Protein engineering and the study of structure--function relationships in receptors.
Protein engineering is a powerful tool for studying relationships between receptor structure and function--providing that it is used and interpreted appropriately. Site-directed mutagenesis, deletion mutagenesis and construction of chimaeric proteins have all been used to characterize receptors. In this review, Walter Ward, David Timms and Alan Fersht describe the application of protein engineering, illustrating important concepts with experimental data. They explain that detailed study of function requires careful dissection of mechanistic steps. Care must also be taken when selecting replacement residues; mutation should not cause delocalized structural reorganization or else the true significance of functional change will remain unclear.
Ward
W H
WH
ICI Pharmaceuticals, Macclesfield, Cheshire, UK.
Timms
D
D
Fersht
A R
AR
D006801:Humans; D015202:Protein Engineering; D011506:Proteins / Q000235:genetics*; D011955:Receptors, Drug / Q000235:genetics*; D013329:Structure-Activity Relationship
D011506:Proteins; D011955:Receptors, Drug