Binding Site Information of Target
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T45299 | Target Info | |||
| Target Name | Tissue-type plasminogen activator (PLAT) | ||||
| Synonyms | TPA; T-plasminogen activator; T-PA; Reteplase; Alteplase | ||||
| Target Type | Successful Target | ||||
| Gene Name | PLAT | ||||
| Biochemical Class | Peptidase | ||||
| UniProt ID | |||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: Aminocaproic acid | Ligand Info | |||||
| Structure Description | SOLUTION STRUCTURE OF THE TISSUE-TYPE PLASMINOGEN ACTIVATOR KRINGLE 2 DOMAIN COMPLEXED TO 6-AMINOHEXANOIC ACID AN ANTIFIBRINOLYTIC DRUG | PDB:1PK2 | ||||
| Method | Solution NMR | Resolution | N.A. | Mutation | No | [1] |
| PDB Sequence |
SEGNSDCYFG
10 NGSAYRGTHS20 LTESGASCLP30 WNSMILIGKV40 YTAQNPSAQA50 LGLGKHNYCR 60 NPDGDAKPWC70 HVLKNRRLTW80 EYCDVPSCST90
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| Ligand Name: Benzamidine | Ligand Info | |||||
| Structure Description | COMPLEX OF BENZAMIDINE WITH THE CATALYTIC DOMAIN OF HUMAN TWO CHAIN TISSUE PLASMINOGEN ACTIVATOR [(TC)-T-PA] | PDB:1RTF | ||||
| Method | X-ray diffraction | Resolution | 2.30 Å | Mutation | No | [2] |
| PDB Sequence |
IKGGLFADIA
25 SHPWQAAIFA35 KHRGERFLCG43 GILISSCWIL53 SAAHCFQERF60C PPHHLTVILG 69 RTYRVVPGEE79 EQKFEVEKYI89 VHKEFDDDTY99 DNDIALLQLK109 SDSSRCAQES 115 SVVRTVCLPP125 ADLQLPDWTE135 CELSGYGKHE145 ALSPFYSERL155 KEAHVRLYPS 165 SRCTSQHLLN173 RTVTDNMLCA183 GDTRSNLHDA190 CQGDSGGPLV200 CLNDGRMTLV 210 GIISWGLGCG221 QKDVPGVYTK230 VTNYLDWIRD240 NMRP
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| Ligand Name: Dansylglutamyl-glycyl-arginine chloromethyl ketone | Ligand Info | |||||
| Structure Description | CATALYTIC DOMAIN OF HUMAN SINGLE CHAIN TISSUE PLASMINOGEN ACTIVATOR IN COMPLEX WITH DANSYL-EGR-CMK (DANSYL-GLU-GLY-ARG CHLOROMETHYL KETONE) | PDB:1BDA | ||||
| Method | X-ray diffraction | Resolution | 3.35 Å | Mutation | No | [3] |
| PDB Sequence |
TCGLRQYSQP
9 QFRIKGGLFA22 DIASHPWQAA32 IFAKHRRSPG37E ERFLCGGILI47 SSCWILSAAH 57 CFQERFPPHH63 LTVILGRTYR73 VVPGEEEQKF83 EVEKYIVHKE93 FDDDTYDNDI 103 ALLQLKSDSS110C RCAQESSVVR119 TVCLPPADLQ129 LPDWTECELS139 GYGKHEALSP 149 FYSERLKEAH159 VRLYPSSRCT169 SQHLLNRTVT177 DNMLCAGDTR186A SGGPQANLHD 189 ACQGDSGGPL199 VCLNDGRMTL209 VGIISWGLGC220 GQKDVPGVYT229 KVTNYLDWIR 239 DNMRP
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .2Z0 or .2Z02 or .2Z03 or :32Z0;style chemicals stick;color identity;select .A:42 or .A:57 or .A:58 or .A:99 or .A:172 or .A:174 or .A:189 or .A:190 or .A:191 or .A:192 or .A:193 or .A:194 or .A:195 or .A:213 or .A:214 or .A:215 or .A:216 or .A:217 or .A:219 or .A:220 or .A:226 or .A:227; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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CYS42
4.883
HIS57
1.516
CYS58
4.101
TYR99
3.102
LEU172
4.503
ARG174
2.989
ASP189
2.733
ALA190
3.037
CYS191
4.211
GLN192
3.799
GLY193
3.151
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| Ligand Name: 2,7-Bis-(4-amidinobenzylidene)-cycloheptan-1-one | Ligand Info | |||||
| Structure Description | CATALYTIC DOMAIN OF HUMAN TWO-CHAIN TISSUE PLASMINOGEN ACTIVATOR COMPLEX OF A BIS-BENZAMIDINE | PDB:1A5H | ||||
| Method | X-ray diffraction | Resolution | 2.90 Å | Mutation | No | [4] |
| PDB Sequence |
IKGGLFADIA
25 SHPWQAAIFA35 KHRRSPGERF40 LCGGILISSC50 WILSAAHCFQ60 ERFPPHHLTV 66 ILGRTYRVVP76 GEEEQKFEVE86 KYIVHKEFDD96 DTYDNDIALL106 QLKSDSSRCA 112 QESSVVRTVC122 LPPADLQLPD132 WTECELSGYG142 KHEALSPFYS152 ERLKEAHVRL 162 YPSSRCTSQH170 LLNRTVTDNM180 LCAGDTRSGG186D PQANLHDACQ192 GDSGGPLVCL 202 NDGRMTLVGI212 ISWGLGCGQK222 DVPGVYTKVT232 NYLDWIRDNM242 RP |
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .BBA or .BBA2 or .BBA3 or :3BBA;style chemicals stick;color identity;select .A:57 or .A:97 or .A:98 or .A:99 or .A:174 or .A:175 or .A:180 or .A:183 or .A:189 or .A:190 or .A:191 or .A:192 or .A:193 or .A:194 or .A:195 or .A:213 or .A:214 or .A:215 or .A:216 or .A:217 or .A:219 or .A:220 or .A:221 or .A:221A or .A:225 or .A:226 or .A:227 or .A:228; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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HIS57
4.484
ASP97
3.403
THR98
2.429
TYR99
2.957
ARG174
3.542
THR175
3.151
MET180
4.715
ALA183
4.976
ASP189
1.909
ALA190
3.090
CYS191
3.910
GLN192
3.660
GLY193
4.082
ASP194
4.975
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| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Solution structure of the tissue-type plasminogen activator kringle 2 domain complexed to 6-aminohexanoic acid an antifibrinolytic drug. J Mol Biol. 1991 Dec 20;222(4):1035-51. | ||||
| REF 2 | The 2.3 A crystal structure of the catalytic domain of recombinant two-chain human tissue-type plasminogen activator. J Mol Biol. 1996 Apr 26;258(1):117-35. | ||||
| REF 3 | Lysine 156 promotes the anomalous proenzyme activity of tPA: X-ray crystal structure of single-chain human tPA. EMBO J. 1997 Aug 15;16(16):4797-805. | ||||
| REF 4 | Structural mapping of the active site specificity determinants of human tissue-type plasminogen activator. Implications for the design of low molecular weight substrates and inhibitors. J Biol Chem. 1997 Aug 29;272(35):21713-9. | ||||
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