Target Binding Site Detail
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T65818 | Target Info | |||
| Target Name | Endoplasmic reticulum aminopeptidase 2 (ERAP2) | ||||
| Synonyms | Leukocyte-derived arginine aminopeptidase; LRAP; L-RAP | ||||
| Target Type | Literature-reported Target | ||||
| Gene Name | ERAP2 | ||||
| Biochemical Class | Peptidase | ||||
| UniProt ID | |||||
| Ligand General Information | Top | ||||
|---|---|---|---|---|---|
| Ligand Name | L-lysine | Ligand Info | |||
| Canonical SMILES | C(CCN)CC(C(=O)O)N | ||||
| InChI | 1S/C6H14N2O2/c7-4-2-1-3-5(8)6(9)10/h5H,1-4,7-8H2,(H,9,10)/t5-/m0/s1 | ||||
| InChIKey | KDXKERNSBIXSRK-YFKPBYRVSA-N | ||||
| PubChem Compound ID | 5962 | ||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| PDB ID: 3SE6 Crystal structure of the human Endoplasmic Reticulum Aminopeptidase 2 | ||||||
| Method | X-ray diffraction | Resolution | 3.08 Å | Mutation | Yes | [1] |
| PDB Sequence |
PVATNGERFP
63 WQELRLPSVV73 IPLHYDLFVH83 PNLTSLDFVA93 SEKIEVLVSN103 ATQFIILHSK 113 DLEITNATLQ123 SEEYMKPGKE136 LKVLSYPAHE146 QIALLVPEKL156 TPHLKYYVAM 166 DFQAKLGDGF176 EGFYKSTYRT186 LGGETRILAV196 TDFEPTQARM206 AFPCFDEPLF 216 KANFSIKIRR226 ESRHIALSNM236 PKVKTIELEG246 GLLEDHFETT256 VKMSTYLVAY 266 IVCDFHSLSG276 FTSSGVKVSI286 YASPDKRNQT296 HYALQASLKL306 LDFYEKYFDI 316 YYPLSKLDLI326 AIPDFAPGAM336 ENWGLITYRE346 TSLLFDPKTS356 SASDKLWVTR 366 VIAHELAHQW376 FGNLVTMEWW386 NDIWLNEGFA396 KYMELIAVNA406 TYPELQFDDY 416 FLNVCFEVIT426 KDSLNSSRPI436 SKPAETPTQI446 QEMFDEVSYN456 KGACILNMLK 466 DFLGEEKFQK476 GIIQYLKKFS486 YRNAKNDDLW496 SSLSNSLGEN531 AEVKEMMTTW 541 TLQKGIPLLV551 VKQDGCSLRL561 QQERFLQGQE582 RYLWHIPLTY592 STSSSNVIHR 602 HILKSKTDTL612 DLPEKTSWVK622 FNVDSNGYYI632 VHYEGHGWDQ642 LITQLNQNHT 652 LLRPKDRVGL662 IHDVFQLVGA672 GRLTLDKALD682 MTYYLQHETS692 SPALLEGLSY 702 LESFYHMMDR712 RNISDISENL722 KRYLLQYFKP732 VIDRQSWSDK742 GSVWDRMLRS 752 ALLKLACDLN762 HAPCIQKAAE772 LFSQWMESSG782 KLNIPTDVLK792 IVYSVGAQTT 802 AGWNYLLEQY812 ELSMSSAEQN822 KILYALSTSK832 HQEKLLKLIE842 LGMEGKVIKT 852 QNLAALLHAI862 ARRPKGQQLA872 WDFVRENWTH882 LLKKFDLGSY892 DIRMIISGTT 902 AHFSSKDKLQ912 EVKLFFESLE922 AQGSHLDIFQ932 TVLETITKNI942 KWLEKNLPTL 952 RTWLMVNTR
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| PDB ID: 4E36 Crystal structure of the human Endoplasmic Reticulum Aminopeptidase 2 variant N392K | ||||||
| Method | X-ray diffraction | Resolution | 3.22 Å | Mutation | No | [2] |
| PDB Sequence |
PVATNGERFP
63 WQELRLPSVV73 IPLHYDLFVH83 PNLTSLDFVA93 SEKIEVLVSN103 ATQFIILHSK 113 DLEITNATLQ123 SEEYMKPGKE136 LKVLSYPAHE146 QIALLVPEKL156 TPHLKYYVAM 166 DFQAKLGDGF176 EGFYKSTYRT186 LGGETRILAV196 TDFEPTQARM206 AFPCFDEPLF 216 KANFSIKIRR226 ESRHIALSNM236 PKVKTIELEG246 GLLEDHFETT256 VKMSTYLVAY 266 IVCDFHSLSG276 FTSSGVKVSI286 YASPDKRNQT296 HYALQASLKL306 LDFYEKYFDI 316 YYPLSKLDLI326 AIPDFAPGAM336 ENWGLITYRE346 TSLLFDPKTS356 SASDKLWVTR 366 VIAHELAHQW376 FGNLVTMEWW386 