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Special Issue "New Breakthroughs in GPCR Structure, Function and Their Impact on Drug Discovery"

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: 31 October 2019

Special Issue Editor

Guest Editor
Prof. Dr. Oliver Zerbe

Department of Chemistry, University of Zurich, Zurich, Switzerland
Website | E-Mail
Interests: G-protein coupled receptors; protein folding; metallothioneins; repeat proteins

Special Issue Information

Dear Colleagues,

G-protein coupled receptors are involved in binding a very large number of pharmacologically relevant drugs. Accordingly, much interest in understanding their structure has led to an ever-accelerating rate of new structures being determined. The first structure of a GPCR, bovine rhodopsin, was published by the Palczewski lab in 2000, and was followed by many more studies by others, culminating in the Nobel Prize awards to Lefkowitz and Kobilka.

Phenomena such as receptor activation and deactivation, the role of receptor oligomerization, receptor desensitization, biased signalling, the importance of receptor modulation by allosteric drugs etc. have been intensively investigated over last two decades.

Interest in understanding any of the above-mentioned aspects of GPCR structures has triggered important methodological developments in time-resolved crystallography, in NMR techniques, in cryoEM and in MD techniques, to mention just some of the techniques involved. It has also been accompanied by important refinements of biochemical procedures for expression in a variety of hosts and purification strategies.

This Special Issue of Molecules is intended for all those researchers who study structural or functional aspects of GPCRs, or help to refine methods that are important for improving our understanding of drug–GPCR interactions in order to produce novel and better GPCR-interacting drugs.

Prof. Dr. Oliver Zerbe
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All papers will be peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 1800 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.


  • GPCR drug interactions
  • Receptor activation and desensitization
  • Allosteric effects
  • Biased signaling
  • Receptor stabilization
  • GPCR dynamics
  • GPCR oligomerization

Published Papers

This special issue is now open for submission.
Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
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