Probing GPCR Dimerization Using Peptides.

Autor:	Farooq Z; Centre for Endocrinology, William Harvey Research Institute, Bart's and The London School of Medicine and Dentistry, Queen Mary University of London, Charterhouse Square, London, United Kingdom.; Department of Chemistry, School of Physical and Chemical Sciences, Queen Mary University of London, Mile End Road, London, United Kingdom., Howell LA; Department of Chemistry, School of Physical and Chemical Sciences, Queen Mary University of London, Mile End Road, London, United Kingdom., McCormick PJ; Centre for Endocrinology, William Harvey Research Institute, Bart's and The London School of Medicine and Dentistry, Queen Mary University of London, Charterhouse Square, London, United Kingdom.
Jazyk:	angličtina
Zdroj:	Frontiers in endocrinology [Front Endocrinol (Lausanne)] 2022 Jul 14; Vol. 13, pp. 843770. Date of Electronic Publication: 2022 Jul 14 (Print Publication: 2022).
DOI:	10.3389/fendo.2022.843770
Abstrakt:	G protein-coupled receptors (GPCRs) are the largest class of membrane proteins and the most common and extensively studied pharmacological target. Numerous studies over the last decade have confirmed that GPCRs do not only exist and function in their monomeric form but in fact, have the ability to form dimers or higher order oligomers with other GPCRs, as well as other classes of receptors. GPCR oligomers have become increasingly attractive to investigate as they have the ability to modulate the pharmacological responses of the receptors which in turn, could have important functional roles in diseases, such as cancer and several neurological & neuropsychiatric disorders. Despite the growing evidence in the field of GPCR oligomerisation, the lack of structural information, as well as targeting the 'undruggable' protein-protein interactions (PPIs) involved in these complexes, has presented difficulties. Outside the field of GPCRs, targeting PPIs has been widely studied, with a variety of techniques being investigated; from small-molecule inhibitors to disrupting peptides. In this review, we will demonstrate several physiologically relevant GPCR dimers and discuss an array of strategies and techniques that can be employed when targeting these complexes, as well as provide ideas for future development. Competing Interests: The authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest. (Copyright © 2022 Farooq, Howell and McCormick.)
Databáze:	MEDLINE
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