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Design of enzyme inhibitors using iterative protein crystallographic analysis.

作者信息

Appelt K, Bacquet R J, Bartlett C A, Booth C L, Freer S T, Fuhry M A, Gehring M R, Herrmann S M, Howland E F, Janson C A

机构信息

Agouron Pharmaceuticals, Inc., La Jolla, California 92037.

出版信息

J Med Chem. 1991 Jul;34(7):1925-34. doi: 10.1021/jm00111a001.

DOI:10.1021/jm00111a001
PMID:2066965
Abstract
摘要

相似文献

1
Design of enzyme inhibitors using iterative protein crystallographic analysis.
J Med Chem. 1991 Jul;34(7):1925-34. doi: 10.1021/jm00111a001.
2
Design, synthesis and evaluation of potent thymidylate synthase X inhibitors.强效胸苷酸合成酶X抑制剂的设计、合成与评价
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3
Structure-based design of lipophilic quinazoline inhibitors of thymidylate synthase.基于结构的胸苷酸合成酶亲脂性喹唑啉抑制剂设计
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Design of thymidylate synthase inhibitors using protein crystal structures: the synthesis and biological evaluation of a novel class of 5-substituted quinazolinones.利用蛋白质晶体结构设计胸苷酸合成酶抑制剂：一类新型5-取代喹唑啉酮的合成与生物学评价
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5
2'-Deoxyuridine 5'-monophosphate substrate displacement in thymidylate synthase through 6-hydroxy-2H-naphtho[1,8-bc]furan-2-one derivatives.6-羟基-2H-萘并[1,8-bc]呋喃-2-酮衍生物在胸苷酸合成酶中对 2'-脱氧尿苷 5'-单磷酸的底物置换作用。
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Synthesis and biological evaluation of N-acylhydrazones as inhibitors of MurC and MurD ligases.N-酰腙类化合物作为MurC和MurD连接酶抑制剂的合成及生物学评价
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Alanine mutants of the interface residues of human thymidylate synthase decode key features of the binding mode of allosteric anticancer peptides.人胸苷酸合成酶界面残基的丙氨酸突变体解析了变构抗癌肽结合模式的关键特征。
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N4-hydroxy-5-halogeno-2'-deoxycytidine S and their 5'-mono-phosphates as inhibitors of thymidylate synthase and in vitro antileukemic agents.N4-羟基-5-卤代-2'-脱氧胞苷S及其5'-单磷酸酯作为胸苷酸合成酶抑制剂和体外抗白血病药物。
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Novel 1,3,4-oxadiazole thioether derivatives targeting thymidylate synthase as dual anticancer/antimicrobial agents.靶向胸苷酸合成酶的新型1,3,4-恶二唑硫醚衍生物作为双重抗癌/抗菌剂
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Design, synthesis and biological evaluation of N-phenyl-(2,4-dihydroxypyrimidine-5-sulfonamido)benzoyl hydrazide derivatives as thymidylate synthase (TS) inhibitors and as potential antitumor drugs.设计、合成及生物评价 N- 苯基-(2,4-二羟基嘧啶-5-磺酰胺基)苯甲酰腙衍生物作为胸苷酸合成酶（TS）抑制剂和潜在的抗肿瘤药物。
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Structure-guided inhibitor design for human FAAH by interspecies active site conversion.通过种间活性位点转换进行人脂肪酸酰胺水解酶的结构导向抑制剂设计。
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Regulation of p53 expression by thymidylate synthase.胸苷酸合成酶对p53表达的调控。
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A phase I study of the lipophilic thymidylate synthase inhibitor Thymitaq (nolatrexed dihydrochloride) given by 10-day oral administration.一项关于亲脂性胸苷酸合成酶抑制剂Thymitaq（盐酸诺拉曲塞）的I期研究，采用为期10天的口服给药方式。
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