Regulation of amantadine hydrochloride binding with IIA subdomain of human serum albumin by fatty acid chains.
Regulation of amantadine hydrochloride binding with IIA subdomain of human serum albumin by fatty acid chains.
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脂肪酸链调节盐酸金刚烷胺与人血清白蛋白 IIA 亚结构域的结合。
DOI：
10.1002/jps.23336
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发表时间：
2013
期刊：
影响因子：
--
通讯作者：
梁宏
中科院分区：
文献类型：
--
作者：
杨峰;梁宏
人血清白蛋白（HSA）是血浆的主要蛋白质成分，已被利用以结合和运输各种内源性和外源性有机化合物。尽管阴离子药物很容易与HSA的IIA子域相关联，但大多数
Human serum albumin (HSA) is a major protein component of blood plasma that has been exploited to bind and transport a wide variety of endogenous and exogenous organic compounds. Although anionic drugs readily associate with the IIA subdomain of HSA, most cationic drugs poorly associate with HSA at this subdomain. In this study, we propose to improve the association between cationic drugs and HSA by modifying HSA with fatty acid chains. For our experiments, we tested amantadine hydrochloride, a cationic drug with antiviral and antiparkinsonian effects. Our results suggest that extensive myristoylation of HSA can help stabilize the interaction between amantadine and HSA in vitro. Our X-ray crystallography data further elucidate the structural basis of this regulation. Additionally, our crystallography data suggest that anionic drugs, with a functional carboxylate group, may enhance the association between amantadine and HSA by a mechanism similar to myristoylation. Ultimately, our results provide critical structural insight into this novel association between cationic drugs and the HSA IIA subdomain, raising the tempting possibility to fully exploit the unique binding capacity of HSA's IIA subdomain to achieve simultaneous delivery of anionic and cationic drugs.
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影响因子：
5.6
作者：
Zunszain, Patricia A.;Ghuman, Jamie;McDonagh, Antony F.;Curry, Stephen
通讯作者：
Curry, Stephen
影响因子：
3.7
作者：
Victor Tuan Giam Chuang;U. Kragh‐Hansen;M. Otagiri
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DOI：
10.1016/s0021-9258(19)62680-3
发表时间：
1986-05
期刊：
The Journal of biological chemistry
影响因子：
--
作者：
P. P. Minghetti-P.;D. E. Ruffner;W. Kuang;O. Dennison;J. Hawkins;W. Beattie;A. Dugaiczyk
通讯作者：
P. P. Minghetti-P.;D. E. Ruffner;W. Kuang;O. Dennison;J. Hawkins;W. Beattie;A. Dugaiczyk
影响因子：
5.6
作者：
Ghuman, J;Zunszain, PA;Curry, S
通讯作者：
Curry, S
DOI：
10.1007/0-306-47058-6_2
发表时间：
2002
期刊：
--
影响因子：
--
作者：
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通讯作者：
M. Eftink