Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTN6J5F)

• DTT Name: Bacterial DNA gyrase (Bact gyrase)
• Synonyms: DNA gyrase
• Gene Name: Bact gyrA
• DTT Type: Successful target; [1]
• BioChemical Class: ATP-hydrolyzing DNA topoisomerase
• UniProt ID: GYRA_STAAU ; GYRB_STAAU
• TTD ID: T22348
• Sequence:
  MAELPQSRINERNITSEMRESFLDYAMSVIVARALPDVRDGLKPVHRRILYGLNEQGMTP
  DKSYKKSARIVGDVMGKYHPHGDSSIYEAMVRMAQDFSYRYPLVDGQGNFGSMDGDGAAA
  MRYTEARMTKITLELLRDINKDTIDFIDNYDGNEREPSVLPARFPNLLANGASGIAVGMA
  TNIPPHNLTELINGVLSLSKNPDISIAELMEDIEGPDFPTAGLILGKSGIRRAYETGRGS
  IQMRSRAVIEERGGGRQRIVVTEIPFQVNKARMIEKIAELVRDKKIDGITDLRDETSLRT
  GVRVVIDVRKDANASVILNNLYKQTPLQTSFGVNMIALVNGRPKLINLKEALVHYLEHQK
  TVVRRRTQYNLRKAKDRAHILEGLRIALDHIDEIISTIRESDTDKVAMESLQQRFKLSEK
  QAQAILDMRLRRLTGLERDKIEAEYNELLNYISELEAILADEEVLLQLVRDELTEIRDRF
  GDDRRTEIQLGGFEDLEDEDLIPEEQIVITLSHNNYIKRLPVSTYRAQNRGGRGVQGMNT
  LEEDFVSQLVTLSTHDHVLFFTNKGRVYKLKGYEVPELSRQSKGIPVVNAIELENDEVIS
  TMIAVKDLESEDNFLVFATKRGVVKRSALSNFSRINRNGKIAISFREDDELIAVRLTSGQ
  EDILIGTSHASLIRFPESTLRPLGRTATGVKGITLREGDEVVGLDVAHANSVDEVLVVTE
  NGYGKRTPVNDYRLSNRGGKGIKTATITERNGNVVCITTVTGEEDLMIVTNAGVIIRLDV
  ADISQNGRAAQGVRLIRLGDDQFVSTVAKVKEDAEDETNEDEQSTSTVSEDGTEQQREAV
  VNDETPGNAIHTEVIDSEENDEDGRIEVRQDFMDRVEEDIQQSLDEDEE
• Function: DNA gyrase negatively supercoils closed circular double- stranded DNA in an ATP-dependent manner and also catalyzes the interconversion of other topological isomers of double-stranded DNA rings, including catenanes and knotted rings.

Molecular Interaction Atlas (MIA) of This DTT

15 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Besifloxacin	DMPHXMI	Ocular inflammation	9C61.24	Approved	[1]
Ciprofloxacin XR	DM2NLS9	Acute gonococcal cervicitis		Approved	[2]
Finafloxacin	DMZEONG	Urinary tract infection	GC08	Approved	[3]
Gatifloxacin	DMSL679	Acute gonococcal cervicitis		Approved	[2]
Gemifloxacin	DMHT34O	Bacterial infection	1A00-1C4Z	Approved	[2]
Grepafloxacin	DMGLX0T	Chronic bronchitis	CA20.1	Approved	[4]
Levofloxacin	DMS60RB	Acute maxillary sinusitis		Approved	[2]
Moxifloxacin	DMU8V4S	Bacterial infection	1A00-1C4Z	Approved	[2]
Nemonoxacin	DM0S9Z1	Community-acquired pneumonia	CA40.Z	Approved	[5]
Norfloxacin	DMIZ6W2	Acute gonococcal cervicitis		Approved	[2]
Ofloxacin	DM0VQN3	Acute gonococcal cervicitis		Approved	[2]
Ozenoxacin	DM6KZMG	Impetigo	1B72	Approved	[6]
Prulifloxacin	DMOK965	Urinary tract infection	GC08	Approved	[7]
Sparfloxacin	DMB4HCT	Bacterial infection	1A00-1C4Z	Approved	[2]
Trovafloxacin	DM6AN32	Acute gonococcal cervicitis		Approved	[2]

