Exploration of GGTase-I substrate requirements. Part 1: Synthesis and biochemical evaluation of novel aryl-modified geranylgeranyl diphosphate analogs

Temple Kayla J.; Wright Elia N.; Fierke Carol A.; Gibbs Richard A.

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Exploration of GGTase-I substrate requirements. Part 1: Synthesis and biochemical evaluation of novel aryl-modified geranylgeranyl diphosphate analogs

机译：探索GGTase-I底物要求。第1部分：新型的芳基修饰的香叶基香叶基二磷酸类似物的合成及生化评估

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Protein geranylgeranylation is a type of post-translational modification that aids in the localization of proteins to the plasma member where they elicit cellular signals. To better understand the isoprenoid requirements of GGTase-I, a series of aryl-modified geranylgeranyl diphosphate analogs were synthesized and screened against mammalian GGTase-I. Of our seven-member library of compounds, six analogs proved to be substrates of GGTase-I, with 6d having a k(rel) = 1.93 when compared to GGPP (k(rel) = 1.0). (C) 2016 Elsevier Ltd. All rights reserved.

机译：蛋白质香叶基香叶基化是一种翻译后修饰，有助于将蛋白质定位在血浆中，在血浆中它们引发细胞信号。为了更好地理解GGTase-I的类异戊二烯需求，合成了一系列芳基修饰的香叶基香叶基二磷酸二磷酸酯类似物，并针对哺乳动物的GGTase-I进行了筛选。在我们的七元化合物库中，六个类似物被证明是GGTase-I的底物，与GGPP（k（rel）= 1.0）相比，6d的k（rel）= 1.93。（C）2016 Elsevier Ltd.保留所有权利。

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《Bioorganic and Medicinal Chemistry Letters》 |2016年第15期|共4页
作者
Temple Kayla J.; Wright Elia N.; Fierke Carol A.; Gibbs Richard A.;
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正文语种 eng
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关键词
Geranylgeranylation; Aryl-modified GGPP analogs; GGTase-I; Post-translational modification; Protein prenylation;

机译：香叶基香叶基化;芳基修饰的GGPP类似物;GGTase-I;翻译后修饰;蛋白质烯丙基化;

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1. Exploration of GGTase-I substrate requirements. Part 1: Synthesis and biochemical evaluation of novel aryl-modified geranylgeranyl diphosphate analogs [J] . Temple Kayla J., Wright Elia N., Fierke Carol A., Bioorganic and Medicinal Chemistry Letters . 2016,第15期

机译：探索GGTase-I底物要求。第1部分：新型的芳基修饰的香叶基香叶基二磷酸类似物的合成及生化评估
2. Specificity of geranylgeranyl diphosphate synthase for homoallylic substrate analogs [J] . Ohya Norimasa, Ichijo Takumi, Sato Hana, Journal of molecular catalysis, B. Enzymatic . 2015,第Null期

机译：香叶基香叶基二磷酸合酶对同型底物类似物的特异性
3. Synthesis of Stable Analogues of Geranylgeranyl Diphosphate Possessing a (Z,E,E)-Geranylgeranyl Side Chain, Docking Analysis, and Biological Assays for Prenyl Protein Transferase Inhibition [J] . Filippo Minutolo, Simone Bertini, Laura Betti, ChemMedChem . 2006,第2期

机译：具有（Z，E，E）-Geranylgeranyl侧链的香叶基香叶基二磷酸酯的稳定类似物的合成，对接分析和异戊二烯基蛋白质转移酶抑制的生物学测定
4. Substrate Promiscuity of Pyruvate Kinase on Various Deoxynucleoside Diphosphates for Synthesis of Deoxynucleoside Triphosphates [C] . . 2008

机译：丙酮酸激酶在各种脱氧核苷二磷酸合成中的底物杂合性
5. Synthesis and evaluation of alternative substrates for farnesyl diphosphate synthase and isopentenyl diphosphate isomerase [D] . Heaps, Nicole Ann 2008

机译：法呢基二磷酸合酶和异戊烯基二磷酸异构酶的替代底物的合成和评估
6. Exploration of GGTase-I substrate requirements. Part 1. Synthesis biochemical evaluation of novel aryl-modified geranylgeranyl diphosphate analogs [O] . Kayla J. Temple, Elia N. Wright, Carol A. Fierke, -1

机译：探索GGTase-I底物要求。第1部分。新型芳基修饰的香叶基香叶基二磷酸类似物的合成及生化评估
7. Exploration of GGTase-I substrate requirements. Part 1: Synthesis and biochemical evaluation of novel aryl-modified geranylgeranyl diphosphate analogs [O] . Kayla J. Temple, Elia N. Wright, Carol A. Fierke, 2016

机译：GGTase-I基底要求的探索。第1部分：新型芳基改性的芳基壬基甲基二磷酸类似物的合成和生化评价

Exploration of GGTase-I substrate requirements. Part 1: Synthesis and biochemical evaluation of novel aryl-modified geranylgeranyl diphosphate analogs

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