Urokinase - Revision history

Michal Harel at 11:03, 14 March 2024

Michal Harel — Thu, 14 Mar 2024 11:03:10 GMT

←Older revision		Revision as of 11:03, 14 March 2024
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	<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='' >		<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 ==

Alexander Berchansky at 12:04, 12 January 2022

Alexander Berchansky — Wed, 12 Jan 2022 12:04:57 GMT

←Older revision		Revision as of 12:04, 12 January 2022
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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 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 ==		== 3D Structures of urokinase ==
	[[Urokinase 3D Structures]]		[[Urokinase 3D Structures]]

Michal Harel at 11:13, 23 March 2020

Michal Harel — Mon, 23 Mar 2020 11:13:27 GMT

←Older revision		Revision as of 11:13, 23 March 2020
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	[[Urokinase 3D Structures]]		[[Urokinase 3D Structures]]
	</StructureSection>		</StructureSection>
-	== 3D Structures of urokinase ==

-	Updated on {{REVISIONDAY2}}-{{MONTHNAME\|{{REVISIONMONTH}}}}-{{REVISIONYEAR}}
-	{{#tree:id=OrganizedByTopic\|openlevels=0\|
-
-	*Urokinase
-
-	**[[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 />
-
-	*Urokinase catalytic domain 179-424 complex with inhibitors
-
-	**[[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 />
-	**[[5yc6]], [[5yc7]] - hUK (mutant) + benzylamine derivative<br />
-	**[[1f5k]] - hUK (mutant) + benzamidine derivative<br />
-	**[[1f5l]] - hUK (mutant) + amiloride derivative<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 />
-	**[[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 />
-	**[[5xg4]] - hUK + quercetin<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
-
-	**[[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
-
-	*Urokinase short chain + catalytic domain complex with inhibitors
-
-	**[[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 />
-
-	*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 />
-	**[[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 />
-	**[[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]]

Michal Harel at 11:12, 23 March 2020

Michal Harel — Mon, 23 Mar 2020 11:12:21 GMT

←Older revision		Revision as of 11:12, 23 March 2020
Line 8:		Line 8:
	== 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 />
Line 37:		Line 40:
	**[[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
Line 63:		Line 72:
	**[[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 />

Alexander Berchansky at 12:21, 10 October 2019

Alexander Berchansky — Thu, 10 Oct 2019 12:21:11 GMT

←Older revision		Revision as of 12:21, 10 October 2019
Line 7:		Line 7:

	== Structural highlights ==		== Structural highlights ==
-	The <scene name='46/465442/Cv/9'>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>.	+	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.
	</StructureSection>		</StructureSection>
	== 3D Structures of urokinase ==		== 3D Structures of urokinase ==

Joel L. Sussman at 12:20, 3 October 2018

Joel L. Sussman — Wed, 03 Oct 2018 12:20:12 GMT

←Older revision		Revision as of 12:20, 3 October 2018
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	**[[4fu7]], [[4fu8]], [[4fu9]], [[4fub]], [[5xg4]] - hUK + inhibitor<br />		**[[4fu7]], [[4fu8]], [[4fu9]], [[4fub]], [[5xg4]] - hUK + inhibitor<br />
	**[[1fv9]] – hUK (mutant) + benzimidazole derivative <br />		**[[1fv9]] – hUK (mutant) + benzimidazole derivative <br />
-	**[[~~4jni~~]], [[~~4jnl~~]] - 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 />

Michal Harel at 08:07, 22 August 2018

Michal Harel — Wed, 22 Aug 2018 08:07:13 GMT

←Older revision		Revision as of 08:07, 22 August 2018
Line 1:		Line 1:
-	<StructureSection load='3ig6' size='~~450~~' side='right' caption='Human urokinase light chain fragment (pink) and catalytic domain (yellow) complex with inhibitor and phosphate, [[3ig6]]' scene='' >	+	<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''' 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).

Joel L. Sussman at 10:25, 26 October 2017

Joel L. Sussman — Thu, 26 Oct 2017 10:25:19 GMT

←Older revision		Revision as of 10:25, 26 October 2017
Line 1:		Line 1:
-	<StructureSection load='' size='450' side='right' caption='Human urokinase light chain fragment (pink) and catalytic domain (yellow) complex with inhibitor and phosphate, [[3ig6]]' scene='' >	+	<StructureSection load='3ig6' size='450' 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''' 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).

Joel L. Sussman at 10:24, 26 October 2017

Joel L. Sussman — Thu, 26 Oct 2017 10:24:27 GMT

←Older revision		Revision as of 10:24, 26 October 2017
Line 1:		Line 1:
-	<StructureSection load='~~3ig6~~' size='450' side='right' caption='Human urokinase light chain fragment (pink) and catalytic domain (yellow) complex with inhibitor and phosphate, [[3ig6]]' scene='' >	+	<StructureSection load='' size='450' 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''' 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).

Michal Harel at 09:26, 26 October 2017

Michal Harel — Thu, 26 Oct 2017 09:26:45 GMT

←Older revision		Revision as of 09:26, 26 October 2017
Line 1:		Line 1:
-	<StructureSection load='3ig6' size='450' side='right' caption='Human urokinase ~~short~~ chain and catalytic domain complex with inhibitor and phosphate, [[3ig6]]' scene='' >	+	<StructureSection load='3ig6' size='450' 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''' 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).