Target
DNA topoisomerase 4 subunit A [V210L]/B
Ligand
BDBM21689
Substrate
Kinetoplast DNA
Meas. Tech.
DNA Topoisomerase IV Assay
pH
7.5±n/a
Temperature
303.15±n/a K
IC50
4200±n/a nM
Citation
 Butler, MMLamarr, WAFoster, KABarnes, MHSkow, DJLyden, PTKustigian, LMZhi, CBrown, NCWright, GEBowlin, TL Antibacterial activity and mechanism of action of a novel anilinouracil-fluoroquinolone hybrid compound. Antimicrob Agents Chemother 51:119-27 (2007) [PubMed]  Article 
Target
Name:
DNA topoisomerase 4 subunit A [V210L]/B
Synonyms:
DNA Topoisomerase IV
Type:
Protein Complex
Mol. Mass.:
n/a
Description:
The parC and parE subunits of B. subtilis topoisomerase IV were purified from recombinant strains and combined to form active heterodimers.
Components:
This complex has 2 components.
Component 1
Name:
DNA topoisomerase 4 subunit A [V210L]
Synonyms:
DNA Topoisomerase IV Chain A | PARC_BACSU | grlA | parC
Type:
Enzyme Subunit
Mol. Mass.:
91336.01
Organism:
Bacillus subtilis
Description:
Q45066[V210L]
Residue:
806
Sequence:
MSQPELFHDLPLEEVIGDRFGRYSKYIIQDRALPDARDGLKPVQRRILYAMHTDGNTFDKNFRKAAKTVGNVIGNYHPHGDSSVYEAMVRMSQDWKVRNVLIEMHGNNGSIDGDPPAAMRYTEARLSPIASELLRDIDKNTVEFVPNFDDTSKEPVVLPAMFPNLLVNGSTGISAGYATDIPPHHLGEVIDAVIKRIQMPSCSVDELMELIKGPDFPTGGIIQGVDGIRKAYETGKGKIIIRGKAEIETIRGGREQIVITEIPFEVNKANLVKKMDEFRIDKKVEGISEVRDETDRTGLRVVIELKKEADAKGILNFLYKNTDLQITYNFNMVAIHNRRPMLMSLPSILDAYIGHQKEVVTNRSVYELQKAKDRHHIVEGLMKALSILDEVIATIRSSSDKRDAKNNLIAKYEFTEPQAEAIVSLQLYRLTNTDITALKEEAEELGKKIEELESILSNDKKLLKVITNSLKALKKKYADTRRSVIEEKIEEIKINLEVMVASEDVYVTVTKDGYLKRTSQRSFAASNGQDFGMKDTDRMLHQFEMNTTDVLLLFTNKGSYIYCPVHQLPDIRWKDMGQHFSNLITIDRDETIVKAIPIKEFDPSAYLLFFTKNGMVKKTELTHYKAQRYSKALVALNLKGEDELIDVHVTNGESQIFMATHLGYGLWFGEDEVNVVGARAAGVKGINLKEDDFVVSGEILQQSDSIVLFTQRGAVKRMSLSEFEKTSRAKRGVVMLRELKKNPHRVVALFACGLEQRLMAETEKGDRKELQTKELRTNDRYSNGSFFFDEEESGKVTAVWRLHTEQ
  
Component 2
Name:
DNA topoisomerase 4 subunit B
Synonyms:
DNA Topoisomerase IV Chain B | PARE_BACSU | grlB | parE
Type:
Enzyme Subunit
Mol. Mass.:
73006.28
Organism:
Bacillus subtilis
Description:
n/a
Residue:
655
Sequence:
MARKQQFDYNEDAIQVLEGLEAVRKRPGMYIGSTDARGLHHLVYEIVDNSVDEVLAGHGDHIIVKIHKDNSISVQDRGRGMPTGMHKLGKPTPEVILTVLHAGGKFGQGGYKTSGGLHGVGASVVNALSEWLTVTIERDGFVYQQRFENGGKPVTSLEKIGKTKKTGTLTHFKPDPTMFSTTTYNFETLSERLRESAFLLKGLKIELIDERNDQREVFYYENGIEAFVAYLNEEKDVLSEVVSFEGEHHSIEVDFAFQFNDGYSENILSFVNNVRTKDGGTHESGAKTAMTRAFNEYARKVALLKEKDKNLEGTDIREGLSAIISVRIPEELLQFEGQTKGKLGTSEARSAVDAIVSEQLAYFLEENRDTATLLVKKAIKASQAREAARKAREEARSGKKRKKSEATLSGKLTPAGSRNPAKNELYLVEGDSAGGSAKQGRDRRFQAVLPLRGKVINTEKAKLADIFKNEEINTIIHAIGGGVGADFSIDDINYDKIIIMTDADTDGAHIQVLLLTFFYRYMKPLIEHGKVFIALPPLYKVSKGSGKKEIIEYAWSDEEMGDVLKKVGKGYTIQRYKGLGEMNADQLWETTMNPESRTLVRVKIDDAARVERRVTTLMGDKVEPRRKWIEKNVAFGLDEESNILENENLSVAEEV
  
Inhibitor
Name:
BDBM21689
Synonyms:
1-cyclopropyl-6,8-difluoro-7-(3-methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid | 340E | AMQ2 | PD125275
Type:
Small organic molecule
Emp. Form.:
C18H19F2N3O3
Mol. Mass.:
363.3586
SMILES:
CC1CN(CCN1)c1c(F)cc2c(c1F)n(cc(C(O)=O)c2=O)C1CC1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Kinetoplast DNA
Synonyms:
KDNA (catenated)
Type:
Duplex DNA
Mol. Mass.:
358.43
Organism:
Crithidia fasciculata
Description:
n/a
Residue:
3
Sequence:
NA