Biased Receptor Signaling in Drug Discovery

Pharmacological Reviews
Terry Kenakin

Abstract

A great deal of experimental evidence suggests that ligands can stabilize different receptor active states that go on to interact with cellular signaling proteins to form a range of different complexes in varying quantities. In pleiotropically linked receptor systems, this leads to selective activation of some signaling pathways at the expense of others (biased signaling). This article summarizes the current knowledge about the complex components of receptor systems, the evidence that biased signaling is used in natural physiology to fine-tune signaling, and the current thoughts on how this mechanism may be applied to the design of better drugs. Although this is a fairly newly discovered phenomenon, theoretical and experimental data suggest that it is a ubiquitous behavior of ligands and receptors and to be expected. Biased signaling is simple to detect in vitro and there are numerous methods to quantify the effect with scales that can be used to optimize this activity in structure-activity medicinal chemistry studies. At present, the major hurdle in the application of this mechanism to therapeutics is the translation of in vitro bias to in vivo effect; this is because of the numerous factors that can modify measures of bias in...Continue Reading

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Oct 28, 2017·Trends in Pharmacological Sciences·Manuel Grundmann, Evi Kostenis
Dec 12, 2017·Nature Chemical Biology·John D McCorvyBryan L Roth
Jan 20, 2018·Molecular Pharmacology·Terry Kenakin
Feb 18, 2018·Protein & Cell·Vsevolod V GurevichVladimir N Uversky
Mar 28, 2018·British Journal of Pharmacology·Rob HillGraeme Henderson
Apr 13, 2018·Anesthesia and Analgesia·Valerie Le RouzicGavril W Pasternak
Apr 22, 2018·British Journal of Pharmacology·Elizabeth A VecchioLauren T May
May 10, 2018·Trends in Pharmacological Sciences·Vsevolod V Gurevich, Eugenia V Gurevich
Jun 11, 2018·Trends in Pharmacological Sciences·Terry Kenakin, Ryan T Strachan

Citations

Nov 28, 2019·International Journal of Molecular Sciences·Szymon HryhorowiczRyszard Słomski
Jun 9, 2019·Molecular Pharmacology·Alexandra E Conibear, Eamonn Kelly
Aug 29, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Joaquim Azevedo NetoGirolamo Calò
Oct 9, 2019·Molecular Pharmacology·Pawel KozielewiczGunnar Schulte
May 6, 2020·Nature Chemical Biology·Reid H J OlsenRyan T Strachan
Feb 11, 2020·Nature·Reed M SteinMargarita L Dubocovich
Aug 28, 2020·Canadian Journal of Physiology and Pharmacology·Pierre E Thibeault, Rithwik Ramachrandran
Apr 29, 2020·Cells·Jieny GröperUrsula Rescher
Jul 25, 2020·Scientific Reports·Sam R J HoareLloyd J Bridge
Aug 18, 2020·Archives of Pharmacal Research·Kiae Kim, Ka Young Chung
Oct 21, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Anette Kaiser, Irene Coin
Oct 31, 2020·The Journal of Biological Chemistry·Kelly KarlKalina Hristova
Nov 27, 2020·Cellular Signalling·Terry Kenakin
Jan 2, 2021·Cellular Signalling·Michael Ippolito, Jeffrey L Benovic
Jun 14, 2020·European Journal of Pharmacology·Pascal TétreaultPhilippe Sarret
Feb 14, 2021·International Journal of Molecular Sciences·Manuel GrundmannFrank Eitner
Dec 29, 2020·Frontiers in Immunology·Beom K Choi, Hyeon-Woo Lee
Feb 17, 2021·Molecular Psychiatry·Ioannis MantasPer Svenningsson
Feb 11, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Krzysztof Jozwiak, Anita Płazińska
Dec 18, 2020·Pharmacological Reviews·Antonio InserraGabriella Gobbi
Jan 10, 2021·International Journal of Molecular Sciences·Katrin DenzingerMarcel Bermudez
Sep 10, 2020·Journal of Medicinal Chemistry·Salvatore PacificoRemo Guerrini
May 28, 2020·Trends in Neurosciences·Mariana Lemos Duarte, Lakshmi A Devi
Dec 15, 2020·Pharmacology & Therapeutics·Jaana van GastelStuart Maudsley
Feb 20, 2021·Cellular Signalling·H Ongun Onaran, Tommaso Costa
Jan 18, 2021·The Journal of Biological Chemistry·Kelly KarlKalina Hristova
Feb 20, 2021·Behavioural Brain Research·Mélanie VivancosPhilippe Sarret
Sep 20, 2020·Biochimica Et Biophysica Acta. Molecular Basis of Disease·Li-Kun YangYa-Xiong Tao
Apr 10, 2021·Pharmacological Reports : PR·Lucja Kudla, Ryszard Przewlocki
Nov 21, 2020·Journal of Medicinal Chemistry·Gang XingMao-Sheng Cheng
Apr 16, 2021·Frontiers in Neuroscience·Joaquim Azevedo NetoGirolamo Calò

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