聖塔非研究所

摘要 G 蛋白質 coupled receptors (GPCRs) activate heterotr

2024-06-12 · 已發表論文 · 更新 2026/08/30 下午12:48

摘要 G 蛋白質 coupled receptors (GPCRs) activate heterotrimeric G 蛋白質s by promoting guanine nucleotide exchange. Here, we investigate the coupling of G 蛋白質s with GPCRs and describe the events tha…

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論文資訊

  • 類型:已發表論文
  • 日期:2024-06-12

摘要

G-蛋白質-coupled receptors (GPCRs) activate heterotrimeric G 蛋白質s by promoting guanine nucleotide exchange. Here, we investigate the coupling of G 蛋白質s with GPCRs and describe the events that ultimately lead to the ejection of GDP from its binding pocket in the G alpha subunit, the rate-limiting step during G-蛋白質 activation. Using molecular dynamics simulations, we investigate the temporal progression of structural rearrangements of GDP-bound Gs 蛋白質 (GsGDP; hereafter GsGDP) upon coupling to the beta 2-adrenergic receptor (beta 2AR) in atomic detail. The binding of GsGDP to the beta 2AR is followed by long-range allosteric effects that significantly reduce the energy needed for GDP release: the opening of alpha 1-alpha F helices, the displacement of the alpha G helix and the opening of the alp

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