Invited review: GPCR structural characterization: Using fragments as building blocks to determine a complete structure.

摘要: The structural characterization of G protein-coupled receptors has surged since the development methodologies to facilitate crystallization these highly helical, seven transmembrane, integral membrane receptors. In past years, eighteen GPCR structures were determined by X-ray crystallography. crystal represent a static picture conformationally flexible signal transducers. Analyses that probe their dynamics and conformational changes require other techniques, in particular solution state nuclear magnetic resonance studies. Such investigations are challenged size GPCRs, α-helical structure, which limits dispersion, tendencies aggregate micellar preparations heterogeneity. For many groups have been studying fragments as means overcome some difficulties. results fragment analyses presented here. Review literature reveals much original work depended on circular dichroism, infra-red spectroscopy fluorescence approaches. High resolution obtained NMR compared, where applicable, available structures. most cases, done biophysical analysis is validated comparisons. Our perspective field together with future goals must be considered if continued.