Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT79JGK)

• DTT Name: Mycobacterium RNA polymerase (MycB RNAP)
• Synonyms: Transcriptase; RNAP; RNA polymerase; Mycobacterium DNA-directed RNA polymerase
• Gene Name: MycB rpoA
• DTT Type: Successful target; [1]
• UniProt ID: RPOA_MYCTU ; RPOB_MYCTU ; RPOC_MYCTU ; RPOZ_MYCTU
• TTD ID: T30938
• Sequence:
  MLISQRPTLSEDVLTDNRSQFVIEPLEPGFGYTLGNSLRRTLLSSIPGAAVTSIRIDGVL
  HEFTTVPGVKEDVTEIILNLKSLVVSSEEDEPVTMYLRKQGPGEVTAGDIVPPAGVTVHN
  PGMHIATLNDKGKLEVELVVERGRGYVPAVQNRASGAEIGRIPVDSIYSPVLKVTYKVDA
  TRVEQRTDFDKLILDVETKNSISPRDALASAGKTLVELFGLARELNVEAEGIEIGPSPAE
  ADHIASFALPIDDLDLTVRSYNCLKREGVHTVGELVARTESDLLDIRNFGQKSIDEVKIK
  LHQLGLSLKDSPPSFDPSEVAGYDVATGTWSTEGAYDEQDYAETEQL
• Function: DNA-dependent RNA polymerase catalyzes the transcription of DNA into RNA using the four ribonucleoside triphosphates as substrates.
• KEGG Pathway:
  Purine metabolism (mtu00230)
  Pyrimidine metabolism (mtu00240)
  Metabolic pathways (mtu01100)
  RNA polymerase (mtu03020)
• Reactome Pathway: Antimicrobial action and antimicrobial resistance in Mtb (R-HSA-9639775)

Molecular Interaction Atlas (MIA) of This DTT

2 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Rifamycin	DMEH3O7	Diarrhea	ME05.1	Approved	[1]
Favipiravir	DMBZ27L	Influenza virus infection	1E30-1E32	Registered	[2]

1 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
TAS-106	DML97KB	Head and neck cancer	2D42	Phase 2	[3]

3 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
JTK-003	DMB0V5Y	Hepatitis C virus infection	1E51.1	Discontinued in Phase 2	[4]
R-1479	DM9C6LN	Hepatitis C virus infection	1E51.1	Discontinued in Phase 1	[5]
XTL-2125	DM3Y6M7	Hepatitis C virus infection	1E51.1	Discontinued in Phase 1	[6]

References

• [1] Rifamycin action on RNA polymerase in antibiotic-tolerant Mycobacterium tuberculosis results in differentially detectable populations.Proc Natl Acad Sci U S A. 2017 Jun 13;114(24):E4832-E4840.
• [2] Favipiravir (T-705), a novel viral RNA polymerase inhibitor.Antiviral Res.2013 Nov;100(2):446-54.
• [3] Phase I and pharmacokinetic study of 3'-C-ethynylcytidine (TAS-106), an inhibitor of RNA polymerase I, II and III,in patients with advanced solid malignancies.Invest New Drugs.2012 Feb;30(1):316-26.
• [4] Antiviral Therapy for Hepatitis C Virus: Beyond the Standard of Care. Viruses. 2010 April; 2(4): 826-866.
• [5] The novel nucleoside analog R1479 (4'-azidocytidine) is a potent inhibitor of NS5B-dependent RNA synthesis and hepatitis C virus replication in cel... J Biol Chem. 2006 Feb 17;281(7):3793-9.
• [6] DOI: 10.1111/j.1365-2036.2009.03927.x