Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTFK8YB)

• DTT Name: Bacterial DNA topoisomerase 4A (Bact parC)
• Synonyms: parC; Topoisomerase IV subunit A of Escherichia coli
• Gene Name: Bact parC
• DTT Type: Successful target; [1]
• BioChemical Class: Topoisomerase GyrA ParC
• UniProt ID: PARC_ECOLI
• TTD ID: T72545
• EC Number: EC 5.6.2.3
• Sequence:
  MSDMAERLALHEFTENAYLNYSMYVIMDRALPFIGDGLKPVQRRIVYAMSELGLNASAKF
  KKSARTVGDVLGKYHPHGDSACYEAMVLMAQPFSYRYPLVDGQGNWGAPDDPKSFAAMRY
  TESRLSKYSELLLSELGQGTADWVPNFDGTLQEPKMLPARLPNILLNGTTGIAVGMATDI
  PPHNLREVAQAAIALIDQPKTTLDQLLDIVQGPDYPTEAEIITSRAEIRKIYENGRGSVR
  MRAVWKKEDGAVVISALPHQVSGARVLEQIAAQMRNKKLPMVDDLRDESDHENPTRLVIV
  PRSNRVDMDQVMNHLFATTDLEKSYRINLNMIGLDGRPAVKNLLEILSEWLVFRRDTVRR
  RLNYRLEKVLKRLHILEGLLVAFLNIDEVIEIIRNEDEPKPALMSRFGLTETQAEAILEL
  KLRHLAKLEEMKIRGEQSELEKERDQLQGILASERKMNNLLKKELQADAQAYGDDRRSPL
  QEREEAKAMSEHDMLPSEPVTIVLSQMGWVRSAKGHDIDAPGLNYKAGDSFKAAVKGKSN
  QPVVFVDSTGRSYAIDPITLPSARGQGEPLTGKLTLPPGATVDHMLMESDDQKLLMASDA
  GYGFVCTFNDLVARNRAGKALITLPENAHVMPPVVIEDASDMLLAITQAGRMLMFPVSDL
  PQLSKGKGNKIINIPSAEAARGEDGLAQLYVLPPQSTLTIHVGKRKIKLRPEELQKVTGE
  RGRRGTLMRGLQRIDRVEIDSPRRASSGDSEE
• 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. MukB stimulates the relaxation activity of topoisomeraseIV and also has a modest effect on decatenation.
• BioCyc Pathway: EcoCyc:EG10686-MON

Molecular Interaction Atlas (MIA) of This DTT

1 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Prulifloxacin	DMOK965	Urinary tract infection	GC08	Approved	[2]

5 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Pazufloxacin	DMHXTAQ	Conjunctivitis	9A60	Phase 3	[3]
Sitafloxacin	DMTV5XC	Escherichia coli infection	1A03	Phase 2/3	[4]
JNJ-32729463	DMQD1GN	Community-acquired pneumonia	CA40.Z	Phase 2	[5]
TNP-2092	DM8DZKI	Skin and skin-structure infection	1F28-1G0Z	Phase 2	[6]
VB 1953	DM0YWQ4	Acne vulgaris	ED80	Phase 2	[7]

1 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
A-62824	DMJ6IMZ	Discovery agent	N.A.	Investigative	[1]

References

• [1] Isothiazoloquinolones containing functionalized aromatic hydrocarbons at the 7-position: synthesis and in vitro activity of a series of potent anti... Bioorg Med Chem Lett. 2006 Mar 1;16(5):1272-6.
• [2] Prulifloxacin: a new antibacterial fluoroquinolone. Expert Rev Anti Infect Ther. 2006 Feb;4(1):27-41.
• [3] Target preference of 15 quinolones against Staphylococcus aureus, based on antibacterial activities and target inhibition. Antimicrob Agents Chemother. 2001 Dec;45(12):3544-7.
• [4] Dual-targeting properties of the 3-aminopyrrolidyl quinolones, DC-159a and sitafloxacin, against DNA gyrase and topoisomerase IV: contribution to reducing in vitro emergence of quinolone-resistant Streptococcus pneumoniae. J Antimicrob Chemother. 2008 Jul;62(1):98-104.
• [5] Antistaphylococcal activities of the new fluoroquinolone JNJ-Q2. Antimicrob Agents Chemother. 2011 Dec;55(12):5512-21.
• [6] Clinical pipeline report, company report or official report of TenNor Therapeutics.
• [7] Clinical pipeline report, company report or official report of Vyome Therapeutics.