Target Information
Target General Information | Top | |||||
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Target ID |
T53601
(Former ID: TTDI01915)
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Target Name |
Bacterial 50S ribosomal RNA (Bact 50S rRNA)
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Gene Name |
NO-GeName
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Target Type |
Successful target
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[1] | ||||
Disease | [+] 6 Target-related Diseases | + | ||||
1 | Acne vulgaris [ICD-11: ED80] | |||||
2 | Bacterial infection [ICD-11: 1A00-1C4Z] | |||||
3 | Gram-positive bacterial infection [ICD-11: 1B74-1F40] | |||||
4 | Impetigo [ICD-11: 1B72] | |||||
5 | Skin and skin-structure infection [ICD-11: 1F28-1G0Z] | |||||
6 | Syphilis [ICD-11: 1A61-1A6Z] | |||||
Function |
Protein L1 is also a translational repressor protein, it controls the translation of the L11 operon by binding to its mRNA.
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UniProt ID |
Drugs and Modes of Action | Top | |||||
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Approved Drug(s) | [+] 13 Approved Drugs | + | ||||
1 | Clarithromycin | Drug Info | Approved | Bacterial infection | [2] | |
2 | Clindamycin | Drug Info | Approved | Acne vulgaris | [3] | |
3 | Dalfopristin | Drug Info | Approved | Bacterial infection | [2] | |
4 | Dirithromycin | Drug Info | Approved | Bacterial infection | [2] | |
5 | Erythromycin | Drug Info | Approved | Bacterial infection | [4], [5] | |
6 | Gentamicine sulfate | Drug Info | Approved | Bacterial infection | [5] | |
7 | Josamycin | Drug Info | Approved | Bacterial infection | [6] | |
8 | Lincomycin | Drug Info | Approved | Gram-positive bacterial infection | [3], [7] | |
9 | Retapamulin | Drug Info | Approved | Impetigo | [8] | |
10 | Tedizolid | Drug Info | Approved | Skin infection | [3] | |
11 | Telithromycin | Drug Info | Approved | Bacterial infection | [9] | |
12 | Troleandomycin | Drug Info | Approved | Bacterial infection | [10] | |
13 | Zithromax | Drug Info | Approved | Syphilis infection | [11] | |
Clinical Trial Drug(s) | [+] 5 Clinical Trial Drugs | + | ||||
1 | DARE-BV1 | Drug Info | Phase 3 | Bacterial vaginosis | [12] | |
2 | Solithromycin | Drug Info | Phase 3 | Bacillus anthracis infection | [13] | |
3 | BC-7013 | Drug Info | Phase 2 | Skin infection | [14] | |
4 | GSK-1399686 | Drug Info | Phase 2 | Inflammatory bowel disease | [15] | |
5 | BC-3205 | Drug Info | Phase 1 | Respiratory tract infection | [16] | |
Discontinued Drug(s) | [+] 6 Discontinued Drugs | + | ||||
1 | Roxithromycin | Drug Info | Withdrawn from market | Bacterial infection | [2], [17] | |
2 | Azithromycin/chloroquine | Drug Info | Discontinued in Phase 3 | Bacterial infection | [18] | |
3 | Eperezolid | Drug Info | Discontinued in Phase 3 | Bacterial infection | [19] | |
4 | Evernimicin | Drug Info | Discontinued in Phase 3 | Bacterial infection | [20] | |
5 | HMR-3562 | Drug Info | Discontinued in Phase 1 | Bacterial infection | [21] | |
6 | HMR-3787 | Drug Info | Terminated | Bacterial infection | [24] | |
Preclinical Drug(s) | [+] 2 Preclinical Drugs | + | ||||
1 | RANBEZOLID HYDROCHLORIDE | Drug Info | Preclinical | Bacterial infection | [22] | |
2 | RX-01-423 | Drug Info | Preclinical | Bacterial infection | [23] | |
Mode of Action | [+] 3 Modes of Action | + | ||||
Binder | [+] 10 Binder drugs | + | ||||
1 | Clarithromycin | Drug Info | [25] | |||
2 | Clindamycin | Drug Info | [25] | |||
3 | Dalfopristin | Drug Info | [26] | |||
4 | Dirithromycin | Drug Info | [27] | |||
5 | Erythromycin | Drug Info | [25], [28], [29] | |||
