M Cruickshank
Aug 4, 2004·European Heart Journal·José López-SendónUNKNOWN Task ForceOn Beta-Blockers of the European Society of Cardiology
Dec 31, 2004·Proceedings of the National Academy of Sciences of the United States of America·Anton F FliriRobert A Volkmann
May 26, 2005·Nature Reviews. Drug Discovery·Eugene C Butcher
Aug 30, 2005·Obstetrics and Gynecology Clinics of North America·Fung Lam, Pamela Gill
Jun 13, 2006·Biophysical Journal·Ye FangJitendra Balakrishnan
Dec 1, 2007·Nucleic Acids Research·David S WishartMurtaza Hassanali
May 13, 2008·Nature Reviews. Cancer·Klaus Strebhardt, Axel Ullrich
Jul 4, 2008·Bioinformatics·Yiqun CaoThomas Girke
Jul 16, 2008·Science·Monica CampillosPeer Bork
Jul 16, 2008·Nature Chemical Biology·Shawn HoonCorey Nislow
Jul 16, 2008·Naunyn-Schmiedeberg's Archives of Pharmacology·Suneet MehrotraAntoinette MaassenVanDenBrink
Jan 28, 2009·Proceedings of the National Academy of Sciences of the United States of America·Long P NguyenRichard A Bond
Feb 13, 2009·Proceedings of the National Academy of Sciences of the United States of America·Raymond B Penn
Jul 18, 2009·Nature Reviews. Drug Discovery·Terry P Kenakin
Nov 3, 2009·Nature·Michael J KeiserBryan L Roth
Jan 12, 2011·Drug Discovery Today. Technologies·Ye Fang
Mar 2, 2011·Nature Reviews. Drug Discovery·M Paul GleesonJohn Overington
May 5, 2011·PloS One·Vasiliy GoralYe Fang
Apr 1, 2010·Drug Discovery Today. Technologies

❮ Previous
Next ❯

Citations

Apr 25, 2012·Naunyn-Schmiedeberg's Archives of Pharmacology·Huayun Deng, Ye Fang
Mar 19, 2013·BMC Pharmacology & Toxicology·Megan MorseYe Fang
Jun 1, 2012·Expert Opinion on Drug Discovery·Ye Fang
Jan 24, 2013·Journal of Pharmacological and Toxicological Methods·Ye Fang
Aug 28, 2015·Future Medicinal Chemistry·Ye Fang
Apr 12, 2014·Frontiers in Pharmacology·Ye Fang
Jan 28, 2015·Integrative Biology : Quantitative Biosciences From Nano to Macro·Siddarth ChandrasekaranYe Fang
Apr 1, 2014·Pharmacology Research & Perspectives·Rhonda L CarterDouglas G Tilley
Aug 31, 2018·PloS One·Davide MalfaciniGirolamo Calo'
Aug 31, 2013·Integrative Biology : Quantitative Biosciences From Nano to Macro·Ann M FerrieYe Fang
Mar 28, 2019·Pharmacological Reviews·Terry Kenakin
Jan 20, 2018·Molecular Pharmacology·Terry Kenakin
Aug 14, 2012·Journal of Biomolecular Screening·Sadashiva PaiYe Fang
Dec 12, 2018·Pharmacology Research & Perspectives·Chiara RuzzaGirolamo Calo
May 28, 2021·Scientific Reports·Hamid KeshmiriMauricio Moreno

❮ Previous
Next ❯

Methods Mentioned

BETA
biosensor
biosensors

Software Mentioned

ChemMine

Related Concepts

Related Feeds

Adrenergic Receptors: Trafficking

Adrenergic receptor trafficking is an active physiological process where adrenergic receptors are relocated from one region of the cell to another or from one type of cell to another. Discover the latest research on adrenergic receptor trafficking here.