1lwx

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{{STRUCTURE_1lwx| PDB=1lwx | SCENE= }}
{{STRUCTURE_1lwx| PDB=1lwx | SCENE= }}
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'''AZT DIPHOSPHATE BINDING TO NUCLEOSIDE DIPHOSPHATE KINASE'''
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===AZT DIPHOSPHATE BINDING TO NUCLEOSIDE DIPHOSPHATE KINASE===
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==Overview==
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To be effective as antiviral agent, AZT (3'-azido-3'-deoxythymidine) must be converted to a triphosphate derivative by cellular kinases. The conversion is inefficient and, to understand why AZT diphosphate is a poor substrate of nucleoside diphosphate (NDP) kinase, we determined a 2.3-A x-ray structure of a complex with the N119A point mutant of Dictyostelium NDP kinase. It shows that the analog binds at the same site and, except for the sugar ring pucker which is different, binds in the same way as the natural substrate thymidine diphosphate. However, the azido group that replaces the 3'OH of the deoxyribose in AZT displaces a lysine side chain involved in catalysis. Moreover, it is unable to make an internal hydrogen bond to the oxygen bridging the beta- and gamma-phosphate, which plays an important part in phosphate transfer.
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(as it appears on PubMed at http://www.pubmed.gov), where 9207061 is the PubMed ID number.
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{{ABSTRACT_PUBMED_9207061}}
==About this Structure==
==About this Structure==
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[[Category: Azidothymidine]]
[[Category: Azidothymidine]]
[[Category: Phosphotransferase]]
[[Category: Phosphotransferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 00:23:04 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jul 2 22:44:15 2008''

Revision as of 19:44, 2 July 2008

Image:1lwx.png

Template:STRUCTURE 1lwx

AZT DIPHOSPHATE BINDING TO NUCLEOSIDE DIPHOSPHATE KINASE

Template:ABSTRACT PUBMED 9207061

About this Structure

1LWX is a Single protein structure of sequence from Dictyostelium discoideum. Full crystallographic information is available from OCA.

Reference

X-ray analysis of azido-thymidine diphosphate binding to nucleoside diphosphate kinase., Xu Y, Sellam O, Morera S, Sarfati S, Biondi R, Veron M, Janin J, Proc Natl Acad Sci U S A. 1997 Jul 8;94(14):7162-5. PMID:9207061

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