Structure for peptidase S01.231: urokinase-type plasminogen activator

Summary Gene structure Alignment Tree Sequences Sequence features Distribution Structure Literature Substrates Pharma

PDB	Organism	Resolution	Comment
1LMW	Homo sapiens	2.50 Å	peptidase domain; complex with Glu-Gly-Arg chloromethyl ketone
Catalytic residues are shown in ball-and-stick representation: His224 in purple, Asp275 in pink and Ser376 in orange. The light chain is shown in grey. Bound inhibitor fragments are shown in grey in ball-and-stick representation.

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TERTIARY STRUCTURE DATA
Comment	Resolution	PDB	PDBe	SCOP	CATH	PDBSum	Proteopedia	Reference
Homo sapiens
mature peptidase	1.94 Å	1C5W	1C5W	1C5W	1C5W	1C5W	1C5W	Katz et al., 2000
mature peptidase	1.75 Å	1C5X	1C5X	1C5X	1C5X	1C5X	1C5X	Katz et al., 2000
mature peptidase	1.65 Å	1C5Y	1C5Y	1C5Y	1C5Y	1C5Y	1C5Y	Katz et al., 2000
mature peptidase	1.85 Å	1C5Z	1C5Z	1C5Z	1C5Z	1C5Z	1C5Z	Katz et al., 2000
complex with B-chain inhibitor N-(1-adamantyl)-N'-(4-guanidinobenzyl)urea	1.80 Å	1EJN	1EJN	1EJN	1EJN	1EJN	1EJN	Sperl et al., 2000
complex with B-chain benzamidine inhibitor	1.80 Å	1F5K	1F5K	1F5K	1F5K	1F5K	1F5K	Zeslawska et al., 2000
complex with 3,5-diamino-N-(aminoiminomethyl)-6-chloropyrazinecarboxamide	2.10 Å	1F5L	1F5L	1F5L	1F5L	1F5L	1F5L	Zeslawska et al., 2000
complex with B-chain UKI-1D inhibitor	2.60 Å	1F92	1F92	1F92	1F92	1F92	1F92	Zeslawska et al., 2000
microurokinase; complex with 2-amino-5-hydroxy-benzimidazole	3.00 Å	1FV9	1FV9	1FV9	1FV9	1FV9	1FV9	Hajduk et al., 2000
mature peptidase	1.79 Å	1GI7	1GI7	1GI7	1GI7	1GI7	1GI7	Katz et al., 2001
mature peptidase	1.75 Å	1GI8	1GI8	1GI8	1GI8	1GI8	1GI8	Katz et al., 2001
mature peptidase	1.80 Å	1GI9	1GI9	1GI9	1GI9	1GI9	1GI9	Katz et al., 2001
engineering inhibitors highly selective for the s1 sites of ser190 trypsin-like serine protease drug targets	1.50 Å	1GJ7	1GJ7	1GJ7	1GJ7	1GJ7	1GJ7	Katz et al., 2001
engineering inhibitors highly selective for the s1 sites of ser190 trypsin-like serine protease drug targets	1.64 Å	1GJ8	1GJ8	1GJ8	1GJ8	1GJ8	1GJ8	Katz et al., 2001
engineering inhibitors highly selective for the s1 sites of ser190 trypsin-like serine protease drug targets	1.80 Å	1GJ9	1GJ9	1GJ9	1GJ9	1GJ9	1GJ9	Katz et al., 2001
engineering inhibitors highly selective for the s1 sites of ser190 trypsin-like serine protease drug targets	1.56 Å	1GJA	1GJA	1GJA	1GJA	1GJA	1GJA	Katz et al., 2001
