Cruzain

Cruzain (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

(1me3).^[2]

Structure of cruzain catalytic domain complex with methylketone inhibitor (PDB entry 1me3)

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3D structures of cruzain3D structures of cruzain

Updated on 21-December-2015

1aim, 2aim, 1me3, 1me4 – Cru catalytic domain + methylketone inhibitor – Trypanosoma cruzi
1f29, 1f2a, 1f2b, 1f2c, 1ewo, 3lxs - Cru catalytic domain + vinyl sulfone derived inhibitor
1ewl, 1ewm – Cru catalytic domain + methylbutane inhibitor
1ewp - Cru catalytic domain + MOR-Leu-HPQ

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

Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)

Michal Harel, Alexander Berchansky

[1] 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

[2] 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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