1e7a
From Proteopedia
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| - | [[Image:1e7a.gif|left|200px]]<br /><applet load="1e7a" size=" | + | [[Image:1e7a.gif|left|200px]]<br /><applet load="1e7a" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="1e7a, resolution 2.20Å" /> | caption="1e7a, resolution 2.20Å" /> | ||
'''CRYSTAL STRUCTURE OF HUMAN SERUM ALBUMIN COMPLEXED WITH THE GENERAL ANESTHETIC PROPOFOL'''<br /> | '''CRYSTAL STRUCTURE OF HUMAN SERUM ALBUMIN COMPLEXED WITH THE GENERAL ANESTHETIC PROPOFOL'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1E7A is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with PFL as [http://en.wikipedia.org/wiki/ligand ligand]. Known structural/functional Sites: <scene name='pdbsite=PF1:Pfl Binding Site For Chain A (Residue 200'>PF1</scene>, <scene name='pdbsite=PF2:Pfl Binding Site For Chain A (Residue 200'>PF2</scene>, <scene name='pdbsite=PF3:Pfl Binding Site For Chain B (Residue 200'>PF3</scene> and <scene name='pdbsite=PF4:Pfl Binding Site For Chain B (Residue 200'>PF4</scene>. Full crystallographic information is available from [http:// | + | 1E7A is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=PFL:'>PFL</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Known structural/functional Sites: <scene name='pdbsite=PF1:Pfl+Binding+Site+For+Chain+A+(Residue+200'>PF1</scene>, <scene name='pdbsite=PF2:Pfl+Binding+Site+For+Chain+A+(Residue+200'>PF2</scene>, <scene name='pdbsite=PF3:Pfl+Binding+Site+For+Chain+B+(Residue+200'>PF3</scene> and <scene name='pdbsite=PF4:Pfl+Binding+Site+For+Chain+B+(Residue+200'>PF4</scene>. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1E7A OCA]. |
==Reference== | ==Reference== | ||
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[[Category: propofol]] | [[Category: propofol]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Feb 3 09:37:54 2008'' |
Revision as of 07:37, 3 February 2008
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CRYSTAL STRUCTURE OF HUMAN SERUM ALBUMIN COMPLEXED WITH THE GENERAL ANESTHETIC PROPOFOL
Contents |
Overview
Human serum albumin (HSA) is one of the most abundant proteins in the, circulatory system and plays a key role in the transport of fatty acids, metabolites, and drugs. For many drugs, binding to serum albumin is a, critical determinant of their distribution and pharmacokinetics; however, there have as yet been no high resolution crystal structures published of, drug-albumin complexes. Here we describe high resolution crystal, structures of HSA with two of the most widely used general anesthetics, propofol and halothane. In addition, we describe a crystal structure of, HSA complexed with both halothane and the fatty acid, myristate. We show, that the intravenous anesthetic propofol binds at two discrete sites on, HSA in preformed pockets that have been shown to accommodate fatty acids., Similarly we show that the inhalational agent halothane binds (at, concentrations in the pharmacologically relevant range) at three sites, that are also fatty acid binding loci. At much higher halothane, concentrations, we have identified additional sites that are occupied. All, of the higher affinity anesthetic binding sites are amphiphilic in nature, with both polar and apolar parts, and anesthetic binding causes only minor, changes in local structure.
Disease
Known diseases associated with this structure: Analbuminemia OMIM:[103600], Dysalbuminemic hyperthyroxinemia OMIM:[103600], Dysalbuminemic hyperzincemia OMIM:[103600]
About this Structure
1E7A is a Single protein structure of sequence from Homo sapiens with as ligand. Known structural/functional Sites: , , and . Full crystallographic information is available from OCA.
Reference
Binding of the general anesthetics propofol and halothane to human serum albumin. High resolution crystal structures., Bhattacharya AA, Curry S, Franks NP, J Biol Chem. 2000 Dec 8;275(49):38731-8. PMID:10940303
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