de Launoit Y, Adamski J
Virology Unit, Faculty of Medicine, CP 614, Free University Brussels, 808 route de Lennik, 1070 Brussels, Belgium.
J Mol Endocrinol. 1999 Jun;22(3):227-40. doi: 10.1677/jme.0.0220227.
Six types of human 17beta-hydroxysteroid dehydrogenases catalyzing the conversion of estrogens and androgens at position C17 have been identified so far. The peroxisomal 17beta-hydroxysteroid dehydrogenase type 4 (17beta-HSD 4, gene name HSD17B4) catalyzes the oxidation of estradiol with high preference over the reduction of estrone. The highest levels of 17beta-HSD 4 mRNA transcription and specific activity are found in liver and kidney followed by ovary and testes. A 3 kb mRNA codes for an 80 kDa (737 amino acids) protein featuring domains which are not present in the other 17beta-HSDs. The N-terminal domain of 17beta-HSD 4 reveals only 25% amino acid similarity with the other types of 17beta-HSDs. The 80 kDa protein is N-terminally cleaved to a 32 kDa enzymatically active fragment. Both the 80 kDa and the N-terminal 32 kDa (amino acids 1-323) protein are able to perform the dehydrogenase reaction not only with steroids at the C17 position but also with D-3-hydroxyacyl-coenzyme A (CoA). The enzyme is not active with L-stereoisomers. The central part of the 80 kDa protein (amino acids 324-596) catalyzes the 2-enoyl-acyl-CoA hydratase reaction with high efficiency. The C-terminal part of the 80 kDa protein (amino acids 597-737) facilitates the transfer of 7-dehydrocholesterol and phosphatidylcholine between membranes in vitro. The HSD17B4 gene is stimulated by progesterone, and ligands of PPARalpha (peroxisomal proliferator activated receptor alpha) such as clofibrate, and is down-regulated by phorbol esters. Mutations in the HSD17B4 lead to a fatal form of Zellweger syndrome.
迄今为止,已鉴定出六种催化雌激素和雄激素在C17位转化的人17β-羟基类固醇脱氢酶。过氧化物酶体4型17β-羟基类固醇脱氢酶(17β-HSD 4,基因名称HSD17B4)催化雌二醇的氧化,对雌酮还原的偏好性更高。在肝脏和肾脏中发现17β-HSD 4 mRNA转录水平和比活性最高,其次是卵巢和睾丸。一个3 kb的mRNA编码一个80 kDa(737个氨基酸)的蛋白质,其具有其他17β-HSD中不存在的结构域。17β-HSD 4的N端结构域与其他类型的17β-HSD仅显示25%的氨基酸相似性。80 kDa的蛋白质在N端被切割成一个32 kDa的酶活性片段。80 kDa和N端32 kDa(氨基酸1-323)的蛋白质不仅能够催化C17位类固醇的脱氢酶反应,还能催化D-3-羟基酰基辅酶A(CoA)的反应。该酶对L-立体异构体无活性。80 kDa蛋白质的中央部分(氨基酸324-596)高效催化2-烯酰基-CoA水合酶反应。80 kDa蛋白质的C端部分(氨基酸597-737)在体外促进7-脱氢胆固醇和磷脂酰胆碱在膜之间的转移。HSD17B4基因受孕酮、PPARα(过氧化物酶体增殖物激活受体α)的配体如氯贝丁酯刺激,并被佛波酯下调。HSD17B4中的突变会导致致命形式的泽尔韦格综合征。