Cruzain: Difference between revisions
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<StructureSection load='1me3' size='350' side='right' caption='Structure of cruzain catalytic domain complex with methylketone inhibitor (PDB entry [[1me3]])' scene='51/517378/Cv/1'> | |||
'''Cruzain''' or '''cruzipain''' (Cru) is the major cysteine protease present in ''Trypanosoma cruzi'' which is the parasite causing Chagas disease. <ref>PMID:10997902</ref> | |||
< | == Relevance == | ||
Cru inhibitors are being investigated for therapeutic use against Chagas disease. | |||
== Structural highlights == | |||
<scene name='51/517378/Cv/5'>Cru catalytic triad is Cys-His-Asn</scene> and <scene name='51/517378/Cv/6'>whole binding site</scene> ([[1me3]]).<ref>PMID:12467703</ref> | |||
</StructureSection> | </StructureSection> | ||
==3D structures of cruzain== | ==3D structures of cruzain== | ||
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Updated on {{REVISIONDAY2}}-{{MONTHNAME|{{REVISIONMONTH}}}}-{{REVISIONYEAR}} | Updated on {{REVISIONDAY2}}-{{MONTHNAME|{{REVISIONMONTH}}}}-{{REVISIONYEAR}} | ||
[[1aim]], [[2aim]], [[1me3]], [[1me4]] – | [[6n3s]] - TcCru catalytic domain 123-337 - ''Trypanosoma cruzi'' <br /> | ||
[[1f29]], [[1f2a]], [[1f2b]], [[1f2c]], [[1ewo]], [[3lxs]] - | [[1aim]], [[2aim]], [[1me3]], [[1me4]], [[3iut]] – TcCru catalytic domain + methylketone inhibitor<br /> | ||
[[1ewl]], [[1ewm]] – | [[1f29]], [[1f2a]], [[1f2b]], [[1f2c]], [[1ewo]], [[2oz2]], [[3hd3]], [[3lxs]], [[6ux6]] - TcCru catalytic domain + vinyl sulfone derived inhibitor<br /> | ||
[[1ewp]] - | [[1ewl]], [[1ewm]] – TcCru catalytic domain + methylbutane inhibitor<br /> | ||
[[1u9q]], [[3i06]], [[3kku]], [[4klb]], [[4pi3]], [[4qh6]], [[4w5b]], [[4w5c]], [[4xui]], [[6o2x]] - TcCru catalytic domain + inhibitor<br /> | |||
[[1ewp]] - TcCru catalytic domain + MOR-Leu-HPQ<br /> | |||
[[4w5b]], [[4xui]], [[4qh6]], [[4pi3]], [[4klb]], [[3kku]], [[3i06]], [[2oz2]], [[1u9q]] – TcCru + inhibitor <br /> | |||
[[4w5c]], [[3iut]], [[3hd3]] – TcCru (mutant) + inhibitor <br /> | |||
[[7juj]], [[7s18]], [[7s19]] - TcCru catalytic domain + gallinamide derivative<br /> | |||
== References == | == References == | ||
<references/> | <references/> | ||
Latest revision as of 12:52, 30 November 2022
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3D structures of cruzain3D structures of cruzain
Updated on 30-November-2022
6n3s - TcCru catalytic domain 123-337 - Trypanosoma cruzi
1aim, 2aim, 1me3, 1me4, 3iut – TcCru catalytic domain + methylketone inhibitor
1f29, 1f2a, 1f2b, 1f2c, 1ewo, 2oz2, 3hd3, 3lxs, 6ux6 - TcCru catalytic domain + vinyl sulfone derived inhibitor
1ewl, 1ewm – TcCru catalytic domain + methylbutane inhibitor
1u9q, 3i06, 3kku, 4klb, 4pi3, 4qh6, 4w5b, 4w5c, 4xui, 6o2x - TcCru catalytic domain + inhibitor
1ewp - TcCru catalytic domain + MOR-Leu-HPQ
4w5b, 4xui, 4qh6, 4pi3, 4klb, 3kku, 3i06, 2oz2, 1u9q – TcCru + inhibitor
4w5c, 3iut, 3hd3 – TcCru (mutant) + inhibitor
7juj, 7s18, 7s19 - TcCru catalytic domain + gallinamide derivative
ReferencesReferences
- ↑ Brinen LS, Hansell E, Cheng J, Roush WR, McKerrow JH, Fletterick RJ. A target within the target: probing cruzain's P1' site to define structural determinants for the Chagas' disease protease. Structure. 2000 Aug 15;8(8):831-40. PMID:10997902
- ↑ Huang L, Brinen LS, Ellman JA. Crystal structures of reversible ketone-Based inhibitors of the cysteine protease cruzain. Bioorg Med Chem. 2003 Jan 2;11(1):21-9. PMID:12467703