Target Information

Target General Infomation
Target ID
T40696
Former ID
TTDS00083
Target Name
Topoisomerase IV
Gene Name
parC
Synonyms
Topo IV; parC
Target Type
Successful
Disease Bacterial pneumonia [ICD10: J13, J15]
Bacterial infections [ICD9: 001-009, 010-018, 020-027, 030-041, 080-088, 090-099, 100-104; ICD10: A00-B99]
Methicillin-resistant staphylococcus aureus infection [ICD10: B95.62]
Mrsa infection [ICD9: 41.12; ICD10: A49.02]
Ocular inflammation [ICD9: 370.33; ICD10: H16.229]
Pneumonia [ICD10: J12-J18]
Respiratory tract infection [ICD9: 460-519; ICD10: J00-J99]
Respiratory tract inflammation [ICD10: J00-J99]
Urinary tract infections [ICD9: 599; ICD10: N39.0]
Unspecified [ICD code not available]
BioChemical Class
Topoisomerase GyrA ParC
Target Validation
T40696
UniProt ID
Q6G9K4
EC Number
EC 5.99.1.-
Sequence
MSEIIQDLSLEDVLGDRFGRYSKYIIQERALPDVRDGLKPVQRRILYAMYSSGNTHDKNF
RKSAKTVGDVIGQYHPHGDSSVYEAMVRLSQDWKLRHVLIEMHGNNGSIDNDPPAAMRYT
EAKLSLLAEELLRDINKETVSFIPNYDDTTLEPMVLPSRFPNLLVNGSTGISAGYATDIP
PHNLAEVIQATLKYIDNPDITVNQLMKYIKGPDFPTGGIIQGIDGIKKAYESGKGRIIVR
SKVEEETLRNGRKQLIITEIPYEVNKSSLVKRIDELRADKKVDGIVEVRDETDRTGLRIA
IELKKDVNSESIKNYLYKNSDLQISYNFNMVAISDGRPKLMGIRQIIDSYLNHQIEVVAN
RTKFELDNAEKRMHIVEGLIKALSILDKVIELIRSSKNKRDAKENLIEVYEFTEEQAEAI
VMLQLYRLTNTDIVALEGEHKELEALIKQLRHILDNHDALLNVIKEELNEIKKKFKSERL
SLIEAEIEEIKIDKEVMVPSEEVILSMTRHGYIKRTSIRSFNASGVEDIGLKDGDSLLKH
QEVNTQDTVLVFTNKGRYLFIPVHKLADIRWKELGQHVSQIVPIEEDEVVINVFNEKDFN
TDAFYVFATQNGMIKKSTVPLFKTTRFNKPLIATKVKENDDLISVMRFEKDQLITVITNK
GMSLTYNTSELSDTGLRAAGVKSINLKAEDFVVVTEGVSENDTILMATQRGSLKRISFKI
LQVAKRAQRGITLLKELKKNPHRIVAAHVVTGEHSQYTLYSKSNEEHGLINDIHKSEQYT
NGSFIVDTDDFGEVIDMYIS
Drugs and Mode of Action
Drug(s) Besifloxacin Drug Info Approved Ocular inflammation [530677], [531950]
Ciprofloxacin Hydrochloride Drug Info Approved Bacterial infections [551871]
Finafloxacin Drug Info Approved Urinary tract infections [533123], [551871]
Gatifloxacin Drug Info Approved Respiratory tract infection [536472]
Gemifloxacin Drug Info Approved Bacterial infections [536094]
Levofloxacin Drug Info Approved Bacterial infections [536773]
Moxifloxacin Drug Info Approved Bacterial infections [536472]
Sparfloxacin Drug Info Approved Bacterial infections [538553]
ABT-492 Drug Info Phase 3 Bacterial infections [546643]
Ciprofloxacin intratympanic - Otonomy Drug Info Phase 3 Unspecified [1559538]
Nemonaxacin Drug Info Phase 3 Methicillin-resistant staphylococcus aureus infection [524857]
Ozenoxacin Drug Info Phase 3 Bacterial infections [524682]
Zabofloxacin Drug Info Phase 3 Pneumonia [524004]
WCK-2349 Drug Info Phase 2 Mrsa infection [549471]
WCK-771 Drug Info Phase 2 Bacterial infections [547481]
WCK-1152 Drug Info Phase 1 Respiratory tract inflammation [547780]
Avarofloxacin Drug Info Discontinued in Phase 2 Bacterial pneumonia [549103]
DX-619 Drug Info Discontinued in Phase 2 Bacterial infections [547823]
DK-507k Drug Info Discontinued in Phase 1 Bacterial infections [547478]
CBR-2092 Drug Info Terminated Bacterial infections [548625]
Modulator ABT-492 Drug Info
Avarofloxacin Drug Info [531620]
Besifloxacin Drug Info [530677], [531950]
CBR-2092 Drug Info
Ciprofloxacin Hydrochloride Drug Info [556264]
Ciprofloxacin intratympanic - Otonomy Drug Info
DK-507k Drug Info
DX-619 Drug Info [527893]
