Structure-function of the G protein–coupled receptor superfamily

V Katritch, V Cherezov… - Annual review of …, 2013 - annualreviews.org
During the past few years, crystallography of G protein–coupled receptors (GPCRs) has
experienced exponential growth, resulting in the determination of the structures of 16 distinct …

Structural diversity of G protein-coupled receptors and significance for drug discovery

MC Lagerström, HB Schiöth - Nature reviews Drug discovery, 2008 - nature.com
G protein-coupled receptors (GPCRs) are the largest family of membrane-bound receptors
and also the targets of many drugs. Understanding of the functional significance of the wide …

Sphingosine 1-phosphate receptors in health and disease: mechanistic insights from gene deletion studies and reverse pharmacology

V Brinkmann - Pharmacology & therapeutics, 2007 - Elsevier
Sphingosine 1-phosphate (S1P) is a bioactive sphingolipid that is critically involved in the
embryonic development of the cardiovascular and central nervous systems. In the adult, S1P …

Altered lipid metabolism in brain injury and disorders

RM Adibhatla, JF Hatcher - Lipids in health and disease, 2008 - Springer
Deregulated lipid metabolism may be of particular importance for CNS injuries and
disorders, as this organ has the highest lipid concentration next to adipose tissue …

Structure-Based Discovery of Novel Chemotypes for Adenosine A2A Receptor Antagonists

V Katritch, VP Jaakola, JR Lane, J Lin… - Journal of medicinal …, 2010 - ACS Publications
The recent progress in crystallography of G-protein coupled receptors opens an
unprecedented venue for structure-based GPCR drug discovery. To test efficiency of the …

Therapeutic antibodies directed at G protein-coupled receptors

CJ Hutchings, M Koglin, FH Marshall - MAbs, 2010 - Taylor & Francis
G protein-coupled receptors (GPCRs) are one of the most important classes of targets for
small molecule drug discovery, but many current GPCRs of interest are proving intractable to …

Novel insights on thyroid-stimulating hormone receptor signal transduction

G Kleinau, S Neumann, A Grüters, H Krude… - Endocrine …, 2013 - academic.oup.com
The TSH receptor (TSHR) is a member of the glycoprotein hormone receptors, a subfamily of
family AG protein-coupled receptors. The TSHR is of great importance for the growth and …

[HTML][HTML] G protein-coupled receptor dimerisation: molecular basis and relevance to function

G Milligan - Biochimica et Biophysica Acta (BBA)-Biomembranes, 2007 - Elsevier
The belief that G protein-coupled receptors exist and function as monomeric, non-interacting
species has been largely supplanted in recent years by evidence, derived from a range of …

[HTML][HTML] The application of artificial intelligence accelerates G protein-coupled receptor ligand discovery

W Chen, C Song, L Leng, S Zhang, S Chen - Engineering, 2024 - Elsevier
G protein-coupled receptors (GPCRs) are crucial players in various physiological processes,
making them attractive candidates for drug discovery. However, traditional approaches to …

[HTML][HTML] G protein-coupled receptors: the evolution of structural insight

SB Gacasan, DL Baker, AL Parrill - AIMS biophysics, 2017 - ncbi.nlm.nih.gov
G protein-coupled receptors (GPCR) comprise a diverse superfamily of over 800 proteins
that have gained relevance as biological targets for pharmaceutical drug design. Although …