Next Article in Journal
Histone Deacetylase Inhibitors in Clinical Studies as Templates for New Anticancer Agents
Next Article in Special Issue
Synthesis, Antiproliferative Activity and Molecular Properties Predictions of Galloyl Derivatives
Previous Article in Journal
Synthesis, Larvicidal Activities and Antifungal Activities of Novel Chlorantraniliprole Derivatives and Their Target in the Ryanodine Receptor
Previous Article in Special Issue
Facile Access to Unnatural Dipeptide-Alcohols Based on cis-2,5-Disubstituted Pyrrolidines
Article Menu

Export Article

Open AccessReview
Molecules 2015, 20(3), 3868-3897; doi:10.3390/molecules20033868

Rational Drug Design and Synthesis of Molecules Targeting the Angiotensin II Type 1 and Type 2 Receptors

1
Department of Chemistry, National and Kapodistrian University of Athens, Panepistimiopolis Zografou 15771, Greece
2
Department of Chemistry, University of Ioannina, Ioannina 45110, Greece
*
Author to whom correspondence should be addressed.
Academic Editor: Panayiotis Koutentis
Received: 18 December 2014 / Revised: 6 February 2015 / Accepted: 15 February 2015 / Published: 2 March 2015

Abstract

The angiotensin II (Ang II) type 1 and type 2 receptors (AT1R and AT2R) orchestrate an array of biological processes that regulate human health. Aberrant function of these receptors triggers pathophysiological responses that can ultimately lead to death. Therefore, it is important to design and synthesize compounds that affect beneficially these two receptors. Cardiovascular disease, which is attributed to the overactivation of the vasoactive peptide hormone Αng II, can now be treated with commercial AT1R antagonists. Herein, recent achievements in rational drug design and synthesis of molecules acting on the two AT receptors are reviewed. Quantitative structure activity relationships (QSAR) and molecular modeling on the two receptors aim to assist the search for new active compounds. As AT1R and AT2R are GPCRs and drug action is localized in the transmembrane region the role of membrane bilayers is exploited. The future perspectives in this field are outlined. Tremendous progress in the field is expected if the two receptors are crystallized, as this will assist the structure based screening of the chemical space and lead to new potent therapeutic agents in cardiovascular and other diseases. View Full-Text
Keywords: angiotensin II receptors; AT1R; AT2R; rational drug design; synthesis; molecular modeling; drug-membrane interactions angiotensin II receptors; AT1R; AT2R; rational drug design; synthesis; molecular modeling; drug-membrane interactions
Figures

Figure 1

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

Scifeed alert for new publications

Never miss any articles matching your research from any publisher
  • Get alerts for new papers matching your research
  • Find out the new papers from selected authors
  • Updated daily for 49'000+ journals and 6000+ publishers
  • Define your Scifeed now

SciFeed Share & Cite This Article

MDPI and ACS Style

Kellici, T.F.; Tzakos, A.G.; Mavromoustakos, T. Rational Drug Design and Synthesis of Molecules Targeting the Angiotensin II Type 1 and Type 2 Receptors. Molecules 2015, 20, 3868-3897.

Show more citation formats Show less citations formats

Related Articles

Article Metrics

Article Access Statistics

1

Comments

[Return to top]

Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top