Chirality-Driven Mode of Binding of alpha-Aminophosphonic Acid-Based Allosteric Inhibitors of the Human Farnesyl Pyrophosphate Synthase (hFPPS)

Feng Yuting; Park Jaeok; Li Shi-Guang; Boutin Rebecca; Viereck Peter; Schilling Matthew A.; Berghuis Albert M.; Tsantrizos Youla S.

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Chirality-Driven Mode of Binding of alpha-Aminophosphonic Acid-Based Allosteric Inhibitors of the Human Farnesyl Pyrophosphate Synthase (hFPPS)

机译：人芳erneyl焦磷酸盐合成酶（HFPPS）的α-氨基膦酸碱抑制剂的α-氨基膦酸基血糖抑制剂的依赖性

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Thienopyrimidine-based allosteric inhibitors of the human farnesyl pyrophosphate synthase (hFPPS), characterized by a chiral alpha-aminophosphonic acid moiety, were synthesized as enantiomerically enriched pairs, and their binding mode was investigated by X-ray crystallography. A general consensus in the binding orientation of all (R)- and (S)-enantiomers was revealed. This finding is a prerequisite for establishing a reliable structure-activity relationship (SAR) model.

机译：由手性α-氨基膦酸部分的人游芳基焦磷酸合酶（HFPP）的基于噻吩甲酰磷酸酯的体抑制剂被作为对映体富集的对合成，并通过X射线晶体学研究其结合模式。揭示了所有（R） - 和（S） - 苯体聚物的结合取向的一般共识。这一发现是建立可靠的结构活动关系（SAR）模型的先决条件。

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《Journal of Medicinal Chemistry》 |2019年第21期|共12页
作者
Feng Yuting; Park Jaeok; Li Shi-Guang; Boutin Rebecca; Viereck Peter; Schilling Matthew A.; Berghuis Albert M.; Tsantrizos Youla S.;
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McGill Univ Dept Chem 801 Sherbrooke St West Montreal PQ H3A 0B8 Canada;

McGill Univ Dept Chem 801 Sherbrooke St West Montreal PQ H3A 0B8 Canada;

McGill Univ Dept Chem 801 Sherbrooke St West Montreal PQ H3A 0B8 Canada;

McGill Univ Dept Chem 801 Sherbrooke St West Montreal PQ H3A 0B8 Canada;

McGill Univ Dept Chem 801 Sherbrooke St West Montreal PQ H3A 0B8 Canada;

McGill Univ Dept Biochem 3649 Promenade Sir William Osler Montreal PQ H3G 0B1 Canada;

McGill Univ Dept Biochem 3649 Promenade Sir William Osler Montreal PQ H3G 0B1 Canada;

McGill Univ Dept Chem 801 Sherbrooke St West Montreal PQ H3A 0B8 Canada;

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正文语种 eng
中图分类药学;
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专利

1. Chirality-Driven Mode of Binding of alpha-Aminophosphonic Acid-Based Allosteric Inhibitors of the Human Farnesyl Pyrophosphate Synthase (hFPPS) [J] . Feng Yuting, Park Jaeok, Li Shi-Guang, Journal of Medicinal Chemistry . 2019,第21期

机译：人芳erneyl焦磷酸盐合成酶（HFPPS）的α-氨基膦酸碱抑制剂的α-氨基膦酸基血糖抑制剂的依赖性
2. Discovery of Novel Allosteric Non-Bisphosphonate Inhibitors of Farnesyl Pyrophosphate Synthase by Integrated Lead Finding [J] . Marzinzik Andreas L., Amstutz Rene, Bold Guido, ChemMedChem . 2015,第11期

机译：通过集成的铅发现发现法呢基焦磷酸合酶的新型变构非双膦酸酯抑制剂
3. Human farnesyl pyrophosphate synthase is allosterically inhibited by its own product [J] . Jaeok Park, Michal Zielinski, Alexandr Magder, Nature Communications . 2017,第期

机译：人类法游坛焦磷酸盐合成酶被其自身产品变得严重抑制
4. Crystal structures and computer screened inhibitors of Helicobacter pylori undecaprenyl pyrophosphate synthase [C] . Chih-Jung Kuo, Rey-Ting Guo, I. Lin Lu, Frontiers in the Convergence of Bioscience and Information Technologies . 2007

机译：幽门螺杆菌非赤烷基焦磷酸术合酶的晶体结构和计算机筛选抑制剂
5. Design and synthesis of bisphosphonate analogs as inhibitors of farnesyl pyrophosphate synthase. [D] . Hogan, James Michael. 2008

机译：设计和合成双膦酸酯类似物作为法呢基焦磷酸合酶的抑制剂。
6. Human farnesyl pyrophosphate synthase is allosterically inhibited by its own product [O] . Jaeok Park, Michal Zielinski, Alexandr Magder, -1

机译：人法呢基焦磷酸合酶被其自身产物变构抑制
7. Chirality-Driven Mode of Binding of Aminophosphonic Acid-Based Allosteric Inhibitors of the Human Farnesyl Pyrophosphate Synthase (hFPPS) [O] . -1

机译：人芳erneyl焦磷酸盐合酶（HFPPS）的氨基膦酸基变构抑制剂的肾上腺磷酸酸性抑制剂的结合方式（HFPPS）
8. Human Serum Albumin: An Allosteric Domain Model for Bilirubin Binding Specificity [R] . Hsia, J. C., Er, S. S., Tan, C. T., 1981

机译：人血清白蛋白：胆红素结合特异性的变构域模型

Chirality-Driven Mode of Binding of alpha-Aminophosphonic Acid-Based Allosteric Inhibitors of the Human Farnesyl Pyrophosphate Synthase (hFPPS)

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