Urokinase

From Proteopedia

Revision as of 08:00, 27 March 2017

spinqualitylabelsall models Human urokinase short chain and catalytic domain complex with inhibitor and phosphate, 3ig6 Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image Function Urokinase (UK) or urokinase plasminogen activator is a serine protease whose principal substrate is plasminogen – the inactive zymogen of plasmin[1]. UK consists of 3 domains: ligand-binding domain and kringle and growth factor domains. Prourokinase (PUK) is the inactive zymogen of UK which becomes active by proteolytic cleavage into catalytic domain (residues 179-431) and short chain (residues 156-178). Relevance Increased levels of UK are associated with poor prognosis in patients with breast cancer and thus is used as prognostic markers for the disease[2]. Structural highlights The and interacts with the active Ser of the catalytic triad[3].

3D Structures of urokinase

Updated on 27-March-2017

References

1. ↑ Carriero MV, Stoppelli MP. The urokinase-type plasminogen activator and the generation of inhibitors of urokinase activity and signaling. Curr Pharm Des. 2011;17(19):1944-61. PMID:21711235
2. ↑ Han B, Nakamura M, Mori I, Nakamura Y, Kakudo K. Urokinase-type plasminogen activator system and breast cancer (Review). Oncol Rep. 2005 Jul;14(1):105-12. PMID:15944776
3. ↑ West CW, Adler M, Arnaiz D, Chen D, Chu K, Gualtieri G, Ho E, Huwe C, Light D, Phillips G, Pulk R, Sukovich D, Whitlow M, Yuan S, Bryant J. Identification of orally bioavailable, non-amidine inhibitors of Urokinase Plasminogen Activator (uPA). Bioorg Med Chem Lett. 2009 Oct 1;19(19):5712-5. Epub 2009 Aug 7. PMID:19703768 doi:10.1016/j.bmcl.2009.08.008