Target Information
| Target General Information | Top | |||||
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| Target ID |
T75273
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| Target Name |
Staphylococcus DNA gyrase A (Stap-coc gyrA)
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| Synonyms |
Stap-coc DNA gyrase subunit A
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| Gene Name |
Stap-coc gyrA
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Impetigo [ICD-11: 1B72] | |||||
| Function |
A type II topoisomerase that negatively supercoils closed circular double-stranded (ds) DNA in an ATP-dependent manner to modulate DNA topology and maintain chromosomes in an underwound state. Negative supercoiling favors strand separation, and DNA replication, transcription, recombination and repair, all of which involve strand separation. Also able to catalyze the interconversion of other topological isomers of dsDNA rings, including catenanes and knotted rings. Type II topoisomerases break and join 2 DNA strands simultaneously in an ATP-dependent manner.
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| UniProt ID | ||||||
| EC Number |
EC 5.6.2.3
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| Sequence |
MAELPQSRINERNITSEMRESFLDYAMSVIVARALPDVRDGLKPVHRRILYGLNEQGMTP
DKSYKKSARIVGDVMGKYHPHGDSSIYEAMVRMAQDFSYRYPLVDGQGNFGSMDGDGAAA MRYTEARMTKITLELLRDINKDTIDFIDNYDGNEREPSVLPARFPNLLANGASGIAVGMA TNIPPHNLTELINGVLSLSKNPDISIAELMEDIEGPDFPTAGLILGKSGIRRAYETGRGS IQMRSRAVIEERGGGRQRIVVTEIPFQVNKARMIEKIAELVRDKKIDGITDLRDETSLRT GVRVVIDVRKDANASVILNNLYKQTPLQTSFGVNMIALVNGRPKLINLKEALVHYLEHQK TVVRRRTQYNLRKAKDRAHILEGLRIALDHIDEIISTIRESDTDKVAMESLQQRFKLSEK QAQAILDMRLRRLTGLERDKIEAEYNELLNYISELEAILADEEVLLQLVRDELTEIRDRF GDDRRTEIQLGGFEDLEDEDLIPEEQIVITLSHNNYIKRLPVSTYRAQNRGGRGVQGMNT LEEDFVSQLVTLSTHDHVLFFTNKGRVYKLKGYEVPELSRQSKGIPVVNAIELENDEVIS TMIAVKDLESEDNFLVFATKRGVVKRSALSNFSRINRNGKIAISFREDDELIAVRLTSGQ EDILIGTSHASLIRFPESTLRPLGRTATGVKGITLREGDEVVGLDVAHANSVDEVLVVTE NGYGKRTPVNDYRLSNRGGKGIKTATITERNGNVVCITTVTGEEDLMIVTNAGVIIRLDV ADISQNGRAAQGVRLIRLGDDQFVSTVAKVKEDAEDETNEDEQSTSTVSEDGTEQQREAV VNDETPGNAIHTEVIDSEENDEDGRIEVRQDFMDRVEEDIQQSLDEDEE Click to Show/Hide
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| Drugs and Modes of Action | Top | |||||
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| Approved Drug(s) | [+] 1 Approved Drugs | + | ||||
| 1 | Ozenoxacin | Drug Info | Approved | Impetigo | [1] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Inhibitor | [+] 1 Inhibitor drugs | + | ||||
| 1 | Ozenoxacin | Drug Info | [1] | |||
| Drug Binding Sites of Target | Top | |||||
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| Ligand Name: N-[(4-chlorophenyl)methyl]-1-[2-(6-methoxy-1,5-naphthyridin-4-yl)ethyl]piperidin-4-amine | Ligand Info | |||||
| Structure Description | Ternary complex of Staphylococcus aureus DNA gyrase with AMK12 and DNA | PDB:6Z1A | ||||
| Method | X-ray diffraction | Resolution | 2.30 Å | Mutation | Yes | [2] |
| PDB Sequence |
KLADCSSKSP
426 EECEIFLVEG436 DSAGGSTKSG446 RDSRTQAILP456 LRGKILNVEK466 ARLDRILNNN 476 EIRQMITAFG486 TGIGGDFDLA496 KARYHKIVIM506 TDADVDGAHI516 RTLLLTFFYR 526 FMRPLIEAGY536 VYIAQPPTGY580 KGLGEMNADQ590 LWETTMNPEH600 RALLQVKLED 610 AIEADQTFEM620 LMGDVVENRR630 QFIEDNAVYN1010 ERNITSEMRE1020 SFLDYAMSVI 1030 VARALPDVRD1040 GLKPVHRRIL1050 YGLNEQGMTP1060 DKSYKKSARI1070 VGDVMGKYHP 1080 HGDSSIYEAM1090 VRMAQDFSYR1100 YPLVDGQGNF1110 GSMDGDGAAA1120 MRFTEARMTK 1130 ITLELLRDIN1140 KDTIDFIDNY1150 DGNEREPSVL1160 PARFPNLLAN1170 GASGIAVGMA 1180 TNIPPHNLTE1190 LINGVLSLSK1200 NPDISIAELM1210 EDIEGPDFPT1220 AGLILGKSGI 1230 RRAYETGRGS1240 IQMRSRAVIE1250 ERGGGRQRIV1260 VTEIPFQVNK1270 ARMIEKIAEL 1280 VRDKKIDGIT1290 DLRDETSLRT1300 GVRVVIDVRK1310 DANASVILNN1320 LYKQTPLQTS 1330 FGVNMIALVN1340 GRPKLINLKE1350 ALVHYLEHQK1360 TVVRRRTQYN1370 LRKAKDRAHI 1380 LEGLRIALDH1390 IDEIISTIRE1400 SDTDKVAMES1410 LQQRFKLSEK1420 QAQAILDMRL 1430 RRLTGLERDK1440 IEAEYNELLN1450 YISELEAILA1460 DEEVLLQLVR1470 DELTEIRDRF 1480 GDDRRTEIQL1490 G
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| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Similarity Proteins
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There is no similarity protein (E value < 0.005) for this target
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| Chemical Structure based Activity Landscape of Target | Top |
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| References | Top | |||||
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| REF 1 | 2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85. | |||||
| REF 2 | Potent DNA gyrase inhibitors bind asymmetrically to their target using symmetrical bifurcated halogen bonds. Nat Commun. 2021 Jan 8;12(1):150. | |||||
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