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[求助]
英译中，谢谢
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Carazolol is a partial inverse agonist that binds with picomolar affinity to β2AR-T4L producinga reduction of the basal activity of the receptor (24). The crystal structure reveals extensiveinteractions between the receptor and carazolol that position the carbazole moiety adjacent toPhe2896.51, Phe2906.52, and Trp2866.48 (Figure 5A,S1 and Table S3). In contrast, cis-retinalis a full inverse agonist covalently bound to rhodopsin, which suppresses all activity towardstransducin (58). Carazolol and retinal occupy similar spaces in their respective receptors, withsignificant overlap of the non-aromatic regions of carazolol. However, the β-ionone ring ofretinal extends deep into the binding pocket of rhodopsin and contacts residues on helix V andVI, where it is sandwiched between Phe2125.47 and Tyr2686.51, and interacts with the highlyconserved Trp2656.48 (Figure 5B). It has been proposed that changes in the rotamer ofTrp2656.48 occur upon activation of rhodopsin and related family members, and constitutesthe “toggle switch” for receptor activation (59). Accordingly, the interactions between cis-retinal and Trp2656.48 are likely to contribute to the absence of basal activity in rhodopsin.Carazolol does not interact directly with the toggle switch on helix VI, however it lowers thebasal activity of the receptor, and may do so by interacting with Phe2896.51 and Phe2906.52,which form an extended aromatic network surrounding the highly conserved Trp2866.48. As aresult, Trp2866.48 adopts the rotamer associated with the inactive state. Thus, the stericconstraints imposed by Phe2906.52 appear to structurally mimic the interaction of the β-iononering of retinal with the conserved Trp2656.48 and Phe2125.47 on rhodopsin (60) (Figure 5C). 求翻译，谢谢 |
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genhunter
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arazolol is a partial inverse agonist that binds with picomolar affinity to β2AR-T4L producing a reduction of the basal activity of the receptor (24). 卡拉洛尔是个部分反向激动剂， 能与β2AR-T4L以微微摩尔亲和力结合，引起该受体的基础活性下调（24）。 CThe crystal structure reveals extensiveinteractions between the receptor and carazolol that position the carbazole moiety adjacent toPhe2896.51, Phe2906.52, and Trp2866.48 (Figure 5A,S1 and Table S3). In contrast, cis-retinalis a full inverse agonist covalently bound to rhodopsin, which suppresses all activity towardstransducin (58). 晶体结构揭示了卡拉洛尔与受体之间的作用有多个，咔唑基团位置与phe2896.51，phe2906.52，和trp2866.48相邻（图5A，S1和S3表）。相反，顺维生素A醛 是完全反向激动剂,与视紫红质共价结合，抑制所有信号转导活性（58）。 Carazolol and retinal occupy similar spaces in their respective receptors, withsignificant overlap of the non-aromatic regions of carazolol. However, the β-ionone ring ofretinal extends deep into the binding pocket of rhodopsin and contacts residues on helix V andVI, where it is sandwiched between Phe2125.47 and Tyr2686.51, and interacts with the highlyconserved Trp2656.48 (Figure 5B). 卡拉洛尔和顺维生素A醛在各自的受体上占据相似的空间，与卡拉洛尔非芳香族部分有显著的重叠。然而，顺维生素A醛的紫罗兰酮环更深地延伸到视紫红质的结合口袋里, 与位于螺旋V、VI上的残基接触,在phe2125.47和tyr2686.51之间互换，并与高度保守的trp2656.48作用（图5b）。 It has been proposed that changes in the rotamer ofTrp2656.48 occur upon activation of rhodopsin and related family members, and constitutesthe “toggle switch” for receptor activation (59). Accordingly, the interactions between cis-retinal and Trp2656.48 are likely to contribute to the absence of basal activity in rhodopsin.Carazolol does not interact directly with the toggle switch on helix VI, however it lowers thebasal activity of the receptor, and may do so by interacting with Phe2896.51 and Phe2906.52, which form an extended aromatic network surrounding the highly conserved Trp2866.48.Carazolol does not interact directly with the toggle switch on helix VI, however it lowers thebasal activity of the receptor, and may do so by interacting with Phe2896.51 and Phe2906.52,which form an extended aromatic network surrounding the highly conserved Trp2866.48. As aresult, Trp2866.48 adopts the rotamer associated with the inactive state. Thus, the stericconstraints imposed by Phe2906.52 appear to structurally mimic the interaction of the β-iononering of retinal with the conserved Trp2656.48 and Phe2125.47 on rhodopsin (60) (Figure 5C). 有人提出trp2656.48的旋转异构体在激活的视紫红质和相关的成员中发生了变化，起到受体激活的“拨动开关”的作用（59）。因此，顺维生素A醛和trp2656.48之间的相互作用可能有助于在视紫红质没有基底活力。卡拉洛尔与螺旋VI上的拨动开关没有直接作用，但是它降低了受体的基础活性，并可能通过与phe2896.51和phe2906.52相互作用得以实现，高度保守的trp2866.48在周边形成一个伸展的芳香基团网络。 结果，trp2866.48在不活跃状态处于异构体构像。因此，由phe2906.52造成的很大的空间约束似乎在结构意义上模仿β-紫罗兰酮环与保守的trp2656.48和phe2125.47在视紫红质上的相互作用（60）（图5c） |
2楼2015-05-28 13:07:38