engineering inhibitors highly selective for the s1 sites of ser190 trypsin-like serine protease drug targets	1.90 Å	1GJB	1GJB	1GJB	1GJB	1GJB	1GJB	Katz et al., 2001
engineering inhibitors highly selective for the s1 sites of ser190 trypsin-like serine protease drug targets	1.73 Å	1GJC	1GJC	1GJC	1GJC	1GJC	1GJC	Katz et al., 2001
engineering inhibitors highly selective for the s1 sites of ser190 trypsin-like serine protease drug targets	1.75 Å	1GJD	1GJD	1GJD	1GJD	1GJD	1GJD	Katz et al., 2001
NMR; kringle domain	0.00 Å	1KDU	1KDU	1KDU	1KDU	1KDU	1KDU	Li et al., 1992
peptidase domain; complex with Glu-Gly-Arg chloromethyl ketone	2.50 Å	1LMW	1LMW	1LMW	1LMW	1LMW	1LMW	Spraggon et al., 1995
mature peptidase	1.81 Å	1O3P	1O3P	1O3P	1O3P	1O3P	1O3P	Katz et al., 2003
dissecting and designing inhibitor selectivity determinants at the s1 site using an artificial ala190 protease (ala190 upa)	1.68 Å	1O5A	1O5A	1O5A	1O5A	1O5A	1O5A	Katz et al., 2004
dissecting and designing inhibitor selectivity determinants at the s1 site using an artificial ala190 protease (ala190 upa)	1.85 Å	1O5B	1O5B	1O5B	1O5B	1O5B	1O5B	Katz et al., 2004
dissecting and designing inhibitor selectivity determinants at the s1 site using an artificial ala190 protease (ala190 upa)	1.63 Å	1O5C	1O5C	1O5C	1O5C	1O5C	1O5C	Katz et al., 2004
substituted 2-naphthamidine inhibitors of urokinase	2.32 Å	1OWD	1OWD	1OWD	1OWD	1OWD	1OWD	Wendt et al., 2004
substituted 2-naphthamidine inhibitors of urokinase	1.60 Å	1OWE	1OWE	1OWE	1OWE	1OWE	1OWE	Wendt et al., 2004
substituted 2-naphthamidine inhibitors of urokinase	1.61 Å	1OWH	1OWH	1OWH	1OWH	1OWH	1OWH	Wendt et al., 2004
substituted 2-naphthamidine inhibitors of urokinase	2.93 Å	1OWI	1OWI	1OWI	1OWI	1OWI	1OWI	Wendt et al., 2004
substituted 2-naphthamidine inhibitors of urokinase	3.10 Å	1OWJ	1OWJ	1OWJ	1OWJ	1OWJ	1OWJ	Wendt et al., 2004
substituted 2-naphthamidine inhibitors of urokinase	2.80 Å	1OWK	1OWK	1OWK	1OWK	1OWK	1OWK	Wendt et al., 2004
urokinase plasminogen activator b-chain-j435 complex	2.40 Å	1SC8	1SC8	1SC8	1SC8	1SC8	1SC8	Schweinitz et al., 2004
substituted 2-naphthamidine inhibitors of urokinase	2.00 Å	1SQA	1SQA	1SQA	1SQA	1SQA	1SQA	Wendt et al., 2004
substituted 2-naphthamidine inhibitors of urokinase	1.84 Å	1SQO	1SQO	1SQO	1SQO	1SQO	1SQO	Wendt et al., 2004
substituted 2-naphthamidine inhibitors of urokinase	1.90 Å	1SQT	1SQT	1SQT	1SQT	1SQT	1SQT	Wendt et al., 2004
substituted 2-naphthamadine inhibitors of urokinase	2.02 Å	1U6Q	1U6Q	1U6Q	1U6Q	1U6Q	1U6Q	Bruncko et al., 2005