NDIWLKEGFA396 KYMELIAVNA406 TYPELQFDDY 416 FLNVCFEVIT426 KDSLNSSRPI436 SKPAETPTQI446 QEMFDEVSYN456 KGACILNMLK 466 DFLGEEKFQK476 GIIQYLKKFS486 YRNAKNDDLW496 SSLSNSLGEN531 AEVKEMMTTW 541 TLQKGIPLLV551 VKQDGCSLRL561 QQERFLQGQE582 RYLWHIPLTY592 STSSSNVIHR 602 HILKSKTDTL612 DLPEKTSWVK622 FNVDSNGYYI632 VHYEGHGWDQ642 LITQLNQNHT 652 LLRPKDRVGL662 IHDVFQLVGA672 GRLTLDKALD682 MTYYLQHETS692 SPALLEGLSY 702 LESFYHMMDR712 RNISDISENL722 KRYLLQYFKP732 VIDRQSWSDK742 GSVWDRMLRS 752 ALLKLACDLN762 HAPCIQKAAE772 LFSQWMESSG782 KLNIPTDVLK792 IVYSVGAQTT 802 AGWNYLLEQY812 ELSMSSAEQN822 KILYALSTSK832 HQEKLLKLIE842 LGMEGKVIKT 852 QNLAALLHAI862 ARRPKGQQLA872 WDFVRENWTH882 LLKKFDLGSY892 DIRMIISGTT 902 AHFSSKDKLQ912 EVKLFFESLE922 AQGSHLDIFQ932 TVLETITKNI942 KWLEKNLPTL 952 RTWLMVNTR
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| PDB ID: 6EA4 ERAP2 bound to Aryl Sulfonamide Uncompetitive Inhibitor | ||||||
| Method | X-ray diffraction | Resolution | 2.45 Å | Mutation | Yes | [3] |
| PDB Sequence |
FPVATNGERF
62 PWQELRLPSV72 VIPLHYDLFV82 HPNLTSLDFV92 ASEKIEVLVS102 NATQFIILHS 112 KDLEITNATL122 QSEEDSRYMK132 PGKELKVLSY142 PAHEQIALLV152 PEKLTPHLKY 162 YVAMDFQAKL172 GDGFEGFYKS182 TYRTLGGETR192 ILAVTDFEPT202 QARMAFPCFD 212 EPLFKANFSI222 KIRRESRHIA232 LSNMPKVKTI242 ELEGGLLEDH252 FETTVKMSTY 262 LVAYIVCDFH272 SLSGFTSSGV282 KVSIYASPDK292 RNQTHYALQA302 SLKLLDFYEK 312 YFDIYYPLSK322 LDLIAIPDFA332 PGAMENWGLI342 TYRETSLLFD352 PKTSSASDKL 362 WVTRVIAHEL372 AHQWFGNLVT382 MEWWNDIWLN392 EGFAKYMELI402 AVNATYPELQ 412 FDDYFLNVCF422 EVITKDSLNS432 SRPISKPAET442 PTQIQEMFDE452 VSYNKGACIL 462 NMLKDFLGEE472 KFQKGIIQYL482 KKFSYRNAKN492 DDLWSSLSNE530 NAEVKEMMTT 540 WTLQKGIPLL550 VVKQDGCSLR560 LQQERFLQGV570 FQEDPEWRAL580 QERYLWHIPL 590 TYSTSSSNVI600 HRHILKSKTD610 TLDLPEKTSW620 VKFNVDSNGY630 YIVHYEGHGW 640 DQLITQLNQN650 HTLLRPKDRV660 GLIHDVFQLV670 GAGRLTLDKA680 LDMTYYLQHE 690 TSSPALLEGL700 SYLESFYHMM710 DRRNISDISE720 NLKRYLLQYF730 KPVIDRQSWS 740 DKGSVWDRML750 RSALLKLACD760 LNHAPCIQKA770 AELFSQWMES780 SGKLNIPTDV 790 LKIVYSVGAQ800 TTAGWNYLLE810 QYELSMSSAE820 QNKILYALST830 SKHQEKLLKL 840 IELGMEGKVI850 KTQNLAALLH860 AIARRPKGQQ870 LAWDFVRENW880 THLLKKFDLG 890 SYDIRMIISG900 TTAHFSSKDK910 LQEVKLFFES920 LEAQGSHLDI930 FQTVLETITK 940 NIKWLEKNLP950 TLRTWLMVNT960 RHH
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| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | The crystal structure of human endoplasmic reticulum aminopeptidase 2 reveals the atomic basis for distinct roles in antigen processing. Biochemistry. 2012 Jan 10;51(1):286-95. | ||||
| REF 2 | A common single nucleotide polymorphism in endoplasmic reticulum aminopeptidase 2 induces a specificity switch that leads to altered antigen processing. J Immunol. 2012 Sep 1;189(5):2383-92. | ||||
| REF 3 | Crystal structure of human ER aminopeptidase 1 bound to aryl sulfonamide inhibitor. | ||||
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