Design, synthesis and activity of bisubstrate, transition-state analogues and competitive inhibitors of aspartate transcarbamylase.

Grison C; Coutrot P; Comoy C; Balas L; Joliez S; Lavecchia G; Oliger P; Penverne B; Serre V; Herve G

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Design, synthesis and activity of bisubstrate, transition-state analogues and competitive inhibitors of aspartate transcarbamylase.

机译：天冬氨酸转氨酶的双底物，过渡态类似物和竞争性抑制剂的设计，合成和活性。

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Aspartate transcarbamylase initiates the de novo biosynthetic pathway for the production of the pyrimidine nucleotides, precursors of nucleic acids. This pathway is particularly active in rapidly growing cells and tissues. Thus, this enzyme has been tested as a potential target for antiproliferative drugs. In the present work, on the basis of its structural and mechanistic properties, a series of substrate analogues, including potential suicide-pseudosubstrates was synthesized and their putative inhibitory effects were tested using E. coli aspartate transcarbamylase as a model. Two of these compounds appear to be very efficient inhibitors of this enzyme.

机译：天冬氨酸转氨酶起始了从头开始的生物合成途径，以产生嘧啶核苷酸，核酸的前体。该途径在迅速生长的细胞和组织中特别活跃。因此，该酶已被测试为抗增殖药的潜在靶标。在目前的工作中，基于其结构和机械性能，合成了一系列底物类似物，包括潜在的自杀性假底物，并使用大肠杆菌天冬氨酸转氨酶作为模型测试了其假定的抑制作用。这些化合物中的两种似乎是该酶的非常有效的抑制剂。

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来源
《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2004年第4期|共12页
作者
Grison C; Coutrot P; Comoy C; Balas L; Joliez S; Lavecchia G; Oliger P; Penverne B; Serre V; Herve G;
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正文语种 eng
中图分类基础医学;
关键词
Aspartate Carbamoyltransferase; inhibitors; competition; Enzymes; Cancer patients and suicide and depression; 天冬氨酸转氨甲酰酶; 酶类;

机译：Aspartate Carbamoyltransferase;inhibitors;competition;Enzymes;Cancer patients and suicide and depression;天冬氨酸转氨甲酰酶;酶类;

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1. Design, synthesis and activity of bisubstrate, transition-state analogues and competitive inhibitors of aspartate transcarbamylase. [J] . Grison C, Coutrot P, Comoy C, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2004,第4期

机译：天冬氨酸转氨酶的双底物，过渡态类似物和竞争性抑制剂的设计，合成和活性。
2. Design, synthesis, topoisomerase I & II inhibitory activity, antiproliferative activity, and structure-activity relationship study of pyrazoline derivatives: An ATP-competitive human topoisomerase II alpha catalytic inhibitor [J] . Ahmad Pervez, Woo Hyunjung, Jun Kyu-Yeon, Bioorganic and medicinal chemistry . 2016,第8期

机译：吡唑啉衍生物的设计，合成，拓扑异构酶I和II的抑制活性，抗增殖活性和构效关系研究：一种具有ATP竞争性的人类拓扑异构酶IIα催化抑制剂
3. Synthesis and structure-activity relationships of cerebroside analogues as substrates of cerebroside sulphotransferase and discovery of a competitive inhibitor [J] . Li Wenjin, Guillaume Joren, Baqi Younis, Trends in Ecology & Evolution . 2020,第1期

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4. Solid Phase Synthesis of Lipidated Peptidotriazoles as Bisubstrate Inhibitors of Protein Geranylgeranyltransferase-I [C] . Animesh V. Aditya, Richard A. Gibbs American Peptide Symposium . 2009

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5. Design and synthesis of molecular probes to modulate cell membrane permeation: I. Design, synthesis, and biological evaluation of novel chicoric acid analogues as inhibitors of HIV-1 integrase. II. Design, synthesis, and biological evaluation of novel estradiol analogues targeting the membrane estrogen receptor. [D] . Charvat, Trevor Thomas. 2004

机译：设计和合成的分子探针，可调节细胞膜的渗透性：I.设计，合成和生物评价作为抗HIV-1整合酶抑制剂的新型菊苣酸类似物。二。针对膜雌激素受体的新型雌二醇类似物的设计，合成和生物学评估。
6. Synthesis and structure-activity relationships of cerebroside analogues as substrates of cerebroside sulphotransferase and discovery of a competitive inhibitor [O] . Wenjin Li, Joren Guillaume, Younis Baqi, 2020

机译：脑脑脂类似物作为脑血管转移酶底物的合成及结构 - 活性关系及竞争性抑制剂的发现
7. Design, synthesis, and bioactivity of novel inhibitors of E. coli aspartate transcarbamoylase [O] . Eldo, J., Heng, S., Kantrowitz, E. 2007

机译：新型大肠杆菌天冬氨酸转氨甲酰酶抑制剂的设计，合成和生物活性

Design, synthesis and activity of bisubstrate, transition-state analogues and competitive inhibitors of aspartate transcarbamylase.

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