Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T02228
|
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| Former ID |
TTDS00084
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| Target Name |
Topoisomerase IV subunit A
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| Gene Name |
parC
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| Synonyms |
DNA topoisomerase IV; parC
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| Target Type |
Clinical Trial
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| Disease | Bacterial infections [ICD9: 001-009, 010-018, 020-027, 030-041, 080-088, 090-099, 100-104; ICD10: A00-B99] | ||||
| Cystic fibrosis [ICD9: 277; ICD10: E84] | |||||
| Otitis externa [ICD10: H60] | |||||
| Function |
Topoisomerase IV is essential for chromosome segregation. It relaxes supercoiled DNA. Performs the decatenation events required during the replication of a circular DNA molecule.
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| BioChemical Class |
Topoisomerase GyrA ParC
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| Target Validation |
T02228
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| UniProt ID | |||||
| EC Number |
EC 5.99.1.-
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| Sequence |
MSNIQNMSLEDIMGERFGRYSKYIIQDRALPDIRDGLKPVQRRILYSMNKDSNTFDKSYR
KSAKSVGNIMGNFHPHGDSSIYDAMVRMSQNWKNREILVEMHGNNGSMDGDPPAAMRYTE ARLSEIAGYLLQDIEKKTVPFAWNFDDTEKEPTVLPAAFPNLLVNGSTGISAGYATDIPP HNLAEVIDAAVYMIDHPTAKIDKLMEFLPGPDFPTGAIIQGRDEIKKAYETGKGRVVVRS KTEIEKLKGGKEQIVIIEIPYEINKANLVKKIDDVRVNNKVAGIAEVRDESDRDGLRIAI ELKKDANTELVLNYLFKYTDLQINYNFNMVAIDNFTPRQVGIVPILSSYIAHRREVILAR SRFDKEKAEKRLHIVEGLIRVISILDEVIALIRASENKADAKENLKVSYDFTEEQAEAIV TLQLYRLTNTDVVVLQEEEAELREKIAMLAAIIGDERTMYNLMKKELREVKKKFATPRLS SLEDTAKAIEIDTASLIAEEDTYVSVTKAGYIKRTSPRSFAASTLEEIGKRDDDRLIFVQ SAKTTQHLLMFTSLGNVIYRPIHELADIRWKDIGEHLSQTITNFETNEEILYVEVLDQFD DATTYFAVTRLGQIKRVERKEFTPWRTYRSKSVKYAKLKDDTDQIVAVAPIKLDDVVLVS QNGYALRFNIEEVPVVGAKAAGVKAMNLKEDDVLQSGFICNTSSFYLLTQRGSLKRVSIE EILATSRAKRGLQVLRELKNKPHRVFLAGAVAEQGFVGDFFSTEVDVNDQTLLVQSNKGT IYESRLQDLNLSERTSNGSFISDTISDEEVFDAYLQEVVTEDK |
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| Drugs and Mode of Action | |||||
| Drug(s) | Cetraxal Otic | Drug Info | Phase 3 | Otitis externa | [1], [2] |
| Inhaled liposomal ciprofloxacin | Drug Info | Phase 2 | Cystic fibrosis | [3] | |
| Modulator | Cetraxal Otic | Drug Info | [1], [2], [4] | ||
| Inhaled liposomal ciprofloxacin | Drug Info | [4] | |||
| Inhibitor | Premafloxacin | Drug Info | [5] | ||
| Pumiliotoxin 251D | Drug Info | [6] | |||
| References | |||||
| REF 1 | DNA topoisomerases and their poisoning by anticancer and antibacterial drugs. Chem Biol. 2010 May 28;17(5):421-33. | ||||
| REF 2 | DNA gyrase, topoisomerase IV, and the 4-quinolones. Microbiol Mol Biol Rev. 1997 Sep;61(3):377-92. | ||||
| REF 3 | Inhaled Ciprofloxacin for the Management of Infections in Non-Cystic Fibrosis Bronchiectasis (BE) Patients | ||||
| REF 4 | Selective Targeting of Topoisomerase IV and DNA Gyrase in Staphylococcus aureus: Different Patterns of Quinolone- Induced Inhibition of DNA Synthesis. Antimicrob Agents Chemother. 2000 August; 44(8):2160-2165. | ||||
| REF 5 | Alteration of Escherichia coli topoisomerase IV to novobiocin resistance. Antimicrob Agents Chemother. 2003 Mar;47(3):941-7. | ||||
| REF 6 | How many modes of action should an antibiotic have? Curr Opin Pharmacol. 2008 Oct;8(5):564-73. Epub 2008 Jul 30. | ||||
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