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Structural basis for allosteric regulation of GPCRs by sodium ions.(REPORTS)(G protein-coupled receptors)(Author abstract)(Report)

Liu, Wei ; Chun, Eugene ; Thompson, Aaron A. ; Chubukov, Pavel ; Xu, Fei ; Katritch, Vsevolod ; Han, Gye Won ; Roth, Christopher B. ; Heitman, Laura H. ; Ijzerman, Adriaan P. ; Cherezov, Vadim ; Stevens, Raymond C.

Science, July 13, 2012, Vol.337(6091), p.232(5) [Tạp chí có phản biện]

ISSN: 0036-8075

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  • Nhan đề:
    Structural basis for allosteric regulation of GPCRs by sodium ions.(REPORTS)(G protein-coupled receptors)(Author abstract)(Report)
  • Tác giả: Liu, Wei ; Chun, Eugene ; Thompson, Aaron A. ; Chubukov, Pavel ; Xu, Fei ; Katritch, Vsevolod ; Han, Gye Won ; Roth, Christopher B. ; Heitman, Laura H. ; Ijzerman, Adriaan P. ; Cherezov, Vadim ; Stevens, Raymond C.
  • Chủ đề: G Proteins -- Chemical Properties ; Receptor-mediated Endocytosis -- Chemical Properties ; Chemistry -- Research
  • Là 1 phần của: Science, July 13, 2012, Vol.337(6091), p.232(5)
  • Mô tả: Pharmacological responses of G protein--coupled receptors (GPCRs) can be fine-tuned by allosteric modulators. Structural studies of such effects have been Limited due to the medium resolution of GPCR structures. We reengineered the human [A.sub.2A] adenosine receptor by replacing its third intracellular loop with apocytochrome [b.sub.562]RIL and solved the structure at 1.8 angstrom resolution. The high-resolution structure allowed us to identify 57 ordered water molecules inside the receptor comprising three major clusters. The central cluster harbors a putative sodium ion bound to the highly conserved aspartate residue [Asp.sup.2.50]. Additionally, two cholesterols stabilize the conformation of helix VI, and one of 23 ordered lipids intercalates inside the ligand-binding pocket. These high-resolution details shed light on the potential role of structured water molecules, sodium ions, and lipids/cholesterol in GPCR stabilization and function. doi: 10.1126/science.1219218
  • Ngôn ngữ: English
  • Số nhận dạng: ISSN: 0036-8075

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