1pwy
From Proteopedia
(New page: 200px<br /> <applet load="1pwy" size="450" color="white" frame="true" align="right" spinBox="true" caption="1pwy, resolution 2.80Å" /> '''CRYSTAL STRUCTURE O...) |
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caption="1pwy, resolution 2.80Å" /> | caption="1pwy, resolution 2.80Å" /> | ||
'''CRYSTAL STRUCTURE OF HUMAN PNP COMPLEXED WITH ACYCLOVIR'''<br /> | '''CRYSTAL STRUCTURE OF HUMAN PNP COMPLEXED WITH ACYCLOVIR'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1PWY 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 SO4 and AC2 as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Purine-nucleoside_phosphorylase Purine-nucleoside phosphorylase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.4.2.1 2.4.2.1] Full crystallographic information is available from [http:// | + | 1PWY 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=SO4:'>SO4</scene> and <scene name='pdbligand=AC2:'>AC2</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Purine-nucleoside_phosphorylase Purine-nucleoside phosphorylase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.4.2.1 2.4.2.1] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1PWY OCA]. |
==Reference== | ==Reference== | ||
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[[Category: synchrotron]] | [[Category: synchrotron]] | ||
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Revision as of 14:41, 15 February 2008
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CRYSTAL STRUCTURE OF HUMAN PNP COMPLEXED WITH ACYCLOVIR
Contents |
Overview
In human, purine nucleoside phosphorylase (HsPNP) is responsible for, degradation of deoxyguanosine and genetic deficiency of this enzyme leads, to profound T-cell mediated immunosuppression. PNP is therefore a target, for inhibitor development aiming at T-cell immune response modulation and, has been submitted to extensive structure-based drug design. This work, reports the first crystallographic study of human PNP complexed with, acyclovir (HsPNP:Acy). Acyclovir is a potent clinically useful inhibitor, of replicant herpes simplex virus that also inhibits human PNP but with a, relatively lower inhibitory activity (K(i)=90 microM). Analysis of the, structural differences among the HsPNP:Acy complex, PNP apoenzyme, and, HsPNP:Immucillin-H provides explanation for inhibitor binding, refines the, purine-binding site, and can be used for future inhibitor design.
Disease
Known diseases associated with this structure: Neutral lipid storage disease with myopathy OMIM:[609059], Nucleoside phosphorylase deficiency, immunodeficiency due to OMIM:[164050]
About this Structure
1PWY is a Single protein structure of sequence from Homo sapiens with and as ligands. Active as Purine-nucleoside phosphorylase, with EC number 2.4.2.1 Full crystallographic information is available from OCA.
Reference
Crystal structure of human purine nucleoside phosphorylase complexed with acyclovir., dos Santos DM, Canduri F, Pereira JH, Vinicius Bertacine Dias M, Silva RG, Mendes MA, Palma MS, Basso LA, de Azevedo WF Jr, Santos DS, Biochem Biophys Res Commun. 2003 Aug 29;308(3):553-9. PMID:12914786
Page seeded by OCA on Fri Feb 15 16:41:51 2008
Categories: Homo sapiens | Purine-nucleoside phosphorylase | Single protein | Azevedo, W.F.De. | Basso, L.A. | Canduri, F. | Dias, M.Vinicius.Bertacine. | Mendes, M.A. | Palma, M.S. | Pereira, J.H. | Santos, D.M.Dos. | Santos, D.S. | Silva, R.G. | AC2 | SO4 | Acyclovir | Crystallography | Drug design | Purine nucleoside phosphorylase | Synchrotron