9 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
AZD0914	DMM6G5D	Neisseria gonorrhoeae infection	1A7Z	Phase 3	[8]
BAY-35-3377	DMWYPZF	Otitis media	AA80-AB0Z	Phase 3	[9]
Pazufloxacin	DMHXTAQ	Conjunctivitis	9A60	Phase 3	[10]
Zabofloxacin	DMEY1F3	Pneumonia	CA40	Phase 3	[11]
Sitafloxacin	DMTV5XC	Escherichia coli infection	1A03	Phase 2/3	[12]
JNJ-32729463	DMQD1GN	Community-acquired pneumonia	CA40.Z	Phase 2	[13]
TNP-2092	DM8DZKI	Skin and skin-structure infection	1F28-1G0Z	Phase 2	[14]
VB 1953	DM0YWQ4	Acne vulgaris	ED80	Phase 2	[15]
WCK-771	DMVQARP	Bacterial infection	1A00-1C4Z	Phase 2	[16]

27 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Temafloxacin	DM3TON2	Bacterial infection	1A00-1C4Z	Withdrawn from market	[17]
OLAMUFLOXACIN MESILATE	DM0O2HP	Bacterial infection	1A00-1C4Z	Discontinued in Phase 3	[18]
99mTc-ciprofloxacin	DMSGY5M	Infectious disease	1A00-CA43.1	Discontinued in Phase 2	[19]
A-86719.1	DM7VSBH	Bacterial infection	1A00-1C4Z	Discontinued in Phase 2	[20]
BAY-Y-3118	DMCZKG0	Bacterial infection	1A00-1C4Z	Discontinued in Phase 2	[21]
Cadrofloxacin	DMHJ3SN	Bacterial infection	1A00-1C4Z	Discontinued in Phase 2	[22]
CFC-222	DMHK8IM	Bacterial infection	1A00-1C4Z	Discontinued in Phase 2	[23]
DANOFLOXACIN	DMF3E51	Bacterial infection	1A00-1C4Z	Discontinued in Phase 2	[24]
DX-619	DMSTA5L	Bacterial infection	1A00-1C4Z	Discontinued in Phase 2	[25]
FANDOFLOXACIN HYDROCHLORIDE	DM8UC0K	Bacterial infection	1A00-1C4Z	Discontinued in Phase 2	[18]
Ro-23-9424	DM4YA63	Bacterial infection	1A00-1C4Z	Discontinued in Phase 2	[26]
AZD-5099	DMWKYV7	Infectious disease	1A00-CA43.1	Discontinued in Phase 1	[27]
Cetefloxacin	DM85SYL	Bacterial infection	1A00-1C4Z	Discontinued in Phase 1	[18]
DV-7751A	DMDC4BA	Bacterial infection	1A00-1C4Z	Discontinued in Phase 1	[28]
GSK945237	DM2AP64	Bacterial infection	1A00-1C4Z	Discontinued in Phase 1	[29]
PD-131112	DMVFGWM	Bacterial infection	1A00-1C4Z	Discontinued in Phase 1	[18]
A-70826	DM9X24J	Bacterial infection	1A00-1C4Z	Terminated	[31]
BMY-40062	DM2TF9P	Bacterial infection	1A00-1C4Z	Terminated	[32]
CBR-2092	DMJAGKY	Bacterial infection	1A00-1C4Z	Terminated	[33]
Clinafloxacin	DM6F8L5	Pneumonia	CA40	Terminated	[34]
CP-67015	DMWFI4A	Bacterial infection	1A00-1C4Z	Terminated	[2]
KB-5246	DM2LFYD	Bacterial infection	1A00-1C4Z	Terminated	[35]
MF-5137	DM72MQP	Staphylococcus infection	1B5Y	Terminated	[2]
PD-117596	DMN1A70	Bacterial infection	1A00-1C4Z	Terminated	[36]
Protosufloxacin	DM57YO8	Bacterial infection	1A00-1C4Z	Terminated	[2]
Ro-23-7777	DM7B2WH	Fungal infection	1F29-1F2F	Terminated	[2]
S-34109	DMPQIUH	Staphylococcus infection	1B5Y	Terminated	[37]

1 Preclinical Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Viquidacin	DMS5LPF	Bacterial infection	1A00-1C4Z	Preclinical	[30]

2 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
NSFQ-105	DMSLA8X	Discovery agent	N.A.	Investigative	[38]
PD-117558	DM3KAY5	Discovery agent	N.A.	Investigative	[39]

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