A New Potent Inhibitor of Glycogen Phosphorylase Reveals the Basicity of the Catalytic Site

Michael Mamais; Alessandra Degli Esposti; Virginia Kouloumoundra; Thomas Gustavsson; Filippo Monti; Alessandro Venturini; Evangelia D. Chrysina; Dimitra Markovitsi; Thanasis Gimisis

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A New Potent Inhibitor of Glycogen Phosphorylase Reveals the Basicity of the Catalytic Site

机译：糖原磷酸化酶的新有效抑制剂揭示了催化位点的碱度

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The design and synthesis of a glucose-based acridone derivative (GLAC), a potent inhibitor of glycogen phosphorylase (GP) are described. GLAC is the first inhibitor of glycogen phosphorylase, the electronic absorption properties of which are clearly distinguishable from those of the enzyme. This allows probing subtle interactions in the catalytic site. The GLAC absorption spectra, associated with X-ray crystallography and quantum chemistry calculations, reveal that part of the catalytic site of GP behaves as a highly basic environment in which GLAC exists as a bis-anion. This is explained by water-bridged hydrogenbonding interactions with specific catalytic site residues.

机译：描述了基于葡萄糖的吖啶酮衍生物（Glac）的设计和合成，糖原磷酸化酶（GP）的有效抑制剂。 Glac是糖原磷酸化酶的第一抑制剂，其电子吸收特性与酶的那些明显区别。这允许探测催化部位的微妙相互作用。与X射线晶体学和量子化学计算相关的Glac吸收光谱揭示了GP的一部分GP的表现为高度基本环境，其中Glac作为双阴离子存在。这是通过与特定催化位点残留物的水桥接氢氢粘合相互作用来解释。

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来源
《Chemistry: A European journal》 |2017年第37期|共6页
作者
Michael Mamais; Alessandra Degli Esposti; Virginia Kouloumoundra; Thomas Gustavsson; Filippo Monti; Alessandro Venturini; Evangelia D. Chrysina; Dimitra Markovitsi; Thanasis Gimisis;
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作者单位

Department of Chemistry National and Kapodistrian University of Athens Athens (Greece);

Istituto ISOF Consiglio Nazionale delle Ricerche Bologna (Italy);

Department of Chemistry National and Kapodistrian University of Athens Athens (Greece);

LIDYL CEA CNRS Université Paris-Saclay Gif-sur-Yvette (France);

Istituto ISOF Consiglio Nazionale delle Ricerche Bologna (Italy);

Istituto ISOF Consiglio Nazionale delle Ricerche Bologna (Italy);

Institute of Biology Medicinal Chemistry and Biotechnology National Hellenic Research Foundation Athens (Greece);

LIDYL CEA CNRS Université Paris-Saclay Gif-sur-Yvette (France);

Department of Chemistry National and Kapodistrian University of Athens Athens (Greece);

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原文格式 PDF
正文语种 eng
中图分类应用化学;
关键词
acridone based inhibitors; glycogen phosphorylase; optical spectra; quantum chemistry; X-ray crystallography;

机译：吖啶基抑制剂;糖原磷酸化酶;光谱;量子化学;X射线晶体学;

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专利

1. A New Potent Inhibitor of Glycogen Phosphorylase Reveals the Basicity of the Catalytic Site [J] . Michael Mamais, Alessandra Degli Esposti, Virginia Kouloumoundra, Chemistry: A European journal . 2017,第37期

机译：糖原磷酸化酶的新有效抑制剂揭示了催化位点的碱度
2. Synthesis of N-Glucopyranosidic Derivatives as Potential Inhibitors that Bind at the Catalytic Site of Glycogen Phosphorylase [J] . T. Gimisis Mini-Reviews in Medicinal Chemistry . 2010,第12期

机译：N-Glucopyranosidic衍生物的合成作为潜在的抑制剂，在糖原磷酸化酶的催化位点结合
3. Synthesis of N-Glucopyranosidic Derivatives as Potential Inhibitors that Bind at the Catalytic Site of Glycogen Phosphorylase. [J] . Gimisis T Mini reviews in medicinal chemistry . 2010,第12期

机译：N-葡糖基糖苷衍生物的合成作为在糖原磷酸化酶催化位点结合的潜在抑制剂。
4. Predicting Cross-Reactivity from Computational Studies for Pre-evaluation of Specific Hepatic Glycogen Phosphorylase Inhibitors -insilico Screening of Drugs for Evaluating Specificity [C] . V. Badireenath Konkimalla International Conference on Bioinformatics and Biomedical Engineering . 2015

机译：从用于特定肝糖原磷酸化酶抑制剂预评估的计算研究预测交叉反应性-评估药物特异性的计算机筛选
5. Identification of Lysyl and Glycyl Residues Located at the Active Site in Glycogen Synthase and Their Roles in the Catalytic Reaction [D] . Furukawa, Koji 1993

机译：糖原合酶活性位点上的赖氨酰和甘氨酰残基的鉴定及其在催化反应中的作用
6. Multiple phosphate positions in the catalytic site of glycogen phosphorylase: structure of the pyridoxal-5-pyrophosphate coenzyme-substrate analog. [O] . S. R. Sprang, N. B. Madsen, S. G. Withers 1992

机译：糖原磷酸化酶催化位点中的多个磷酸盐位置：吡x醛-5-焦磷酸盐辅酶-底物类似物的结构。
7. A multidisciplinary study of 3-(β- d -glucopyranosyl)-5-substituted-1,2,4-triazole derivatives as glycogen phosphorylase inhibitors: Computation, synthesis, crystallography and kinetics reveal new potent inhibitors [O] . Sándor Kun, Jaida Begum, Efthimios Kyriakis, 2018

机译：3-（β-D-葡糖基）-5-取代的-1,2,4-三唑衍生物作为糖原磷酸化酶抑制剂的多学科研究：计算，合成，晶体学和动力学显示出新的有效抑制剂

A New Potent Inhibitor of Glycogen Phosphorylase Reveals the Basicity of the Catalytic Site

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