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Cruzain or cruzipain (Cru) is the major cysteine protease present in Trypanosoma cruzi which is the parasite causing Chagas disease. [1]
Relevance
Cru inhibitors are being investigated for therapeutic use against Chagas disease.
Structural highlights
Cru catalytic triad is Cys-His-Asn and whole binding site (1me3).[2]
- ↑ 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
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3D structures of cruzain
Updated on 13-June-2021
1me3 - Cru catalytic domain 123-337 - Trypanosoma cruzi
1aim, 2aim, 1me3, 1me4, 3iut – Cru catalytic domain + methylketone inhibitor
1f29, 1f2a, 1f2b, 1f2c, 1ewo, 2oz2, 3hd3, 3lxs, 6ux6 - Cru catalytic domain + vinyl sulfone derived inhibitor
1ewl, 1ewm – Cru catalytic domain + methylbutane inhibitor
1u9q, 3i06, 3kku, 4klb, 4pi3, 4qh6, 4w5b, 4w5c, 4xui, 6o2x - Cru catalytic domain + inhibitor
1ewp - Cru catalytic domain + MOR-Leu-HPQ
4w5b, 4xui, 4qh6, 4pi3, 4klb, 3kku, 3i06, 2oz2, 1u9q – TcPRO + inhibitor
4w5c, 3iut, 3hd3 – TcPRO (mutant) + inhibitor
References