6 | Gentamicine sulfate | Drug Info | [30] | |||
7 | Josamycin | Drug Info | [31] | |||
8 | Telithromycin | Drug Info | [34], [35] | |||
9 | Troleandomycin | Drug Info | [36] | |||
10 | Azithromycin/chloroquine | Drug Info | [44], [45] | |||
Inhibitor | [+] 3 Inhibitor drugs | + | ||||
1 | Lincomycin | Drug Info | [32] | |||
2 | Retapamulin | Drug Info | [33] | |||
3 | Roxithromycin | Drug Info | [43] | |||
Modulator | [+] 13 Modulator drugs | + | ||||
1 | Tedizolid | Drug Info | [1] | |||
2 | Zithromax | Drug Info | [37] | |||
3 | Solithromycin | Drug Info | [39] | |||
4 | BC-7013 | Drug Info | [40] | |||
5 | GSK-1399686 | Drug Info | [41] | |||
6 | BC-3205 | Drug Info | [42] | |||
7 | Eperezolid | Drug Info | [46] | |||
8 | Evernimicin | Drug Info | [47] | |||
9 | HMR-3562 | Drug Info | [48] | |||
10 | RANBEZOLID HYDROCHLORIDE | Drug Info | [49] | |||
11 | RX-01-423 | Drug Info | [50] | |||
12 | HMR-3787 | Drug Info | [48] | |||
13 | Erythromycin salnacedin | Drug Info | [37] |
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-Related Models and Studies | Top | |||||
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Target Validation |
References | Top | |||||
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REF 1 | 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81. | |||||
REF 2 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. | |||||
REF 3 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
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: 1456). | |||||
REF 5 | How many modes of action should an antibiotic have Curr Opin Pharmacol. 2008 Oct;8(5):564-73. | |||||
REF 6 | Drug information of Josamycin, 2008. eduDrugs. | |||||
REF 7 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 050317. | |||||
REF 8 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 022055. | |||||
REF 9 | Recently approved and investigational antibiotics for treatment of severe infections caused by Gram-positive bacteria. Curr Opin Microbiol. 2005 Oct;8(5):510-7. | |||||
REF 10 | Drug Information of Dihydrotachysterol from nextbio research in illumina. 2015. | |||||
REF 11 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | |||||
REF 12 | ClinicalTrials.gov (NCT04370548) DARE-BV1 in the Treatment of Bacterial Vaginosis (DARE-BVFREE). U.S. National Institutes of Health. | |||||
REF 13 | ClinicalTrials.gov (NCT01756339) Efficacy and Safety Study of Oral Solithromycin (CEM-101) Compared to Oral Moxifloxacin in Treatment of Patients With Community-Acquired Bacterial Pneumonia. U.S. National Institutes of Health. | |||||
REF 14 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 15 | ClinicalTrials.gov (NCT01036022) Effect of GSK1399686 in Patients With Mild to Moderately Active Ulcerative Colitis. U.S. National Institutes of Health. | |||||
REF 16 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029896) | |||||
REF 17 | 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: 1465). | |||||
REF 18 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019101) | |||||
REF 19 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005626) | |||||
REF 20 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002696) | |||||
REF 21 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012748) | |||||
REF 22 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017411) | |||||
REF 23 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019836) | |||||
REF 24 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012749) | |||||
REF 25 | Structural basis for the interaction of antibiotics with the peptidyl transferase centre in eubacteria. Nature. 2001 Oct 25;413(6858):814-21. | |||||
