GPCR structure, function, drug discovery and crystallography: report from Academia-Industry International Conference (UK Royal Society) Chicheley Hall, 1-2 September 2014

Naunyn-Schmiedeberg's Archives of Pharmacology
Alexander HeifetzPhilip C Biggin

Abstract

G-protein coupled receptors (GPCRs) are the targets of over half of all prescribed drugs today. The UniProt database has records for about 800 proteins classified as GPCRs, but drugs have only been developed against 50 of these. Thus, there is huge potential in terms of the number of targets for new therapies to be designed. Several breakthroughs in GPCRs biased pharmacology, structural biology, modelling and scoring have resulted in a resurgence of interest in GPCRs as drug targets. Therefore, an international conference, sponsored by the Royal Society, with world-renowned researchers from industry and academia was recently held to discuss recent progress and highlight key areas of future research needed to accelerate GPCR drug discovery. Several key points emerged. Firstly, structures for all three major classes of GPCRs have now been solved and there is increasing coverage across the GPCR phylogenetic tree. This is likely to be substantially enhanced with data from x-ray free electron sources as they move beyond proof of concept. Secondly, the concept of biased signalling or functional selectivity is likely to be prevalent in many GPCRs, and this presents exciting new opportunities for selectivity and the control of side eff...Continue Reading

References

May 31, 2002·Expert Opinion on Investigational Drugs·John J Oppenheimer, Thomas B Casale
Apr 3, 2004·Nature Reviews. Drug Discovery·Bryan L RothWesley K Kroeze
Nov 24, 2004·Pharmacology & Therapeutics·Torsten SchönebergKatrin Sangkuhl
Oct 6, 2006·Genome Biology·Eugenia V Gurevich, Vsevolod V Gurevich
Apr 3, 2008·Progress in Medicinal Chemistry·Nathaniel J T Monck, Guy A Kennett
Nov 13, 2008·Molecular Pharmacology·Roland Seifert, Stefan Dove
Apr 14, 2009·Current Biology : CB·Xiufeng SongVsevolod V Gurevich
Apr 21, 2009·Trends in Pharmacological Sciences·Rie NygaardThue W Schwartz
Apr 23, 2009·Journal of Chemical Information and Modeling·Hina PatelValerie J Gillet
Nov 3, 2009·Nature·Michael J KeiserBryan L Roth
Mar 18, 2010·British Journal of Pharmacology·K SalchowM E Bradley
Sep 28, 2010·Annual Review of Pharmacology and Toxicology·John A Allen, Bryan L Roth
Apr 8, 2011·The Journal of Biological Chemistry·Sergey A VishnivetskiyVsevolod V Gurevich
Jun 24, 2011·Nature·Tatsuro ShimamuraSo Iwata
Jul 21, 2011·Nature·Søren G F RasmussenBrian K Kobilka
Oct 11, 2011·Journal of the American Chemical Society·Peter SchmidtkeXavier Barril
Nov 1, 2011·The Journal of Allergy and Clinical Immunology·F Estelle R Simons, Keith J Simons
Feb 24, 2012·Nature·Andrew C KruseBrian K Kobilka
Apr 24, 2012·The Journal of Biological Chemistry·Maya BreitmanVsevolod V Gurevich
Jun 6, 2012·Cellular Signalling·Vsevolod V Gurevich, Eugenia V Gurevich
Jul 13, 2012·Trends in Biochemical Sciences·Christopher G Tate
Jul 13, 2012·The Journal of Biological Chemistry·Luis E GimenezVsevolod V Gurevich
Jul 17, 2012·Science·Wei LiuRaymond C Stevens
Jan 30, 2013·Biochemical Society Transactions·Cassandra KoolePatrick M Sexton
Mar 12, 2013·The Journal of Biological Chemistry·Sergey A VishnivetskiyVsevolod V Gurevich
Mar 13, 2013·Proceedings of the National Academy of Sciences of the United States of America·Denise WoottenPatrick M Sexton
Jun 4, 2013·Journal of Chemical Information and Modeling·Andrea BortolatoJonathan S Mason
Oct 4, 2013·Journal of Medicinal Chemistry·Christofer S TautermannPaola Casarosa
Nov 22, 2013·Journal of Chemical Information and Modeling·Clara D Christ, Thomas Fox
Dec 3, 2013·Handbook of Experimental Pharmacology·Eugenia V Gurevich, Vsevolod V Gurevich

❮ Previous
Next ❯

Citations

Dec 8, 2015·Journal of Chemical Information and Modeling·Alexander HeifetzMike Bodkin
Nov 28, 2015·Naunyn-Schmiedeberg's Archives of Pharmacology·Ursula KösterMartin C Michel
May 10, 2016·Biochimica Et Biophysica Acta. General Subjects·Zehra SayersInes Karmous
May 26, 2016·Naunyn-Schmiedeberg's Archives of Pharmacology·Roland Seifert
Oct 21, 2016·Current Opinion in Pharmacology·Christofer S Tautermann, David E Gloriam
Aug 18, 2016·Journal of Biomolecular Structure & Dynamics·Abigail L EmtageCharles A Laughton
Jan 19, 2018·The Anatomical Record : Advances in Integrative Anatomy and Evolutionary Biology·Nada AbdellahRoeland Buckinx
Mar 27, 2019·Future Medicinal Chemistry·Christian Espinosa-BustosCristian O Salas
Mar 28, 2018·Journal of Computer-aided Molecular Design·Xin ZhangJ Christian Baber
Oct 28, 2019·International Journal of Molecular Sciences·Luis Jaimes Santiago, Ravinder Abrol
Apr 14, 2016·Biochemical Society Transactions·Alexander HeifetzPhilip C Biggin
Oct 13, 2020·Frontiers in Cell and Developmental Biology·Claudia Peregrina, Daniel Del Toro
Jul 2, 2019·Journal of Medicinal Chemistry·Jeffrey J JacksonMikhail Zibinsky

❮ Previous
Next ❯

Methods Mentioned

BETA
surface plasmon resonance
GTPase
pharmacotherapy
chemical modification
NMR

Software Mentioned

Evotec
HGMP
ChEMBL

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.

Related Papers

Nature Reviews. Drug Discovery
Rosamaria Lappano, Marcello Maggiolini
Bioorganic & Medicinal Chemistry Letters
Christofer S Tautermann
Bioorganic & Medicinal Chemistry
Jeremy ShonbergStefan Löber
Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology
Steven D Chang, Michael R Bruchas
© 2021 Meta ULC. All rights reserved