Target Information
Target General Information | Top | |||||
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Target ID |
T62094
(Former ID: TTDI01930)
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Target Name |
Bacterial 30S ribosomal RNA (Bact 30S rRNA)
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Gene Name |
NO-GeName
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Target Type |
Successful target
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[1] | ||||
Disease | [+] 7 Target-related Diseases | + | ||||
1 | Acne vulgaris [ICD-11: ED80] | |||||
2 | Bacterial infection [ICD-11: 1A00-1C4Z] | |||||
3 | Gingival/edentulous alveolar ridge disorder [ICD-11: DA0D] | |||||
4 | Infectious gastroenteritis/colitis [ICD-11: 1A40] | |||||
5 | Periodontal disease [ICD-11: DA0C] | |||||
6 | Pneumonia [ICD-11: CA40] | |||||
7 | Skin sensation disturbance [ICD-11: ME65] | |||||
UniProt ID |
Drugs and Modes of Action | Top | |||||
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Approved Drug(s) | [+] 7 Approved Drugs | + | ||||
1 | Doxycycline | Drug Info | Approved | Chronic periodontitis | [2], [3] | |
2 | Gentamicin | Drug Info | Approved | Bacterial infection | [3], [4] | |
3 | Nitrofurazone | Drug Info | Approved | Skin burns | [5] | |
4 | Omadacycline | Drug Info | Approved | Acute bacterial skin infection | [6] | |
5 | Sarecycline | Drug Info | Approved | Acne vulgaris | [7] | |
6 | Tobramycin | Drug Info | Approved | Bacterial infection | [3] | |
7 | TP-434 | Drug Info | Approved | Intra-abdominal infection | [8] | |
Clinical Trial Drug(s) | [+] 4 Clinical Trial Drugs | + | ||||
1 | ME1100 | Drug Info | Phase 1 | Bacterial pneumonia | [9] | |
2 | TP 6076 | Drug Info | Phase 1 | Multidrug resistant infection | [10] | |
3 | TP-271 | Drug Info | Phase 1 | Respiratory tract infection | [11] | |
4 | TP-6076 | Drug Info | Phase 1 | Enterobacteriaceae infection | [10] | |
Discontinued Drug(s) | [+] 2 Discontinued Drugs | + | ||||
1 | Wetimicin | Drug Info | Discontinued in Phase 1 | Infectious disease | [12] | |
2 | DACTIMICIN | Drug Info | Terminated | Bacterial infection | [13] | |
Mode of Action | [+] 2 Modes of Action | + | ||||
Modulator | [+] 3 Modulator drugs | + | ||||
1 | Doxycycline | Drug Info | [14] | |||
2 | Gentamicin | Drug Info | [14] | |||
3 | Tobramycin | Drug Info | [15] | |||
Inhibitor | [+] 9 Inhibitor drugs | + | ||||
1 | Nitrofurazone | Drug Info | [1] | |||
2 | Omadacycline | Drug Info | [6] | |||
3 | Sarecycline | Drug Info | [7] | |||
4 | TP-434 | Drug Info | [8] | |||
5 | ME1100 | Drug Info | [16] | |||
6 | TP 6076 | Drug Info | [17] | |||
7 | TP-271 | Drug Info | [18] | |||
8 | Wetimicin | Drug Info | [19] | |||
9 | DACTIMICIN | Drug Info | [20] |
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 |
References | Top | |||||
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REF 1 | The antibiotic Furvina targets the P-site of 30S ribosomal subunits and inhibits translation initiation displaying start codon bias. Nucleic Acids Res. 2012 Nov 1;40(20):10366-74. | |||||
REF 2 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6464). | |||||
REF 3 | How many modes of action should an antibiotic have Curr Opin Pharmacol. 2008 Oct;8(5):564-73. | |||||
REF 4 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2427). | |||||
REF 5 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
REF 6 | Omadacycline Enters the Ring: A New Antimicrobial Contender.Pharmacotherapy. 2018 Dec;38(12):1194-1204. | |||||
REF 7 | Microbiological Profile of Sarecycline, a Novel Targeted Spectrum Tetracycline for the Treatment of Acne Vulgaris.Antimicrob Agents Chemother. 2018 Dec 21;63(1). pii: e01297-18. | |||||
REF 8 | The antibiotic arms race: current and emerging therapy for Klebsiella pneumoniae carbapenemase (KPC) - producing bacteria.Expert Opin Pharmacother. 2018 Oct 22:1-13. | |||||
REF 9 | ClinicalTrials.gov (NCT01907776) Pharmacokinetics and Safety Study of ME1100 in Healthy Volunteers. U.S. National Institutes of Health. | |||||
REF 10 | ClinicalTrials.gov (NCT03691584) Phase 1, Safety and Bronchopulmonary PK Study in Healthy Volunteers (BAL). U.S. National Institutes of Health. | |||||
REF 11 | ClinicalTrials.gov (NCT03234738) A Phase 1 Safety and PK Study of IV TP-271. U.S. National Institutes of Health. | |||||
REF 12 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028068) | |||||
REF 13 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000500) | |||||
REF 14 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | |||||
REF 15 | Mechanism of action of aminoglycoside antibiotics.Binding studies of tobramycin and its 6'-N-acetyl derivative to the bacterial ribosome and its subunits.Eur J Biochem.1979 Dec;102(1):73-81. | |||||
REF 16 | ClinicalTrials.gov (NCT01961830) Intrapulmonary Pharmacokinetics of ME1100 in Healthy Volunteers. U.S. National Institutes of Health. | |||||
REF 17 | Clinical pipeline report, company report or official report of Tetraphase Pharmaceuticals. | |||||
REF 18 | Clinical pipeline report, company report or official report of Tetraphase Pharmaceuticals. | |||||
REF 19 | Cross susceptibility of ototoxicity about aminoglycoside antibiotics. Lin Chuang Er Bi Yan Hou Ke Za Zhi. 1997 Jan;11(1):9-10. | |||||
REF 20 | Aminoglycosides: Activity and Resistance. Antimicrob Agents Chemother. 1999 April; 43(4): 727-737. |
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