Angiotensis-based peptides as AT2R agonists

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Abstract

This chapter discusses the effects of both endogenous and synthetic peptides in the context of use as AT2R agonists. Historically, -peptides have often been disregarded for therapeutic development due to their poor in vivo stability and lack of receptor subtype selectivity. However, recent developments in drug delivery technologies and advanced knowledge of chemical modifications to alter -pharmacological characteristics have reinvigorated the field of peptide therapeutics. Indeed, peptides have been frequently utilized as the basis of drug design due to beneficial properties such as relatively cheap and simple synthesis, high-affinity binding at cognate receptors, and potential for further chemical additions and substitutions. Moreover, considering the still unresolved role of AT2R function in many contexts, -peptide agonists are also likely to remain invaluable experimental tools for the field of AT2R research well into the future. ? 2015 Elsevier Inc. The renin?angiotensin system continues to occupy pharmacologists and physicians alike for well over 50 years, as a result of a number of important recent discoveries, including (i) the discovery of subtype 1 and subtype 2 angiotensin receptors (AT1R and AT2R, respectively) that heralded a new era of drug discovery; (ii) the development and study of nonpeptide AT1R antagonists that led to the concept that AT2R stimulation may contribute to the cardiovascular benefit derived from sartan compounds, at least in preclinical studies; and (iii) academic research that championed the view that AT2R agonists may offer therapeutic benefit for a number of cardiovascular diseases, as discussed at length in this book. This chapter will discuss vascular AT2R effects and their impact on blood pressure (BP).
Original languageEnglish
Title of host publicationThe Protective Arm of the Renin-Angiotensin System
Subtitle of host publicationFunctional Aspects and Therapeutic Implications
EditorsThomas Unger, Ulrike M. Steckelings, Robson A. S. dos Santos
Place of PublicationLondon UK
PublisherElsevier
Pages141 - 147
Number of pages7
Edition1st
ISBN (Print)9780128013649
DOIs
Publication statusPublished - 2015

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