NMR; N-terminal fragment	0.00 Å	1URK	1URK	1URK	1URK	1URK	1URK	Hansen et al., 1994
B-chain; complex with JT464	2.40 Å	1VJ9	1VJ9	1VJ9	1VJ9	1VJ9	1VJ9	Schweinitz et al., 2004
B-chain; complex with JT464	2.00 Å	1VJA	1VJA	1VJA	1VJA	1VJA	1VJA	Schweinitz et al., 2004
complex with inhibitor SI1 (N-(butylsulfonyl)-D-seryl-N-4-[amino(imino)methyl]benzyl-L-alaninamide)	1.90 Å	1W0Z	1W0Z	1W0Z	1W0Z	1W0Z	1W0Z	Zeslawska et al., 2003
complex with inhibitor SJ1 (N-(isobutoxycarbonyl)-D-seryl-N-((1S)-4-[amino(imino)methyl]amino-1-formylbutyl)-L-alaninamide )	2.00 Å	1W10	1W10	1W10	1W10	1W10	1W10	Zeslawska et al., 2003
complex with inhibitor SK1 (N-(benzylsulfonyl)-D-seryl-N-4-[amino(imino)methyl]benzyl-L-alaninamide)	2.00 Å	1W11	1W11	1W11	1W11	1W11	1W11	Zeslawska et al., 2003
complex with inhibitor SL1 (N-((1S)-4-[aminomethyl]amino-1-formylbutyl)-2-(3R)-3-[(benzylsulfonyl)amino]-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-1-ylacetamide)	2.40 Å	1W12	1W12	1W12	1W12	1W12	1W12	Zeslawska et al., 2003
complex with inhibitor SM1 (N-(benzylsulfonyl)-D-seryl-N-(4-[amino(imino)methyl]aminobenzyl)-L-alaninamide)	2.00 Å	1W13	1W13	1W13	1W13	1W13	1W13	Zeslawska et al., 2003
complex with inhibitor SH1 (N-[(2-phenylethyl)sulfonyl]-D-seryl-N-[(1S)- 4-[(diaminomethylene)amino]-1-(hydroxymethyl)butyl]-L-alaninamide)	2.20 Å	1W14	1W14	1W14	1W14	1W14	1W14	Zeslawska et al., 2003
mature peptidase	1.90 Å	2FD6	2FD6	2FD6	2FD6	2FD6	2FD6	Huai et al., 2006
mature peptidase	1.90 Å	2I9A	2I9A	2I9A	2I9A	2I9A	2I9A	Barinka et al., 2006
mature peptidase	2.80 Å	2I9B	2I9B	2I9B	2I9B	2I9B	2I9B	Barinka et al., 2006
new pharmacophore for serine protease inhibition revealed by crystal structure of human urokinase-type plasminogen activator complexed with a cyclic peptidyl inhibitor, upain-	2.15 Å	2NWN	2NWN	2NWN	2NWN	2NWN	2NWN	Zhao et al., 2007
crystal structure and binding epitopes of urokinase-type plasminogen activator (c122a/n145q) in complex with inhibitors	1.45 Å	2O8T	2O8T	2O8T	2O8T	2O8T	2O8T
crystal structure and binding epitopes of urokinase-type plasminogen activator (c122a/n145q/s195a) in complex with inhibitors	1.70 Å	2O8U	2O8U	2O8U	2O8U	2O8U	2O8U
crystal structure and binding epitopes of urokinase-type plasminogen activator (c122a/n145q/s195a) in complex with inhibitors	1.86 Å	2O8W	2O8W	2O8W	2O8W	2O8W	2O8W
urokinase plasminogen activator b-chain-gppe complex	2.01 Å	2R2W	2R2W	2R2W	2R2W	2R2W	2R2W	Zeslawska et al., 2007
