Urokinase
From Proteopedia
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| - | <StructureSection load='' size=' | + | <StructureSection load='3ig6' size='350' side='right' caption='Human urokinase light chain fragment (pink) and catalytic domain (yellow) complex with inhibitor and phosphate, [[3ig6]]' scene='' > |
== Function == | == Function == | ||
| - | '''Urokinase''' (UK) or '''urokinase plasminogen activator''' is a serine protease whose principal substrate is plasminogen – the inactive zymogen of plasmin<ref>PMID:21711235</ref>. 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). | + | '''Urokinase''' (UK) or '''urokinase plasminogen activator''' or '''urokinase-type plasminogen activator''' is a serine protease whose principal substrate is plasminogen – the inactive zymogen of plasmin<ref>PMID:21711235</ref>. 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 == | == Relevance == | ||
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== Structural highlights == | == Structural highlights == | ||
| - | The <scene name='46/465442/Cv/ | + | The <scene name='46/465442/Cv/10'>inhibitor of UK binds in the active site of UK</scene> and interacts with the active Ser of the catalytic triad<ref>PMID:19703768</ref>. Water molecules are shown as red spheres. |
| + | == 3D Structures of urokinase == | ||
| + | [[Urokinase 3D Structures]] | ||
</StructureSection> | </StructureSection> | ||
| - | == 3D Structures of urokinase == | ||
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| - | Updated on {{REVISIONDAY2}}-{{MONTHNAME|{{REVISIONMONTH}}}}-{{REVISIONYEAR}} | ||
| - | {{#tree:id=OrganizedByTopic|openlevels=0| | ||
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| - | *Urokinase | ||
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| - | **[[2i9a]] - hUK Hc N terminal (residues 21-163) - human<br /> | ||
| - | **[[1urk]] - hUK Hc N terminal – NMR<br /> | ||
| - | **[[1kdu]] – hUK kringle domain (residues 69-153) - NMR<br /> | ||
| - | **[[4dva]] – hUK catalytic domain (residues 179-431) <br /> | ||
| - | **[[4xsk]] - hUK catalytic domain (mutant) <br /> | ||
| - | **[[5lhs]] - UK catalytic domain (mutant) - mouse<br /> | ||
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| - | *Urokinase catalytic domain complex with inhibitors | ||
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| - | **[[4fu7]], [[4fu8]], [[4fu9]], [[4fub]], [[5xg4]] - hUK + inhibitor<br /> | ||
| - | **[[1fv9]] – hUK (mutant) + benzimidazole derivative <br /> | ||
| - | **[[4jni]], [[4jnl]] - hUK (mutant) + benzylamine derivative<br /> | ||
| - | **[[1f5k]] - hUK (mutant) + benzamidine derivative<br /> | ||
| - | **[[1f5l]] - hUK (mutant) + amiloride derivative<br /> | ||
| - | **[[1f92]], [[1sc8]], [[1vj9]], [[1vja]], [[2o8t]], [[2o8u]], [[2o8w]], [[4h42]], [[4mnv]] - hUK (mutant) + inhibitor<br /> | ||
| - | **[[1owd]], [[1owe]], [[1owh]], [[1owi]], [[1owj]], [[1owk]], [[1sqa]], [[1sqo]], [[1u6q]], [[1sqt]], [[4fuc]], [[4fud]], [[4fue]], [[4fuf]], [[4fug]], [[4fuh]], [[4fui]], [[4fuj]]- hUK + naphthamidine inhibitor<br /> | ||
| - | **[[1ejn]] - hUK (mutant) + urea derivative inhibitor<br /> | ||
| - | **[[2vin]], [[2vio]], [[2vip]], [[2viq]], [[2viv]], [[2viw]] - hUK (mutant) + mexiletine derivative<br /> | ||
