Operational models of allosteric modulation : caution is needed
Giraldo, Jesús (Universitat Autònoma de Barcelona. Institut de Neurociències)

Date:	2015
Abstract:	The operational model of allosteric modulation and allosteric agonism [1-5] is being used routinely to assess the functional effects of allosteric modulators. Because the meaning of parameters and concepts often loses precision after extensive use, it may be timely to revise some particularities of the model to preclude possible misinterpretations. To do so, I will use the equation for the model as expressed in [4]:where Em is the maximum effect of the system; n, a parameter related with the slope of the curves; [A] and [B], the concentrations of the agonist A and the allosteric modulator B, respectively; τA and τB, the operational efficacies of A and B, respectively; KA and KB, the dissociation constants of A and B, respectively; and α and β, the cooperativity parameters governing binding and function, respectively.
Rights:	Aquest document està subjecte a una llicència d'ús Creative Commons. Es permet la reproducció total o parcial i la comunicació pública de l'obra, sempre que no sigui amb finalitats comercials, i sempre que es reconegui l'autoria de l'obra original. No es permet la creació d'obres derivades.
Language:	Anglès
Document:	Article ; recerca ; Versió acceptada per publicar
Published in:	Trends in pharmacological sciences, Vol. 36, Issue 1 (January 2015) , p. 1-2, ISSN 0165-6147

DOI: 10.1016/j.tips.2014.10.010

Post-print 6 p, 123.3 KB

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Research literature > UAB research groups literature > Research Centres and Groups (research output) > Health sciences and biosciences > Institut de Neurociències (INc)
Articles > Research articles
Articles > Published articles