Target Information

Target General Information

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Target ID

T53601 (Former ID: TTDI01915)

Target Name

Bacterial 50S ribosomal RNA (Bact 50S rRNA)

Gene Name

NO-GeName

Target Type

Successful target

[1]

Disease

[+] 6 Target-related Diseases

Acne vulgaris [ICD-11: ED80]

Bacterial infection [ICD-11: 1A00-1C4Z]

Gram-positive bacterial infection [ICD-11: 1B74-1F40]

Impetigo [ICD-11: 1B72]

Skin and skin-structure infection [ICD-11: 1F28-1G0Z]

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

NOUNIPROTAC

Drugs and Modes of Action

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Approved Drug(s)

[+] 11 Approved Drugs

Clindamycin

Drug Info

Approved

Acne vulgaris

[4]

Dalfopristin

Drug Info

Approved

Bacterial infection

[2]

Dirithromycin

Drug Info

Approved

Bacterial infection

[2]

Erythromycin

Drug Info

Approved

Bacterial infection

[5], [6]

Gentamicine sulfate

Drug Info

Approved

Bacterial infection

[6]

Lincomycin

Drug Info

Approved

Gram-positive bacterial infection

[4], [7]

Retapamulin

Drug Info

Approved

Impetigo

[8]

Tedizolid

Drug Info

Approved

Skin infection

[4]

Telithromycin

Drug Info

Approved

Bacterial infection

[9]

Troleandomycin

Drug Info

Approved

Bacterial infection

[10]

Zithromax

Drug Info

Approved

Syphilis infection

[11]

Clinical Trial Drug(s)

[+] 3 Clinical Trial Drugs

BC-7013

Drug Info

Phase 2

Skin infection

[14]

GSK-1399686

Drug Info

Phase 2

Inflammatory bowel disease

[15]

BC-3205

Drug Info

Phase 1

Respiratory tract infection

[16]

Discontinued Drug(s)

[+] 4 Discontinued Drugs

Azithromycin/chloroquine

Drug Info

Discontinued in Phase 3

Bacterial infection

[19]

Evernimicin

Drug Info

Discontinued in Phase 3

Bacterial infection

[20]

HMR-3562

Drug Info

Discontinued in Phase 1

Bacterial infection

[21]

HMR-3787

Drug Info

Terminated

Bacterial infection

[24]

Preclinical Drug(s)

[+] 2 Preclinical Drugs

RANBEZOLID HYDROCHLORIDE

Drug Info

Preclinical

Bacterial infection

[22]

RX-01-423

Drug Info

Preclinical

Bacterial infection

[23]

Mode of Action

[+] 3 Modes of Action

Binder

[+] 8 Binder drugs

Clindamycin

Drug Info

[25]

Dalfopristin

Drug Info

[26]

Dirithromycin

Drug Info

[27]

Erythromycin

Drug Info

[25], [28], [29]

Gentamicine sulfate

Drug Info

[30]

Telithromycin

Drug Info

[33], [34]

Troleandomycin

Drug Info

[35]

Azithromycin/chloroquine

Drug Info

[40], [41]

Inhibitor

[+] 2 Inhibitor drugs

Lincomycin

Drug Info

[31]

Retapamulin

Drug Info

[32]

Modulator

[+] 11 Modulator drugs

Tedizolid

Drug Info

[1]

Zithromax

Drug Info

[36]

BC-7013

Drug Info

[37]

GSK-1399686

Drug Info

[38]

BC-3205

Drug Info

[39]

Evernimicin

Drug Info

[42]

HMR-3562

Drug Info

[43]

RANBEZOLID HYDROCHLORIDE

Drug Info

[44]

RX-01-423

Drug Info

[45]

HMR-3787

Drug Info

[43]

Erythromycin salnacedin

Drug Info

[36]

Drug Property Profile of Target

Top

(1) Molecular Weight (mw) based Drug Clustering

(2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering

(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering

(4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering

(5) Rotatable Bond Count (rotbonds) based Drug Clustering

(6) Topological Polar Surface Area (polararea) based Drug Clustering

"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

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Co-Targets

Co-Targets Info

Target-Related Models and Studies

Top

Target Validation

Target Validation Info

References

Top

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

Drug information of Josamycin, 2008. eduDrugs.

REF 4

Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

REF 5

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 6

How many modes of action should an antibiotic have Curr Opin Pharmacol. 2008 Oct;8(5):564-73.

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 (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 13

ClinicalTrials.gov (NCT04370548) DARE-BV1 in the Treatment of Bacterial Vaginosis (DARE-BVFREE). 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

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 800005626)

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 800019101)

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

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 32

Retapamulin inhibition of translation and 50S ribosomal subunit formation in Staphylococcus aureus cells. Antimicrob Agents Chemother. 2007 Sep;51(9):3385-7.

REF 33

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 34

Clinical pharmacokinetics of telithromycin, the first ketolide antibacterial. Clin Pharmacokinet. 2005;44(9):915-34.

REF 35

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 36

The ChEMBL database in 2017. Nucleic Acids Res. 2017 Jan 4;45(D1):D945-D954.

REF 37

Company report (briva)

REF 38

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 39

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 40

Pfizer. Product Development Pipeline. March 31 2009.

REF 41

Time-resolved binding of azithromycin to Escherichia coli ribosomes. J Mol Biol. 2009 Jan 30;385(4):1179-92.

REF 42

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 43

Structure-activity relationships for six ketolide antibiotics. Curr Microbiol. 2001 Mar;42(3):203-10.

REF 44

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 45

DOI: 10.1038/nrd2202

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