REF 26 | The streptogramin antibiotics: update on their mechanism of action. Expert Opin Investig Drugs. 1998 Apr;7(4):591-9. | |||||
REF 27 | Review of macrolides and ketolides: focus on respiratory tract infections. Drugs. 2001;61(4):443-98. | |||||
REF 28 | A synthetic alanyl-initiator tRNA with initiator tRNA properties as determined by fluorescence measurements: comparison to a synthetic alanyl-elongator tRNA. Nucleic Acids Res. 1991 Oct 25;19(20):5749-54. | |||||
REF 29 | Inhibition of 50S ribosomal subunit assembly in Haemophilus influenzae cells by azithromycin and erythromycin. Curr Microbiol. 2002 Jun;44(6):418-24. | |||||
REF 30 | The protein synthesis inhibitors, oxazolidinones and chloramphenicol, cause extensive translational inaccuracy in vivo. J Mol Biol. 2002 Sep 13;322(2):273-9. | |||||
REF 31 | The mechanism of action of macrolides, lincosamides and streptogramin B reveals the nascent peptide exit path in the ribosome. J Mol Biol. 2003 Jul 25;330(5):1005-14. | |||||
REF 32 | Specific inhibition of 50S ribosomal subunit formation in Staphylococcus aureus cells by 16-membered macrolide, lincosamide, and streptogramin B antibiotics. Curr Microbiol. 2000 Aug;41(2):126-35. | |||||
REF 33 | Retapamulin inhibition of translation and 50S ribosomal subunit formation in Staphylococcus aureus cells. Antimicrob Agents Chemother. 2007 Sep;51(9):3385-7. | |||||
REF 34 | An examination of the differential sensitivity to ketolide antibiotics in ermB strains of Streptococcus pyogenes and Streptococcus pneumoniae. Curr Microbiol. 2004 Oct;49(4):239-47. | |||||
REF 35 | Clinical pharmacokinetics of telithromycin, the first ketolide antibacterial. Clin Pharmacokinet. 2005;44(9):915-34. | |||||
REF 36 | Depression of colony formation by human thymus-derived lymphocytes with rifampin and other antimicrobial agents. J Infect Dis. 1981 Jun;143(6):832-5. | |||||
REF 37 | The ChEMBL database in 2017. Nucleic Acids Res. 2017 Jan 4;45(D1):D945-D954. | |||||
REF 38 | Characterization of Escherichia coli 50S ribosomal protein L31. FEMS Microbiol Lett. 1999 Nov 15;180(2):345-9. | |||||
REF 39 | Company report (cempra) | |||||
REF 40 | Company report (briva) | |||||
REF 41 | Current, new and future biological agents on the horizon for the treatment of inflammatory bowel diseases. Therap Adv Gastroenterol. 2015 March; 8(2): 66-82. | |||||
REF 42 | Disk Diffusion and MIC Quality Control Ranges for BC-3205 and BC-3781, Two Novel Pleuromutilin Antibiotics. J Clin Microbiol. 2012 October; 50(10): 3361-3364. | |||||
REF 43 | Molecular insights into 14-membered macrolides using the MM-PBSA method. J Chem Inf Model. 2009 Jun;49(6):1558-67. | |||||
REF 44 | Pfizer. Product Development Pipeline. March 31 2009. | |||||
REF 45 | Time-resolved binding of azithromycin to Escherichia coli ribosomes. J Mol Biol. 2009 Jan 30;385(4):1179-92. | |||||
REF 46 | The oxazolidinone eperezolid binds to the 50S ribosomal subunit and competes with binding of chloramphenicol and lincomycin. | |||||
REF 47 | Evernimicin binds exclusively to the 50S ribosomal subunit and inhibits translation in cell-free systems derived from both gram-positive and gram-n... Antimicrob Agents Chemother. 2000 May;44(5):1121-6. | |||||
REF 48 | Structure-activity relationships for six ketolide antibiotics. Curr Microbiol. 2001 Mar;42(3):203-10. | |||||
REF 49 | Mode of Action of Ranbezolid against Staphylococci and Structural Modeling Studies of Its Interaction with Ribosomes . Antimicrob Agents Chemother. 2009 April; 53(4): 1427-1433. | |||||
REF 50 | DOI: 10.1038/nrd2202 |
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