Результаты исследований: Научные публикации в периодических изданиях › Обзорная статья › Рецензирование
Rhodopsin has served as the primary model for studying G protein-coupled receptors (GPCRs)-the largest group in the human genome, and consequently a primary target for pharmaceutical development. Understanding the functions and activation mechanisms of GPCRs has proven to be extraordinarily difficult, as they are part of a complex signaling cascade and reside within the cell membrane. Although X-ray crystallography has recently solved several GPCR structures that may resemble the activated conformation, the dynamics and mechanism of rhodopsin activation continue to remain elusive. Notably solid-state 2H NMR spectroscopy provides key information pertinent to how local dynamics of the retinal ligand change during rhodopsin activation. When combined with molecular mechanics simulations of proteolipid membranes, a new paradigm for the rhodopsin activation process emerges. Experiment and simulation both suggest that retinal isomerization initiates the rhodopsin photocascade to yield not a single activated structure, but rather an ensemble of activated conformational states. This article is part of a Special Issue entitled: Membrane protein structure and function.
Язык оригинала | английский |
---|---|
Страницы (с-по) | 241-251 |
Число страниц | 11 |
Журнал | Biochimica et Biophysica Acta - Biomembranes |
Том | 1818 |
Номер выпуска | 2 |
DOI | |
Состояние | Опубликовано - фев 2012 |
Опубликовано для внешнего пользования | Да |
ID: 5520781