2eu3
From Proteopedia
(New page: 200px<br /> <applet load="2eu3" size="450" color="white" frame="true" align="right" spinBox="true" caption="2eu3, resolution 1.6Å" /> '''Human Carbonic anhyd...) |
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| - | [[Image:2eu3.gif|left|200px]]<br /> | + | [[Image:2eu3.gif|left|200px]]<br /><applet load="2eu3" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="2eu3" size=" | + | |
caption="2eu3, resolution 1.6Å" /> | caption="2eu3, resolution 1.6Å" /> | ||
'''Human Carbonic anhydrase II in complex with novel inhibitors'''<br /> | '''Human Carbonic anhydrase II in complex with novel inhibitors'''<br /> | ||
==Overview== | ==Overview== | ||
| - | Human carbonic anhydrases (CAs) are well studied targets for the | + | Human carbonic anhydrases (CAs) are well studied targets for the development of inhibitors for pharmaceutical applications. The crystal structure of human CA II has been determined in complex with two CA inhibitors (CAIs) containing conventional sulfonamide and thiadiazole moieties separated by a -CF2- or -CHNH2- spacer group. The structures presented here reveal that these spacer groups allow novel binding modes for the thiadiazole moiety compared with conventional CAIs. |
==Disease== | ==Disease== | ||
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==About this Structure== | ==About this Structure== | ||
| - | 2EU3 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 ZN and FF3 as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Carbonate_dehydratase Carbonate dehydratase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=4.2.1.1 4.2.1.1] Full crystallographic information is available from [http:// | + | 2EU3 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=ZN:'>ZN</scene> and <scene name='pdbligand=FF3:'>FF3</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Carbonate_dehydratase Carbonate dehydratase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=4.2.1.1 4.2.1.1] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2EU3 OCA]. |
==Reference== | ==Reference== | ||
| - | X-ray crystallographic studies reveal that the incorporation of spacer groups in carbonic anhydrase inhibitors causes alternate binding modes., Fisher SZ, Govindasamy L, Boyle N, Agbandje-McKenna M, Silverman DN, Blackburn GM, McKenna R, Acta | + | X-ray crystallographic studies reveal that the incorporation of spacer groups in carbonic anhydrase inhibitors causes alternate binding modes., Fisher SZ, Govindasamy L, Boyle N, Agbandje-McKenna M, Silverman DN, Blackburn GM, McKenna R, Acta Crystallogr Sect F Struct Biol Cryst Commun. 2006 Jul 1;62(Pt, 7):618-22. Epub 2006 Jun 10. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=16820676 16820676] |
[[Category: Carbonate dehydratase]] | [[Category: Carbonate dehydratase]] | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Agbandje-McKenna, M.]] | [[Category: Agbandje-McKenna, M.]] | ||
| - | [[Category: Blackburn, G | + | [[Category: Blackburn, G M.]] |
[[Category: Boyle, N.]] | [[Category: Boyle, N.]] | ||
| - | [[Category: Fisher, S | + | [[Category: Fisher, S Z.]] |
[[Category: Govindasamy, L.]] | [[Category: Govindasamy, L.]] | ||
[[Category: McKenna, R.]] | [[Category: McKenna, R.]] | ||
| - | [[Category: Silverman, D | + | [[Category: Silverman, D N.]] |
[[Category: FF3]] | [[Category: FF3]] | ||
[[Category: ZN]] | [[Category: ZN]] | ||
[[Category: carbonic anhydrase ii proton transfer inhibitor]] | [[Category: carbonic anhydrase ii proton transfer inhibitor]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:14:32 2008'' |
Revision as of 15:14, 21 February 2008
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Human Carbonic anhydrase II in complex with novel inhibitors
Contents |
Overview
Human carbonic anhydrases (CAs) are well studied targets for the development of inhibitors for pharmaceutical applications. The crystal structure of human CA II has been determined in complex with two CA inhibitors (CAIs) containing conventional sulfonamide and thiadiazole moieties separated by a -CF2- or -CHNH2- spacer group. The structures presented here reveal that these spacer groups allow novel binding modes for the thiadiazole moiety compared with conventional CAIs.
Disease
Known disease associated with this structure: Osteopetrosis, autosomal recessive 3, with renal tubular acidosis OMIM:[611492]
About this Structure
2EU3 is a Single protein structure of sequence from Homo sapiens with and as ligands. Active as Carbonate dehydratase, with EC number 4.2.1.1 Full crystallographic information is available from OCA.
Reference
X-ray crystallographic studies reveal that the incorporation of spacer groups in carbonic anhydrase inhibitors causes alternate binding modes., Fisher SZ, Govindasamy L, Boyle N, Agbandje-McKenna M, Silverman DN, Blackburn GM, McKenna R, Acta Crystallogr Sect F Struct Biol Cryst Commun. 2006 Jul 1;62(Pt, 7):618-22. Epub 2006 Jun 10. PMID:16820676
Page seeded by OCA on Thu Feb 21 17:14:32 2008