Finafloxacin Drug Info [533123]
Gatifloxacin Drug Info [556264]
Gemifloxacin Drug Info [556264]
Levofloxacin Drug Info [556264]
Moxifloxacin Drug Info [556264]
Nemonaxacin Drug Info
NSFQ-105 Drug Info
Ozenoxacin Drug Info
Sparfloxacin Drug Info [556264]
WCK-1152 Drug Info
WCK-2349 Drug Info
WCK-771 Drug Info
Zabofloxacin Drug Info
Inhibitor Premafloxacin Drug Info [535701]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
DRM DRM Info
References
Ref 524004ClinicalTrials.gov (NCT01658020) A Study to Evaluate Efficacy and Safety Profile of Zabofloxacin Tablet 400mg and Moxifloxacin Tablet 400mg. U.S. National Institutes of Health.
Ref 524682ClinicalTrials.gov (NCT02090764) Efficacy and Safety of Ozenoxacin 1% Cream Versus Placebo in the Treatment of Patients With Impetigo. U.S. National Institutes of Health.
Ref 524857ClinicalTrials.gov (NCT02205112) A Phase III Study to Evaluate the Efficacy and Safety of Intravenous Infusion of Nemonoxacin in Treating CAP. U.S. National Institutes of Health.
Ref 530677Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
Ref 531950Besifloxacin ophthalmic suspension, 0.6%: a novel topical fluoroquinolone for bacterial conjunctivitis. Adv Ther. 2012 Jun;29(6):473-90.
Ref 5331232014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
Ref 536094Emerging drugs for bacterial urinary tract infections. Expert Opin Emerg Drugs. 2005 May;10(2):275-98.
Ref 536472Novel agents in the management of Mycobacterium tuberculosis disease. Curr Med Chem. 2007;14(18):2000-8.
Ref 536773How many modes of action should an antibiotic have? Curr Opin Pharmacol. 2008 Oct;8(5):564-73. Epub 2008 Jul 30.
Ref 538553FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 020677.
Ref 546643Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009417)
Ref 547478Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016728)
Ref 547481Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016734)
Ref 547780Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019222)
Ref 547823Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019670)
Ref 548625Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027165)
Ref 549103Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032241)
Ref 549471Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800038027)
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 1559538DOI: 10.1093/jac/48.4.479
Ref 527893DX-619, a novel des-fluoro(6) quinolone manifesting low frequency of selection of resistant Staphylococcus aureus mutants: quinolone resistance beyond modification of type II topoisomerases. Antimicrob Agents Chemother. 2005 Dec;49(12):5051-7.
Ref 530677Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
Ref 531620Antistaphylococcal activities of the new fluoroquinolone JNJ-Q2. Antimicrob Agents Chemother. 2011 Dec;55(12):5512-21.
Ref 531950Besifloxacin ophthalmic suspension, 0.6%: a novel topical fluoroquinolone for bacterial conjunctivitis. Adv Ther. 2012 Jun;29(6):473-90.
Ref 5331232014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
Ref 535701Alteration of Escherichia coli topoisomerase IV to novobiocin resistance. Antimicrob Agents Chemother. 2003 Mar;47(3):941-7.
Ref 556264Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.

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