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allosterism - Articles and news items

Drug Targets Supplement 2012

Drug Targets: In-depth focus 2012

Drug Targets, Issue 6 2012, Supplements / 11 December 2012 / Patricia McDonald / Emmanuel Sturchler / Dayue Darrel Duan

GPCR allosteric modulation: new opportunities and challenges for drug discovery.
Chloride channels and cardiac arrhythmia: novel therapeutic targets?

Figure 1: Classification Scheme of GPCRs. R (Rhodopsin-like), S (Secretin-like), G (Glutamate-like), Others (Adhesion, Frizzled, Taste type-2, unclassified)

G protein coupled receptors – exploiting flexible conformations

Drug Targets, Issue 4 2012 / 3 September 2012 / Kathryn L. Chapman, Imperial Drug Discovery Centre, Imperial College London and John B.C. Findlay & Gemma K. Kinsella, Department of Biology, National University of Ireland Maynooth

G-protein coupled receptors (GPCRs) are a diverse super-family of proteins located within the plasma membrane of eukaryotic cells which have a common architecture consisting of seven-transmembrane (7-TM) segments, connected by extracellular (ECL) and intracellular (ICL) loops. They differ from other 7-TM proteins in their ability to activate guanine-nucleotide binding proteins or β-arrestin and so initiate a signalling cascade. They have a wide range of physiological roles and provide many successful drug targets, playing a role in disorders including allergies, cardiovascular dysfunction, depression, obesity, cancer, pain, diabetes and a variety of central nervous system conditions. This review will give a general overview of GPCRs and how their structures and activities can be used in drug discovery…


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