Urokinase
From Proteopedia
(Difference between revisions)
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== Structural highlights == | == Structural highlights == | ||
The <scene name='46/465442/Cv/10'>inhibitor of 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. | The <scene name='46/465442/Cv/10'>inhibitor of 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 == | == 3D Structures of urokinase == | ||
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**[[5lhs]] - UK catalytic domain (mutant) - mouse<br /> | **[[5lhs]] - UK catalytic domain (mutant) - mouse<br /> | ||
| - | *Urokinase catalytic domain complex with inhibitors | + | *Urokinase catalytic domain 179-424 complex with inhibitors |
| - | **[[4fu7]], [[4fu8]], [[4fu9]], [[4fub]], [[5xg4]] - hUK + inhibitor<br /> | + | **[[4fu7]], [[4fu8]], [[4fu9]], [[4fub]], [[5xg4]], [[5wxs]] - hUK + inhibitor<br /> |
| + | **[[1f92]], [[1sc8]], [[1vj9]], [[1vja]], [[2o8t]], [[2o8u]], [[2o8w]], [[4h42]], [[4mnv]],[[5wxt]] - hUK (mutant) + inhibitor<br /> | ||
**[[1fv9]] – hUK (mutant) + benzimidazole derivative <br /> | **[[1fv9]] – hUK (mutant) + benzimidazole derivative <br /> | ||
**[[5yc6]], [[5yc7]] - hUK (mutant) + benzylamine derivative<br /> | **[[5yc6]], [[5yc7]] - hUK (mutant) + benzylamine derivative<br /> | ||
**[[1f5k]] - hUK (mutant) + benzamidine derivative<br /> | **[[1f5k]] - hUK (mutant) + benzamidine derivative<br /> | ||
**[[1f5l]] - hUK (mutant) + amiloride 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 /> | **[[1owd]], [[1owe]], [[1owh]], [[1owi]], [[1owj]], [[1owk]], [[1sqa]], [[1sqo]], [[1u6q]], [[1sqt]], [[4fuc]], [[4fud]], [[4fue]], [[4fuf]], [[4fug]], [[4fuh]], [[4fui]], [[4fuj]]- hUK + naphthamidine inhibitor<br /> | ||
| + | **[[6nmb]]- hUK + tranexamic acid inhibitor<br /> | ||
**[[1ejn]] - hUK (mutant) + urea derivative inhibitor<br /> | **[[1ejn]] - hUK (mutant) + urea derivative inhibitor<br /> | ||
**[[2vin]], [[2vio]], [[2vip]], [[2viq]], [[2viv]], [[2viw]] - hUK (mutant) + mexiletine derivative<br /> | **[[2vin]], [[2vio]], [[2vip]], [[2viq]], [[2viv]], [[2viw]] - hUK (mutant) + mexiletine derivative<br /> | ||
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**[[4mnw]], [[4mnx]], [[4mny]], [[4os1]], [[4os2]], [[4os4]], [[4os5]], [[4os6]], [[4os7]] - hUK (mutant) + bicyclic peptide <br /> | **[[4mnw]], [[4mnx]], [[4mny]], [[4os1]], [[4os2]], [[4os4]], [[4os5]], [[4os6]], [[4os7]] - hUK (mutant) + bicyclic peptide <br /> | ||
**[[2vnt]], [[2r2w]] - hUK + guanidine derivative<br /> | **[[2vnt]], [[2r2w]] - hUK + guanidine derivative<br /> | ||
| + | **[[5xg4]] - hUK + quercetin<br /> | ||
**[[1w0z]], [[1w10]], [[1w11]], [[1w12]], [[1w13]], [[1w14]] - hUK + alanineamide derivative<br /> | **[[1w0z]], [[1w10]], [[1w11]], [[1w12]], [[1w13]], [[1w14]] - hUK + alanineamide derivative<br /> | ||
| + | **[[6xvd]]- hUK + UPAIN-1-W3F<br /> | ||
| + | **[[5wxf]]- hUK + UPAIN-2<br /> | ||
| + | **[[5wxo]]- hUK + UPAIN-2-W3F<br /> | ||
| + | **[[5wxp]]- hUK + UPAIN-2-3-W3F<br /> | ||
| + | **[[5wxr]]- hUK + UPAIN-2-4-W3F<br /> | ||
*Urokinase C terminal complex with inhibitors | *Urokinase C terminal complex with inhibitors | ||
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**[[4k24]] - hUK Hc N terminal + vitronectin + antibody<br /> | **[[4k24]] - hUK Hc N terminal + vitronectin + antibody<br /> | ||
**[[3laq]], [[3u73]] - hUK Hc N terminal + UK receptor<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 /> | **[[2i9b]] - hUK Hc N terminal + UK receptor (mutant)<br /> | ||
| + | **[[3pb1]] - hUK Hc C terminal (mutant) + UK inhibitor<br /> | ||
**[[4dw2]] - hUK B chain catalytic domain + antibody<br /> | **[[4dw2]] - hUK B chain catalytic domain + antibody<br /> | ||
**[[5hgg]] - hUK catalytic domain (mutant) + antibody<br /> | **[[5hgg]] - hUK catalytic domain (mutant) + antibody<br /> | ||
Revision as of 11:12, 23 March 2020
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3D Structures of urokinase
Updated on 23-March-2020
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