| - | **[[3qn7]], [[4jk5]], [[4jk6]], [[4x1n]], [[4x1q]], [[4x1r]], [[4x1s]], [[4x0w]], [[4x1p]], [[4zhl]], [[4zhm]], [[4zkn]], [[4zko]], [[4zkr]], [[4zks]] - hUK (mutant) + peptide inhibitor<br /> | ||
| - | **[[4mnw]], [[4mnx]], [[4mny]], [[4os1]], [[4os2]], [[4os4]], [[4os5]], [[4os6]], [[4os7]] - hUK (mutant) + bicyclic peptide <br /> | ||
| - | **[[2vnt]], [[2r2w]] - hUK + guanidine derivative<br /> | ||
| - | **[[1w0z]], [[1w10]], [[1w11]], [[1w12]], [[1w13]], [[1w14]] - hUK + alanineamide derivative<br /> | ||
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| - | *Urokinase C terminal complex with inhibitors | ||
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| - | **[[3kgp]] – hUK Hc C terminal (mutant) + benzoic acid derivative<br /> | ||
| - | **[[3khv]] - hUK Hc C terminal (mutant) + methanol derivative<br /> | ||
| - | **[[3mwi]] - hUK Hc C terminal (mutant) + amidine derivative<br /> | ||
| - | **[[3ox7]], [[3oy5]], [[3oy6]] - hUK Hc C terminal (mutant) + peptide inhibitor<br /> | ||
| - | **[[3kid]], [[3mhw]] - hUK Hc C terminal (mutant) + aminobenzothiazole derivative<br /> | ||
| - | **[[2nwn]], [[4gly]] - hUK Hc C terminal + cyclic peptide<br /> | ||
| - | **[[3m61]] - hUK Hc C terminal (mutant) + cyclic peptide | ||
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| - | *Urokinase short chain + catalytic domain complex with inhibitors | ||
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| - | **[[1lmw]] – hUK A+B catalytic domain + EGRCMK<br /> | ||
| - | **[[1c5w]], [[1c5x]], [[1c5y]], [[1c5z]] - hUK A+B chain catalytic domain + carboxamidine derivative<br /> | ||
| - | **[[1gi7]], [[1gi8]], [[1gi9]], [[1gj7]], [[1gj8]], [[1gj9]], [[1gja]], [[1gjb]], [[1gjc]], [[1gjd]] - hUK A+B chain catalytic domain (mutant) + carboxamidine derivative<br /> | ||
| - | **[[1o3p]], [[1o5a]], [[1o5b]], [[1o5c]] - hUK A+B chain catalytic domain (mutant) + benzenolate derivative<br /> | ||
| - | **[[3ig6]] – hUK A+B chain catalytic domain + inhibitor<br /> | ||
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| - | *Urokinase complex with protein | ||
| - | **[[2fd6]] – hUK Hc N terminal + antibody + UK receptor<br /> | ||
| - | **[[3bt1]], [[3bt2]] - hUK Hc N terminal + vitronectin + UK receptor<br /> | ||
| - | **[[4k24]] - hUK Hc N terminal + vitronectin + antibody<br /> | ||
| - | **[[3laq]], [[3u73]] - hUK Hc N terminal + UK receptor<br /> | ||
| - | **[[3pb1]] - hUK Hc C terminal (mutant) + UK inhibitor<br /> | ||
| - | **[[2i9b]] - hUK Hc N terminal + UK receptor (mutant)<br /> | ||
| - | **[[4dw2]] - hUK B chain catalytic domain + antibody<br /> | ||
| - | **[[5hgg]] - hUK catalytic domain (mutant) + antibody<br /> | ||
| - | **[[5lhn]], [[5lhr]] - mUK catalytic domain (mutant) + antibody<br /> | ||
| - | **[[5lhp]], [[5lhq]] - mUK catalytic domain (mutant) + antibody + inhibitor<br /> | ||
| - | }} | ||
==References== | ==References== | ||
<references /> | <references /> | ||
[[Category:Topic Page]] | [[Category:Topic Page]] | ||
Current revision
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References
- ↑ 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
- ↑ 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
- ↑ 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
