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单词 Serpinopathy
释义

Serpinopathy

中文百科

丝氨酸蛋白酶抑制剂 Serpin

(重定向自Serpinopathy)
A protease (grey) bound to a serpin reactive centre loop (RCL, blue). When the protease's catalytic triad (red) cleaves the RCL, it becomes trapped in an inactive conformation. (PDB: 1K9O​)
The native state of serpins is an equilibrium between a fully stressed state (left) and a partially relaxed state (right). The five-stranded A-sheet (light blue) contains two functionally important regions for the serpin's mechanism, the breach and the shutter. The reactive centre loop (RCL, blue) exists in a dynamic equilibrium between the fully exposed conformation (left) and a conformation where it is partially inserted into the breach of the A-sheet (right).(PDB: 1QLP, 1YXA​)[42][43]
The inhibitory mechanism of serpins involves a large conformational change (S to R transition). The serpin (white) first binds a protease (grey) with the exposed reactive centre loop (blue). When this loop is cleaved by the protease, it rapidly inserts into the A-sheet (light blue), deforming and inhibiting the protease. (PDB: 1K9O, 1EZX​)Serine and cysteine proteases operate by a two-step catalytic mechanism. First, the substrate (blue) is attacked by the cysteine or serine of the catalytic triad (red) to form an acyl-enzyme intermediate. For typical substrates, the intermediate is resolved by hydrolysis by water. However, when the reactive centre loop (RCL) of a serpin is attacked, the conformational change (blue arrow) pulls the catalytic triad out of position, preventing it from completing catalysis. (Based on PDB: 1K9O, 1EZX​)

丝氨酸蛋白酶抑制剂英语:serpin)是具有相似结构蛋白质的蛋白质超家族,它是由于蛋白酶抑制活性被识别的,和在生命的各个界被发现的第一个蛋白质超家族。英文缩写丝氨酸蛋白酶抑制剂(英语:serpin)最初被创造,是因为第一个丝氨酸蛋白酶抑制剂对胰凝乳蛋白酶样丝氨酸蛋白酶(丝氨酸蛋白酶抑制剂)将要被识别的行为。

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更新时间:2025/6/18 11:06:43