磷酸甘油酸激酶稳定双底物配体的合成与结合
Synthesis and binding of stable bisubstrate ligands for phosphoglycerate kinase.
作者信息
Williams D M, Jakeman D L, Vyle J S, Williamson M P, Blackburn G M
机构信息
Krebs Institute, Department of Chemistry, University of Sheffield, UK.
出版信息
Bioorg Med Chem Lett. 1998 Sep 22;8(18):2603-8. doi: 10.1016/s0960-894x(98)00466-1.
Stable bisubstrate ligands of phosphoglycerate kinase (PGK) have been synthesized with AMP or ADP conjugated to hydrolytically-stable, symmetrical analogues of 1,3-bisphosphoglycerate and their binding to yeast PGK evaluated. Their Kds decrease with net negative charge, with a penta-anionic analogue 7 showing highest affinity-in accordance with its approximation to the transition state for the reaction catalysed by PGK.
磷酸甘油酸激酶（PGK）的稳定双底物配体已被合成，其中AMP或ADP与1,3-二磷酸甘油酸的水解稳定对称类似物共轭，并评估了它们与酵母PGK的结合。它们的解离常数（Kds）随着净负电荷的增加而降低，五阴离子类似物7显示出最高的亲和力，这与其接近PGK催化反应的过渡态一致。
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