Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Review
. 2009:552:51-66.
doi: 10.1007/978-1-60327-317-6_4.

An overview on GPCRs and drug discovery: structure-based drug design and structural biology on GPCRs

Kenneth Lundstrom  1
Affiliations
Review

An overview on GPCRs and drug discovery: structure-based drug design and structural biology on GPCRs

Kenneth Lundstrom. Methods Mol Biol. 2009.

Abstract

G protein-coupled receptors (GPCRs) represent 50-60% of the current drug targets. There is no doubt that this family of membrane proteins plays a crucial role in drug discovery today. Classically, a number of drugs based on GPCRs have been developed for such different indications as cardiovascular, metabolic, neurodegenerative, psychiatric, and oncologic diseases. Owing to the restricted structural information on GPCRs, only limited exploration of structure-based drug design has been possible. Much effort has been dedicated to structural biology on GPCRs and very recently an X-ray structure of the beta2-adrenergic receptor was obtained. This breakthrough will certainly increase the efforts in structural biology on GPCRs and furthermore speed up and facilitate the drug discovery process.

PubMed Disclaimer

References

    1. Blundel T.L. Structure-based drug design. Nature. 1996;384S:23–26. - PubMed
    1. Stoll V., Qin W., Stewart K.D., Jakob C., Park C., Walter K., Simmer R.L., Helfrich R., Bussiere D., Kao J., Kempf D., Sham H.L., Norbeck D.W. X-ray crystallographic structure of ABT-378 (lopinavir) bound to HIV-1 protease. Bioorg. Med. Chem. 2002;10:2803–2806. doi: 10.1016/S0968-0896(02)00051-2. - DOI - PubMed
    1. Varghese J.N. Development of neuraminidase inhibitors as anti-influenza virus drugs. Drug Dev. Res. 1999;46:176–196. doi: 10.1002/(SICI)1098-2299(199903/04)46:3/4<176::AID-DDR4>3.0.CO;2-6. - DOI
    1. http://www.mpibp-frankfurt.mpg.de/michel/public/memprotstruct.html
    1. Civelli O., Nothacker H.P., Saito Y., Wang Z., Lin S.H., Reinsheid R.K. Novel neurotransmitters as natural ligands of orphan G protein-coupled receptors. Trends Neurosci. 2001;24:230–237. doi: 10.1016/S0166-2236(00)01763-X. - DOI - PubMed

Substances

LinkOut - more resources