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Cholesterol as a Key Molecule That Regulates TRPV1 Channel Function

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Direct Mechanisms in Cholesterol Modulation of Protein Function

Part of the book series: Advances in Experimental Medicine and Biology ((AEMB,volume 1135))

Abstract

Cholesterol is the one of the major constituents of cell membranes providing these structures with a certain degree of rigidity. Proteins, such as ion channels, are molecules inserted in cell membranes and their activity is regulated by cholesterol and other molecules of a lipidic nature present in them. The molecular mechanisms underlying the regulation of ion channels by lipids and similar molecules have been an object of study for several years. A little over two decades ago, the first mammalian member of the Transient Receptor Potential (TRP) family of ion channels was cloned. This protein, the TRPV1 channel, was shown to integrate several types of noxious signals in sensory neurons and to participate in processes associated to the generation of pain. Thus, TRPV1 has become the target of intense research directed towards finding potential inhibitors of its activity in an effort to control pain. To date, several activators and positive modulators of the activity of TRPV1 have been described. However, very few naturally-occurring inhibitors are known. An endogenously-produced molecule that inhibits the activity of TRPV1 is cholesterol. This chapter focuses on describing the mechanisms by which the activity of TRPV1 can be regulated by this sterol.

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Acknowledgments

This work was supported by grants from Dirección General de Asuntos del Personal Académico (DGAPA)-Programa de Apoyo a Proyectos de Investigación e Innovación Tecnológica (PAPIIT) IN206819 and by Estímulos a Investigaciones Médicas Miguel Alemán Valdés to S.LM.L. and Consejo Nacional de Ciencia y Tecnología (CONACyT) A1-S-8760, grant from Fronteras en la Ciencia No. 77 from CONACyT and DGAPA-PAPIIT IN200717 to T.R.

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Authors and Affiliations

  1. Departamento de Neurociencia Cognitiva, Instituto de Fisiología Celular, Universidad Nacional Autónoma de México, Coyoacan, México City, México

    Sara L. Morales-Lázaro & Tamara Rosenbaum

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  1. Sara L. Morales-Lázaro
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  2. Tamara Rosenbaum
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Correspondence to Sara L. Morales-Lázaro or Tamara Rosenbaum .

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Editors and Affiliations

  1. Department of Chemistry, University of Illinois, Chicago, IL, USA

    Avia Rosenhouse-Dantsker

  2. Department of Pharmacology, The University of Tennessee HSC, Memphis, TN, USA

    Anna N. Bukiya

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Morales-Lázaro, S.L., Rosenbaum, T. (2019). Cholesterol as a Key Molecule That Regulates TRPV1 Channel Function. In: Rosenhouse-Dantsker, A., Bukiya, A. (eds) Direct Mechanisms in Cholesterol Modulation of Protein Function. Advances in Experimental Medicine and Biology, vol 1135. Springer, Cham. https://doi.org/10.1007/978-3-030-14265-0_6

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