Three-Dimensional Structure of the Ligand-Binding Core of GluR2 in Complex with the Agonist (S)-ATPA: Implications for Receptor Subunit Selectivity

Marie-Louise Lunn; Anders Hogner; Tine B. Stensbol; Eric Gouaux; Jan Egebjerg; Jette S. Kastrup

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Three-Dimensional Structure of the Ligand-Binding Core of GluR2 in Complex with the Agonist (S)-ATPA: Implications for Receptor Subunit Selectivity

机译：GluR2配体结合核心与激动剂（S）-ATPA配合的三维结构：受体亚基选择性的含义。

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Two X-ray structures of the GluR2 ligand-binding core in complex with (S)-2-amino-3-(5-tert-butyl-3-hydroxy-4-isoxazolyl)propionic acid ((S)-ATPA) have been determined with and without Zn~(2+) ions. (S)-ATPA induces a domain closure of ca. 21° compared to the apo form. The tert-butyl moiety of (S)-ATPA is buried in a partially hydrophobic pocket and forces the ligand into the glutamate-like binding mode. The structures provide new insight into the molecular basis of agonist selectivity between AMPA and kainate receptors.

机译：与（S）-2-氨基-3-（5-叔丁基-3-羟基-4-异恶唑基）丙酸（（S）-ATPA）配合使用的GluR2配体结合核的两个X射线结构具有在有和没有Zn〜（2+）离子的条件下测定。（S）-ATPA诱导ca的域关闭。与载脂蛋白形式相比为21°。（S）-ATPA的叔丁基部分埋在部分疏水的口袋中，并迫使配体进入谷氨酸样结合模式。该结构为AMPA和海藻酸酯受体之间激动剂选择性的分子基础提供了新的见识。

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《Journal of Medicinal Chemistry》 |2003年第5期|共4页
作者
Marie-Louise Lunn; Anders Hogner; Tine B. Stensbol; Eric Gouaux; Jan Egebjerg; Jette S. Kastrup;
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1. Three-Dimensional Structure of the Ligand-Binding Core of GluR2 in Complex with the Agonist (S)-ATPA: Implications for Receptor Subunit Selectivity [J] . Marie-Louise Lunn, Anders Hogner, Tine B. Stensbol, Journal of Medicinal Chemistry . 2003,第5期

机译：GluR2配体结合核心与激动剂（S）-ATPA配合的三维结构：受体亚基选择性的含义。
2. Structural features of ATPA and thio-ATPA-potent and selective GluR5 receptor agonists. Crystal structure determinations and quantum chemical calculations [J] . Frydenvang K., Greenwood JR., Vogensen SB., Structural Chemistry . 2002,第5a6期

机译：ATPA的结构特征和硫-ATPA强效和选择性GluR5受体激动剂。晶体结构测定和量子化学计算
3. Competitive antagonism of AMPA receptors by ligands of different classes: crystal structure of ATPO bound to the GluR2 ligand-binding core, in comparison with DNQX. [J] . Hogner A, Greenwood JR, Liljefors T, Journal of Medicinal Chemistry . 2003,第2期

机译：不同类别的配体对AMPA受体的竞争拮抗作用：与DNQX相比，ATPO的晶体结构与GluR2配体结合核心结合。
4. Structure-activity relationship studies of new cyclic MSH analogues using cloned-human melanocortin receptors lead to greater selectivity and inverse agonists [C] . Minying Cai, Paolo Grieco, Jonathan Wiens, the International Peptide Symposium . 2001

机译：使用克隆人黑素激素受体的新循环MSH类似物的结构 - 活性关系研究导致更大的选择性和反向激动剂
5. Structure-Function Studies of Nicotinic Acetylcholine Receptors Using Selective Agonists and Positive Allosteric Modulators [D] . Marotta, Christopher Bruno 2015

机译：烟碱乙酰胆碱受体的结构功能研究使用选择性激动剂和正变构调节剂。
6. Correlating AMPA-Receptor Activation and Cleft Closure Across Subunits: Crystal Structures of the GluR4 Ligand-Binding Domain in Complex with Full and Partial Agonists [O] . Avinash Gill, Amanda Birdsey-Benson, Brian L. Jones, -1

机译：跨亚基的相关AMPA受体激活和缝隙闭合：与完整和部分激动剂复杂的GluR4配体结合域的晶体结构。
7. GluR2 ligand-binding core complexes: importance of the isoxazolol moiety and 5-substituent for the binding mode of AMPA-type agonists [O] . Kasper C, Lunn M.-L, Liljefors T, 2002

机译：GluR2配体结合核心复合物：异恶唑醇部分和5-取代基对AMPA型激动剂结合模式的重要性

Three-Dimensional Structure of the Ligand-Binding Core of GluR2 in Complex with the Agonist (S)-ATPA: Implications for Receptor Subunit Selectivity

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