fragment-based discovery of mexiletine derivatives as orally bioavailable inhibitors of urokinase-type plasminogen activator	1.90 Å	2VIN	2VIN	2VIN	2VIN	2VIN	2VIN	Frederickson et al., 2008
fragment-based discovery of mexiletine derivatives as orally bioavailable inhibitors of urokinase-type plasminogen activator	1.80 Å	2VIO	2VIO	2VIO	2VIO	2VIO	2VIO	Frederickson et al., 2008
fragment-based discovery of mexiletine derivatives as orally bioavailable inhibitors of urokinase-type plasminogen activator	1.72 Å	2VIP	2VIP	2VIP	2VIP	2VIP	2VIP	Frederickson et al., 2008
fragment-based discovery of mexiletine derivatives as orally bioavailable inhibitors of urokinase-type plasminogen activator	2.00 Å	2VIQ	2VIQ	2VIQ	2VIQ	2VIQ	2VIQ	Frederickson et al., 2008
fragment-based discovery of mexiletine derivatives as orally bioavailable inhibitors of urokinase-type plasminogen activator	1.72 Å	2VIV	2VIV	2VIV	2VIV	2VIV	2VIV	Frederickson et al., 2008
fragment-based discovery of mexiletine derivatives as orally bioavailable inhibitors of urokinase-type plasminogen activator	2.05 Å	2VIW	2VIW	2VIW	2VIW	2VIW	2VIW	Frederickson et al., 2008
urokinase-type plasminogen activator inhibitor complex with a 1-(7-sulphoamidoisoquinolinyl)guanidine	2.20 Å	2VNT	2VNT	2VNT	2VNT	2VNT	2VNT	Fish et al., 2007
mature peptidase	2.80 Å	3BT1	3BT1	3BT1	3BT1	3BT1	3BT1	Huai et al., 2008
mature peptidase	2.50 Å	3BT2	3BT2	3BT2	3BT2	3BT2	3BT2	Huai et al., 2008
mature peptidase	1.83 Å	3IG6	3IG6	3IG6	3IG6	3IG6	3IG6	West et al., 2009
mature peptidase	2.35 Å	3KGP	3KGP	3KGP	3KGP	3KGP	3KGP
mature peptidase	2.35 Å	3KHV	3KHV	3KHV	3KHV	3KHV	3KHV
mature peptidase	2.71 Å	3KID	3KID	3KID	3KID	3KID	3KID
mature peptidase	1.68 Å	3M61	3M61	3M61	3M61	3M61	3M61
mature peptidase	1.45 Å	3MHW	3MHW	3MHW	3MHW	3MHW	3MHW
mature peptidase	2.03 Å	3MWI	3MWI	3MWI	3MWI	3MWI	3MWI
mature peptidase	1.58 Å	3OX7	3OX7	3OX7	3OX7	3OX7	3OX7	Jiang et al., 2011
mature peptidase	2.31 Å	3OY5	3OY5	3OY5	3OY5	3OY5	3OY5	Jiang et al., 2011
mature peptidase	2.31 Å	3OY6	3OY6	3OY6	3OY6	3OY6	3OY6	Jiang et al., 2011
mature peptidase	2.30 Å	3PB1	3PB1	3PB1	3PB1	3PB1	3PB1	Lin et al., 2011
mature peptidase	1.90 Å	3QN7	3QN7	3QN7	3QN7	3QN7	3QN7	Angelini et al., 2012
mature peptidase	3.19 Å	3U73	3U73	3U73	3U73	3U73	3U73	Xu et al., 2012
mature peptidase	1.94 Å	4DVA	4DVA	4DVA	4DVA	4DVA	4DVA	Jiang et al., 2013
mature peptidase	2.97 Å	4DW2	4DW2	4DW2	4DW2	4DW2	4DW2	Jiang et al., 2013
mature peptidase	2.00 Å	4FU7	4FU7	4FU7	4FU7	4FU7	4FU7
mature peptidase	2.20 Å	4FU8	4FU8	4FU8	4FU8	4FU8	4FU8
