一种导致高血压的突变型盐皮质激素受体的晶体结构。
Crystal structure of a mutant mineralocorticoid receptor responsible for hypertension.
作者信息
Fagart Jérôme, Huyet Jessica, Pinon Grégory M, Rochel Marina, Mayer Claudine, Rafestin-Oblin Marie-Edith
机构信息
INSERM U478, Faculté de Médecine Xavier Bichat, 16 rue Henri Huchard, B.P. 416, 75870 Paris Cedex 18, France.
出版信息
Nat Struct Mol Biol. 2005 Jun;12(6):554-5. doi: 10.1038/nsmb939. Epub 2005 May 22.
The S810L mutation within the human mineralocorticoid receptor (MR S810L) induces severe hypertension and switches progesterone from antagonist to agonist. Here we report the crystal structures of the ligand-binding domain of MR S810L in complex with progesterone and deoxycorticosterone, an agonist of both wild-type and mutant MRs. These structures, the first for MR, identify the specific contacts created by Leu810 and clarify the mechanism of activation of MR S810L.
人类盐皮质激素受体中的S810L突变（MR S810L）会引发严重高血压，并使孕酮从拮抗剂转变为激动剂。在此，我们报告了MR S810L配体结合结构域与孕酮和脱氧皮质酮（野生型和突变型MR的激动剂）复合物的晶体结构。这些结构是首次针对MR的结构，确定了Leu810产生的特定接触，并阐明了MR S810L的激活机制。
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