The design and synthesis of inhibitors of pantothenate synthetase
The design and synthesis of inhibitors of pantothenate synthetase
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DOI：
10.1039/b609482a
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发表时间：
2006-01-01
影响因子：
3.2
通讯作者：
Abell, Chris
中科院分区：
文献类型：
--
作者：
Tuck, Kellie L.;Saldanha, S. Adrian;Abell, Chris
泛酸合成酶催化D-泛解酸和β-丙氨酸的ATP依赖性缩合以形成泛酸。十个类似物的反应中间体泛酰腺苷酸，其中的磷酸二酯被取代的酯或氨磺酰基基团，被设计为潜在的抑制剂的酶。这些酯都是适度的竞争性抑制剂，氨磺酰更有效，这与它们与泛酰腺苷酸中间体更接近的结构相似性一致。
Pantothenate synthetase catalyses the ATP-dependent condensation of D-pantoate and beta-alanine to form pantothenate. Ten analogues of the reaction intermediate pantoyl adenylate, in which the phosphodiester is replaced by either an ester or sulfamoyl group, were designed as potential inhibitors of the enzyme. The esters were all modest competitive inhibitors, the sulfamoyls were more potent, consistent with their closer structural similarity to the pantoyl adenylate intermediate.