mature peptidase	1.60 Å	4FU9	4FU9	4FU9	4FU9	4FU9	4FU9
mature peptidase	1.90 Å	4FUB	4FUB	4FUB	4FUB	4FUB	4FUB
mature peptidase	1.72 Å	4FUC	4FUC	4FUC	4FUC	4FUC	4FUC
mature peptidase	2.00 Å	4FUD	4FUD	4FUD	4FUD	4FUD	4FUD
mature peptidase	2.00 Å	4FUE	4FUE	4FUE	4FUE	4FUE	4FUE
mature peptidase	2.00 Å	4FUF	4FUF	4FUF	4FUF	4FUF	4FUF
mature peptidase	1.80 Å	4FUG	4FUG	4FUG	4FUG	4FUG	4FUG
mature peptidase	1.60 Å	4FUH	4FUH	4FUH	4FUH	4FUH	4FUH
mature peptidase	2.00 Å	4FUI	4FUI	4FUI	4FUI	4FUI	4FUI
mature peptidase	2.05 Å	4FUJ	4FUJ	4FUJ	4FUJ	4FUJ	4FUJ
mature peptidase	1.52 Å	4GLY	4GLY	4GLY	4GLY	4GLY	4GLY	Chen et al., 2013
mature peptidase	2.01 Å	4H42	4H42	4H42	4H42	4H42	4H42
mature peptidase	1.55 Å	4JK5	4JK5	4JK5	4JK5	4JK5	4JK5	Chen et al., 2013
mature peptidase	2.20 Å	4JK6	4JK6	4JK6	4JK6	4JK6	4JK6	Chen et al., 2013
mature peptidase	1.17 Å	4JNI	4JNI	4JNI	4JNI	4JNI	4JNI
mature peptidase	2.00 Å	4JNL	4JNL	4JNL	4JNL	4JNL	4JNL
mature peptidase	4.50 Å	4K24	4K24	4K24	4K24	4K24	4K24	Xu et al., 2014
mature peptidase	1.80 Å	4MNV	4MNV	4MNV	4MNV	4MNV	4MNV	Chen et al., 2014
mature peptidase	1.49 Å	4MNW	4MNW	4MNW	4MNW	4MNW	4MNW	Chen et al., 2014
mature peptidase	1.85 Å	4MNX	4MNX	4MNX	4MNX	4MNX	4MNX	Chen et al., 2014
mature peptidase	1.70 Å	4MNY	4MNY	4MNY	4MNY	4MNY	4MNY	Chen et al., 2014
mature peptidase	2.20 Å	4OS1	4OS1	4OS1	4OS1	4OS1	4OS1	Chen et al., 2014
mature peptidase	1.79 Å	4OS2	4OS2	4OS2	4OS2	4OS2	4OS2	Chen et al., 2014
mature peptidase	2.00 Å	4OS4	4OS4	4OS4	4OS4	4OS4	4OS4	Chen et al., 2014
mature peptidase	2.26 Å	4OS5	4OS5	4OS5	4OS5	4OS5	4OS5	Chen et al., 2014
mature peptidase	1.75 Å	4OS6	4OS6	4OS6	4OS6	4OS6	4OS6	Chen et al., 2014
mature peptidase	2.00 Å	4OS7	4OS7	4OS7	4OS7	4OS7	4OS7	Chen et al., 2014
mature peptidase	2.10 Å	4X0W	4X0W	4X0W	4X0W	4X0W	4X0W	Jiang et al., 2015
mature peptidase	1.80 Å	4X1N	4X1N	4X1N	4X1N	4X1N	4X1N	Zhao et al., 2014
mature peptidase	1.60 Å	4X1P	4X1P	4X1P	4X1P	4X1P	4X1P	Jiang et al., 2015
mature peptidase	2.28 Å	4X1Q	4X1Q	4X1Q	4X1Q	4X1Q	4X1Q	Zhao et al., 2014
mature peptidase	2.10 Å	4X1R	4X1R	4X1R	4X1R	4X1R	4X1R	Zhao et al., 2014
mature peptidase	1.90 Å	4X1S	4X1S	4X1S	4X1S	4X1S	4X1S	Zhao et al., 2014
paitrap, an upa mutant	1.50 Å	4XSK	4XSK	4XSK	4XSK	4XSK	4XSK
mature peptidase	2.06 Å	4ZHL	4ZHL	4ZHL	4ZHL	4ZHL	4ZHL	Sorensen et al., 2015
mature peptidase	1.90 Å	4ZHM	4ZHM	4ZHM	4ZHM	4ZHM	4ZHM	Sorensen et al., 2015
complex with upain-1-w3a at ph5.5	1.36 Å	4ZKN	4ZKN	4ZKN	4ZKN	4ZKN	4ZKN
