Modified 5-Fluorouracil: Uridine Phosphorylase Inhibitor

Lashkov A. A.; Shchekotikhin A. A.; Shtil A. A.; Sotnichenko S. E.; Mikhailov A. M.

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Modified 5-Fluorouracil: Uridine Phosphorylase Inhibitor

机译：修饰的5-氟尿嘧啶：尿苷磷酸化酶抑制剂

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5-Fluorouracil (5-FU) is a medication widely used in chemotherapy to treat various types of cancer. Being a substrate for the reverse reaction catalyzed by uridine phosphorylase (UPase), 5-FU serves as a promising prototype molecule (molecular scaffold) for the design of a selective UPase inhibitor that enhances the antitumor activity of 5-FU and exhibits intrinsic cytostatic effects on cancer cells. The chemical formula of the new compound, which binds to the uracil-binding site and, in the presence of a phosphate anion, to the phosphate-binding site of UPase, is proposed and investigated by molecular simulation methods.

机译：5-氟尿嘧啶（5-FU）是一种广泛用于化学疗法中的药物，用于治疗各种类型的癌症。 5-FU是尿苷磷酸化酶（UPase）催化的逆向反应的底物，可作为一种有前途的原型分子（分子支架），用于设计选择性的UPase抑制剂，该抑制剂可增强5-FU的抗肿瘤活性并表现出固有的细胞抑制作用在癌细胞上。提出并通过分子模拟方法研究了新化合物的化学式，该化合物与尿嘧啶结合位点结合，并且在存在磷酸根阴离子的情况下与UPase的磷酸结合位点结合。

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《Crystallography reports》 |2016年第5期|共4页
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Lashkov A. A.; Shchekotikhin A. A.; Shtil A. A.; Sotnichenko S. E.; Mikhailov A. M.;
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正文语种 eng
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1. Modified 5-Fluorouracil: Uridine Phosphorylase Inhibitor [J] . Lashkov A. A., Shchekotikhin A. A., Shtil A. A., Crystallography reports . 2016,第5期

机译：修饰的5-氟尿嘧啶：尿苷磷酸化酶抑制剂
2. In silico analysis of the three-dimensional structures of the homodimer of uridine phosphorylase from Yersinia Pseudotuberculosis in the ligand-free state and in a complex with 5-fluorouracil [J] . Lashkov A.A., Sotnichenko S.E., Mikhailov A.M. Crystallography reports . 2013,第2期

机译：在计算机上分析耶尔森氏菌假结核中尿苷磷酸化酶同二聚体的三维结构，无配体状态且与5-氟尿嘧啶复合
3. Synthesis and evaluation of 6-methylene-bridged uracil derivatives. Part 2: Optimization of inhibitors of human thymidine phosphorylase and their selectivity with uridine phosphorylase. [J] . Yano S, Kazuno H, Sato T, Bioorganic and medicinal chemistry . 2004,第13期

机译：6-亚甲基桥接的尿嘧啶衍生物的合成和评价。第2部分：人胸苷磷酸化酶抑制剂的优化及其对尿苷磷酸化酶的选择性。
4. Crystallization of uridine phosphorylase from E.coli on earth, macrogravity and microgravity [C] . E.Blagova, E.Morgunova, E.Smirnova, Third International Workshop on Materials Processing at High Gravity, held June 2-7, 1996 at Clarkson University, Potsdam, New York . 1996

机译：地球上，大重力和微重力下大肠杆菌中尿苷磷酸化酶的结晶
5. Purification and Characterization of Bovine Liver Uridine Phosphorylase. [D] . Avant, Jamie D. 2014

机译：牛肝尿苷磷酸化酶的纯化和表征。
6. Crystallization and preliminary X-ray diffraction analysis of Salmonella typhimurium uridine phosphorylase complexed with 5-fluorouracil [O] . A. A. Lashkov, A. G. Gabdoulkhakov, A. A. Shtil, 2009

机译：与5-氟尿嘧啶复合的鼠伤寒沙门氏菌尿苷磷酸化酶的结晶和初步X射线衍射分析
7. Crystallization and preliminary X-ray diffraction analysis of Salmonella typhimurium uridine phosphorylase complexed with 5-fluorouracil [O] . Lashkov, A. A., Gabdoulkhakov, A. G., Shtil, A. A., 2009

机译：与5-氟尿嘧啶复合的鼠伤寒沙门氏菌尿苷磷酸化酶的结晶和初步X射线衍射分析
8. P53 Regulation of Uridine Phosphorylase Activity, Pyrimidine Salvage Pathway and Their Effects on Breast Cancer Therapy [R] . Cao, D. , Pizzorno, G. 2003

机译：p53调节尿苷磷酸化酶活性，嘧啶补救途径及其对乳腺癌治疗的影响

Modified 5-Fluorouracil: Uridine Phosphorylase Inhibitor

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