Target Information
| Target General Information | Top | |||||
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| Target ID |
T30938
(Former ID: TTDI00934)
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| Target Name |
Mycobacterium RNA polymerase (MycB RNAP)
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| Synonyms |
Transcriptase; RNAP; RNA polymerase; Mycobacterium DNA-directed RNA polymerase
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| Gene Name |
MycB rpoA; MycB rpoB; MycB rpoC; MycB rpoZ
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Bowel habit change [ICD-11: ME05] | |||||
| Function |
DNA-dependent RNA polymerase catalyzes the transcription of DNA into RNA using the four ribonucleoside triphosphates as substrates.
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| UniProt ID | ||||||
| Sequence |
MLISQRPTLSEDVLTDNRSQFVIEPLEPGFGYTLGNSLRRTLLSSIPGAAVTSIRIDGVL
HEFTTVPGVKEDVTEIILNLKSLVVSSEEDEPVTMYLRKQGPGEVTAGDIVPPAGVTVHN PGMHIATLNDKGKLEVELVVERGRGYVPAVQNRASGAEIGRIPVDSIYSPVLKVTYKVDA TRVEQRTDFDKLILDVETKNSISPRDALASAGKTLVELFGLARELNVEAEGIEIGPSPAE ADHIASFALPIDDLDLTVRSYNCLKREGVHTVGELVARTESDLLDIRNFGQKSIDEVKIK LHQLGLSLKDSPPSFDPSEVAGYDVATGTWSTEGAYDEQDYAETEQL Click to Show/Hide
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| Drugs and Modes of Action | Top | |||||
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| Approved Drug(s) | [+] 2 Approved Drugs | + | ||||
| 1 | Rifamycin | Drug Info | Approved | Diarrhea | [1] | |
| 2 | Favipiravir | Drug Info | Registered | Influenza virus infection | [2] | |
| Clinical Trial Drug(s) | [+] 1 Clinical Trial Drugs | + | ||||
| 1 | TAS-106 | Drug Info | Phase 2 | Head and neck cancer | [3] | |
| Discontinued Drug(s) | [+] 3 Discontinued Drugs | + | ||||
| 1 | JTK-003 | Drug Info | Discontinued in Phase 2 | Hepatitis C virus infection | [4] | |
| 2 | R-1479 | Drug Info | Discontinued in Phase 1 | Hepatitis C virus infection | [5] | |
| 3 | XTL-2125 | Drug Info | Discontinued in Phase 1 | Hepatitis C virus infection | [6] | |
| Mode of Action | [+] 2 Modes of Action | + | ||||
| Inhibitor | [+] 3 Inhibitor drugs | + | ||||
| 1 | Rifamycin | Drug Info | [1] | |||
| 2 | JTK-003 | Drug Info | [9] | |||
| 3 | R-1479 | Drug Info | [10] | |||
| Modulator | [+] 3 Modulator drugs | + | ||||
| 1 | Favipiravir | Drug Info | [7] | |||
| 2 | TAS-106 | Drug Info | [8] | |||
| 3 | XTL-2125 | Drug Info | [11] | |||
| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
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| Co-Targets | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| KEGG Pathway | [+] 4 KEGG Pathways | + | ||||
| 1 | Purine metabolism | |||||
| 2 | Pyrimidine metabolism | |||||
| 3 | Metabolic pathways | |||||
| 4 | RNA polymerase | |||||
| References | Top | |||||
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| REF 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. | |||||
| REF 2 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014667) | |||||
| REF 3 | ClinicalTrials.gov (NCT00737360) Phase II Study of TAS-106 to Treat Head and Neck Cancer. U.S. National Institutes of Health. | |||||
| REF 4 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017555) | |||||
| REF 5 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018944) | |||||
| REF 6 | Emerging drugs for hepatitis C. Expert Opin Emerg Drugs. 2008 Mar;13(1):1-19. | |||||
| REF 7 | Favipiravir (T-705), a novel viral RNA polymerase inhibitor.Antiviral Res.2013 Nov;100(2):446-54. | |||||
| REF 8 | 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. | |||||
| REF 9 | Antiviral Therapy for Hepatitis C Virus: Beyond the Standard of Care. Viruses. 2010 April; 2(4): 826-866. | |||||
| REF 10 | 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. | |||||
| REF 11 | DOI: 10.1111/j.1365-2036.2009.03927.x | |||||
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