Replacements for lysine in L-seryl-L-lysyl dipeptide amide inhibitors of Candida albicans myristoyl-CoA: Protein N-myristoyltransferase

Replacements for lysine in L-seryl-L-lysyl dipeptide amide inhibitors of Candida albicans myristoyl-CoA: Protein N-myristoyltransferase
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DOI:
10.1016/s0960-894x(97)00030-9
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发表时间:
1997-02-04
影响因子:
2.7
通讯作者:
Sikorski, JA
Sikorski, JA
中科院分区:
医学4区
文献类型:
--
作者:
Brown, DL;Devadas, B;Sikorski, JA

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对已知的C.白色念珠菌NMT鉴定硫醚16和甘氨酰胺18为亚微摩尔的C.白色念珠菌NMT,其保留了对人酶的良好选择性。所有被检测的杂环赖氨酸模拟物显示出与真菌酶的显著较弱的亲和力。(C)1997年,Elsevier Science Ltd.
A survey of potential cyclic and acyclic lysine replacements in known L-seryl-L-lysyl dipeptide inhibitors of C. albicans NMT identified the thioether 16 and glycinamide 18 as submicromolar inhibitors of C. albicans NMT, which retained goad selectivity over the human enzyme. Al of the heterocyclic lysine mimetics that were examined exhibited dramatically weaker affinity with the fungal enzyme. (C) 1997, Elsevier Science Ltd.