Isoprenoids, also known as terpenes or terpenoids, represent a large family of natural products composed of five‐carbon isopentenyl diphosphate or its isomer dimethylallyl diphosphate as the building blocks. Isoprenoids are structurally and functionally diverse and include dolichols, steroid hormones, carotenoids, retinoids, aromatic metabolites, the isoprenoid side‐chain of ubiquinone, and isoprenoid attached signaling proteins. Productions of isoprenoids are catalyzed by a group of enzymes known as prenyltransferases, such as farnesyltransferases, geranylgeranyltransferases, terpenoid cyclase, squalene synthase, aromatic prenyltransferase, and cis‐ and trans‐prenyltransferases. Because these enzymes are key in cellular processes and metabolic pathways, they are expected to be potential targets in new drug discovery. In this review, six distinct subsets of characterized prenyltransferases are structurally and mechanistically classified, including (1) head‐to‐tail prenyl synthase, (2) head‐to‐head prenyl synthase, (3) head‐to‐middle prenyl synthase, (4) terpenoid cyclase, (5) aromatic prenyltransferase, and (6) protein prenylation. Inhibitors of those enzymes for potential therapies against several diseases are discussed. Lastly, recent results on the structures of integral membrane enzyme, undecaprenyl pyrophosphate phosphatase, are also discussed.

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异戊二烯转移酶的结构、催化和抑制机制

类异戊二烯，也称为萜烯或萜类化合物，是一大类天然产物，由五碳异戊烯基二磷酸或其异构体二甲基烯丙基二磷酸作为结构单元组成。类异戊二烯在结构和功能上是多种多样的，包括多酚、类固醇激素、类胡萝卜素、类视黄醇、芳香族代谢物、泛醌的类异戊二烯侧链和类异戊二烯附着的信号蛋白。类异戊二烯的生产由一组称为异戊二烯基转移酶的酶催化，例如法尼基转移酶、香叶基香叶基转移酶、萜类环化酶、角鲨烯合酶、芳香异戊二烯基转移酶以及顺式和反式异戊二烯基转移酶。因为这些酶是细胞过程和代谢途径的关键，所以它们有望成为新药发现的潜在目标。在本次审查中，六种不同的异戊二烯基转移酶亚群在结构和机制上进行分类，包括 (1) 头对尾异戊二烯基合酶，(2) 头对头异戊二烯基合酶，(3) 头对中间异戊二烯基合酶，(4) 萜类化合物环化酶，（5）芳香异戊二烯转移酶，和（6）蛋白质异戊二烯化。讨论了用于针对几种疾病的潜在疗法的这些酶的抑制剂。最后，还讨论了关于整合膜酶十一碳烯焦磷酸磷酸酶结构的最新结果。讨论了用于针对几种疾病的潜在疗法的这些酶的抑制剂。最后，还讨论了关于整合膜酶十一碳烯焦磷酸磷酸酶结构的最新结果。讨论了用于针对几种疾病的潜在疗法的这些酶的抑制剂。最后，还讨论了关于整合膜酶十一碳烯焦磷酸磷酸酶结构的最新结果。