2,3-二磷酸甘油类似物的合成及功能评价研究进展

姚菀腾, 尹紫悦, 郭茜文, 李文斌, 王荣

中国药学杂志 ›› 2023, Vol. 58 ›› Issue (18) : 1671-1675.

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中国药学杂志
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中国药学杂志 ›› 2023, Vol. 58 ›› Issue (18) : 1671-1675. DOI: 10.11669/cpj.2023.18.007
综述

2,3-二磷酸甘油类似物的合成及功能评价研究进展

  • 姚菀腾1,2, 尹紫悦1, 郭茜文1, 李文斌1*, 王荣1,2*
作者信息 +

Advances in Synthesis and Functional Evaluation of Glycerol 2, 3-diphosphate Analogues

  • YAO Wanteng1,2, YIN Ziyue1, GUO Qianwen1, LI Wenbin1*, WANG Rong1,2*
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文章历史 +

摘要

2,3-二磷酸甘油(2,3-DPG)是血红蛋白氧亲和力的变构调节剂之一,它能与脱氧态血红蛋白(T态)结合,降低其对氧气的亲和力,增加血红蛋白在肌肉等组织中的释氧量,对维持机体缺氧有不可或缺的作用。而2,3-DPG由于透膜性较差,通过外源给药的方式起到的效果极为有限,设计可透膜的血红蛋白变构剂可为抗缺氧药物研究提供新的途径。本研究报道了2,3-DPG的作用方式、2,3-DPG类似物的研究进展及相关功能表征方法,为合成新的2,3-DPG类似物提供新的思路。

Abstract

Glycerol 2, 3-diphosphate (2,3-DPG) is one of the allosteric regulators of oxygen affinity of hemoglobin. It can combine with deoxygenated hemoglobin (T-state), reduce its affinity for oxygen, increase the oxygen release of hemoglobin in muscles and other tissues, and play an indispensable role in maintaining hypoxia. However, the effect of exogenous administration of 2, 3-DPG is extremely limited due to its poor membrane permeability. The design of membrane permeable hemoglobin allosteric agent can provide a new way for the study of anti-hypoxia drugs. This article reviews the action mode of 2,3-DPG, the research progress of 2,3-DPG analogues and related functional characterization methods to provide new ideas for synthesis of novel 2,3-DPG analogues.

关键词

2,3-二磷酸甘油酸 / 血红蛋白 / 变构剂 / 亲脂性化合物 / 高原缺氧

Key words

glycerol 2, 3-diphosphate / hemoglobin / allosteric agent / lipophilic compounds / high altitude hypoxia

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姚菀腾, 尹紫悦, 郭茜文, 李文斌, 王荣. 2,3-二磷酸甘油类似物的合成及功能评价研究进展[J]. 中国药学杂志, 2023, 58(18): 1671-1675 https://doi.org/10.11669/cpj.2023.18.007
YAO Wanteng, YIN Ziyue, GUO Qianwen, LI Wenbin, WANG Rong. Advances in Synthesis and Functional Evaluation of Glycerol 2, 3-diphosphate Analogues[J]. Chinese Pharmaceutical Journal, 2023, 58(18): 1671-1675 https://doi.org/10.11669/cpj.2023.18.007
中图分类号： G353   

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基金

国家自然科学基金项目资助(82173738);部队拔尖培育项目资助(2021yxky005);全军青年培育项目资助(20QNPY070)

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