Modelling G-protein-coupled receptors for drug design.
The G-protein coupled receptors form a large and diverse multi-gene superfamily with many important physiological functions. As such, they have become important targets in pharmaceutical research. Molecular modelling and site-directed mutagenesis have played an important role in our increasing understanding of the structural basis of drug action at these receptors. Aspects of this understanding, how these techniques can be used within a drug-design programme, and remaining challenges for the future are reviewed.
Flower
D R
DR
Department of Physical Sciences, ASTRA Charnwood, Bakewell Rd, Loughborough, Leicestershire, UK. flower@jenner.ac.uk
D001665:Binding Sites; D020650:Combinatorial Chemistry Techniques; D015195:Drug Design; D019204:GTP-Binding Proteins / Q000737:chemistry*; D008024:Ligands; D008958:Models, Molecular; D015394:Molecular Structure; D016297:Mutagenesis, Site-Directed; D044140:Receptor, Angiotensin, Type 1; D044139:Receptor, Angiotensin, Type 2; D018343:Receptors, Adrenergic, beta-2 / Q000737:chemistry; D011945:Receptors, Angiotensin / Q000737:chemistry; D011956:Receptors, Cell Surface / Q000737:chemistry* / Q000145:classification / Q000235:genetics; D043562:Receptors, G-Protein-Coupled; D029701:Saccharomyces cerevisiae Proteins
C109334:GPR1 protein, S cerevisiae; D008024:Ligands; D044140:Receptor, Angiotensin, Type 1; D044139:Receptor, Angiotensin, Type 2; D018343:Receptors, Adrenergic, beta-2; D011945:Receptors, Angiotensin; D011956:Receptors, Cell Surface; D043562:Receptors, G-Protein-Coupled; D029701:Saccharomyces cerevisiae Proteins; D019204:GTP-Binding Proteins