complex with upain-1-w3a at ph7.4	1.29 Å	4ZKO	4ZKO	4ZKO	4ZKO	4ZKO	4ZKO
complex with upain-1-w3a at ph9.0	1.36 Å	4ZKR	4ZKR	4ZKR	4ZKR	4ZKR	4ZKR
Ser195Ala mutant; complex with upain-1-w3a at ph7.4	1.85 Å	4ZKS	4ZKS	4ZKS	4ZKS	4ZKS	4ZKS
complex with a camelid-derived antibody fragment	1.97 Å	5HGG	5HGG	5HGG	5HGG	5HGG	5HGG
complex with upain-2-2	1.46 Å	5WXF	5WXF	5WXF	5WXF	5WXF	5WXF
complex with upain-2-2-w3a	1.64 Å	5WXO	5WXO	5WXO	5WXO	5WXO	5WXO
complex with upain-2-3-w3a	1.75 Å	5WXP	5WXP	5WXP	5WXP	5WXP	5WXP
complex with upain-2-4	1.79 Å	5WXQ	5WXQ	5WXQ	5WXQ	5WXQ	5WXQ
complex with upain-2-4-w3a	1.75 Å	5WXR	5WXR	5WXR	5WXR	5WXR	5WXR
complex with s2444	2.30 Å	5WXS	5WXS	5WXS	5WXS	5WXS	5WXS
Ser195Ala mutant; complex with s2444	2.10 Å	5WXT	5WXT	5WXT	5WXT	5WXT	5WXT
complex with quercetin	3.00 Å	5XG4	5XG4	5XG4	5XG4	5XG4	5XG4
complex with 4-bromobenzylamirne at pH4.6	1.18 Å	5YC6	5YC6	5YC6	5YC6	5YC6	5YC6
complex with 4-bromobenzylamirne at pH7.4	2.00 Å	5YC7	5YC7	5YC7	5YC7	5YC7	5YC7
complex with 4-iodobenzylamine at pH7.4	1.45 Å	5Z1C	5Z1C	5Z1C	5Z1C	5Z1C	5Z1C
upa-hma	1.70 Å	5ZA7	5ZA7	5ZA7	5ZA7	5ZA7	5ZA7
upa-bb2-27f	1.90 Å	5ZA8	5ZA8	5ZA8	5ZA8	5ZA8	5ZA8
upa-bb2-50f	1.62 Å	5ZA9	5ZA9	5ZA9	5ZA9	5ZA9	5ZA9
upa-6f-hma	1.73 Å	5ZAE	5ZAE	5ZAE	5ZAE	5ZAE	5ZAE
upa-bb2-28f	1.65 Å	5ZAF	5ZAF	5ZAF	5ZAF	5ZAF	5ZAF
upa-bb2-94f	1.95 Å	5ZAG	5ZAG	5ZAG	5ZAG	5ZAG	5ZAG
upa-bb2-30f	2.98 Å	5ZAH	5ZAH	5ZAH	5ZAH	5ZAH	5ZAH
upa-31f	1.65 Å	5ZAJ	5ZAJ	5ZAJ	5ZAJ	5ZAJ	5ZAJ
upa-nu-09f	1.90 Å	5ZC5	5ZC5	5ZC5	5ZC5	5ZC5	5ZC5
tranexamic acid is an active site inhibitor of urokinase plasminogen activator	2.30 Å	6NMB	6NMB	6NMB	6NMB	6NMB	6NMB
Mus musculus
mature peptidase	3.20 Å	3LAQ	3LAQ	3LAQ	3LAQ	3LAQ	3LAQ	Lin et al., 2010
catalytic domain; complex with the allosteric inhibitory nanobody nb7	2.55 Å	5LHN	5LHN	5LHN	5LHN	5LHN	5LHN
catalytic domain; complex with p-aminobenzamidine and the allosteric inhibitory nanobody nb7	2.63 Å	5LHP	5LHP	5LHP	5LHP	5LHP	5LHP
the egr-cmk active site inhibited catalytic domain of murine urokinase-type plasminogen activator in complex with the allosteric inhibitory nanobody nb7	2.60 Å	5LHQ	5LHQ	5LHQ	5LHQ	5LHQ	5LHQ
catalytic domain; complex with the active site binding inhibitory nanobody nb22	2.30 Å	5LHR	5LHR	5LHR	5LHR	5LHR	5LHR
the ligand free catalytic domain of murine urokinase-type plasminogen activator	3.05 Å	5LHS	5LHS	5LHS	5LHS	5LHS	5LHS
complex with mupa-spd at ph8.5	2.53 Å	6A8G	6A8G	6A8G	6A8G	6A8G	6A8G
complex with mupa-spd at ph8.5	2.49 Å	6A8N	6A8N	6A8N	6A8N	6A8N	6A8N