Literature DB >> 7297703

Conformational changes and drug action.

A S Burgen.   

Abstract

Conformational changes induced or selected by drugs in receptors may be coupled to second sites on receptor molecules giving negative or positive cooperative binding. The structure-activity relationships may be changed depending on the predominant conformation. Some conformational changes can be identified by nuclear magnetic resonance spectroscopy. Conformational coupling between subunits is complex and provides a mechanism for modulation of receptor affinity.

Mesh:

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Year:  1981        PMID: 7297703

Source DB:  PubMed          Journal:  Fed Proc        ISSN: 0014-9446


  30 in total

1.  Deciphering biased-agonism complexity reveals a new active AT1 receptor entity.

Authors:  Aude Saulière; Morgane Bellot; Hervé Paris; Colette Denis; Frédéric Finana; Jonas T Hansen; Marie-Françoise Altié; Marie-Hélène Seguelas; Atul Pathak; Jakob L Hansen; Jean-Michel Sénard; Céline Galés
Journal:  Nat Chem Biol       Date:  2012-05-27       Impact factor: 15.040

Review 2.  Seven transmembrane receptors as shapeshifting proteins: the impact of allosteric modulation and functional selectivity on new drug discovery.

Authors:  Terry Kenakin; Laurence J Miller
Journal:  Pharmacol Rev       Date:  2010-04-14       Impact factor: 25.468

Review 3.  The mass action equation in pharmacology.

Authors:  Terry Kenakin
Journal:  Br J Clin Pharmacol       Date:  2015-12-21       Impact factor: 4.335

Review 4.  Protein Allostery and Conformational Dynamics.

Authors:  Jingjing Guo; Huan-Xiang Zhou
Journal:  Chem Rev       Date:  2016-02-15       Impact factor: 60.622

Review 5.  In silico pharmacology for drug discovery: methods for virtual ligand screening and profiling.

Authors:  S Ekins; J Mestres; B Testa
Journal:  Br J Pharmacol       Date:  2007-06-04       Impact factor: 8.739

Review 6.  Cellular assays as portals to seven-transmembrane receptor-based drug discovery.

Authors:  Terry P Kenakin
Journal:  Nat Rev Drug Discov       Date:  2009-07-17       Impact factor: 84.694

Review 7.  The role of G proteins in transmembrane signalling.

Authors:  C W Taylor
Journal:  Biochem J       Date:  1990-11-15       Impact factor: 3.857

8.  Activation of muscarinic acetylcholine receptors via their allosteric binding sites.

Authors:  J Jakubík; L Bacáková; V Lisá; E E el-Fakahany; S Tucek
Journal:  Proc Natl Acad Sci U S A       Date:  1996-08-06       Impact factor: 11.205

9.  Conformational Dynamics in Extended RGD-Containing Peptides.

Authors:  William R Lindemann; Alexander J Mijalis; José L Alonso; Peter P Borbat; Jack H Freed; M Amin Arnaout; Bradley L Pentelute; Julia H Ortony
Journal:  Biomacromolecules       Date:  2020-06-16       Impact factor: 6.988

10.  Allosteric theory: taking therapeutic advantage of the malleable nature of GPCRs.

Authors:  Terry Kenakin
Journal:  Curr Neuropharmacol       Date:  2007-09       Impact factor: 7.363

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