Target Information

Target General Information

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Target ID

T62094 (Former ID: TTDI01930)

Target Name

Bacterial 30S ribosomal RNA (Bact 30S rRNA)

Gene Name

NO-GeName

Target Type

Successful target

[1]

Disease

[+] 7 Target-related Diseases

Acne vulgaris [ICD-11: ED80]

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

Gingival/edentulous alveolar ridge disorder [ICD-11: DA0D]

Infectious gastroenteritis/colitis [ICD-11: 1A40]

Periodontal disease [ICD-11: DA0C]

Pneumonia [ICD-11: CA40]

Skin sensation disturbance [ICD-11: ME65]

UniProt ID

NOUNIPROTAC

Drugs and Modes of Action

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Approved Drug(s)

[+] 7 Approved Drugs

Doxycycline

Drug Info

Approved

Chronic periodontitis

[2], [3]

Gentamicin

Drug Info

Approved

Bacterial infection

[3], [4]

Nitrofurazone

Drug Info

Approved

Skin burns

[5]

Omadacycline

Drug Info

Approved

Acute bacterial skin infection

[6]

Sarecycline

Drug Info

Approved

Acne vulgaris

[7]

Tobramycin

Drug Info

Approved

Bacterial infection

[3]

TP-434

Drug Info

Approved

Intra-abdominal infection

[8]

Clinical Trial Drug(s)

[+] 1 Clinical Trial Drugs

ME1100

Drug Info

Phase 1

Bacterial pneumonia

[11]

Discontinued Drug(s)

[+] 2 Discontinued Drugs

Wetimicin

Drug Info

Discontinued in Phase 1

Infectious disease

[12]

DACTIMICIN

Drug Info

Terminated

Bacterial infection

[13]

Mode of Action

[+] 2 Modes of Action

Modulator

[+] 3 Modulator drugs

Doxycycline

Drug Info

[14]

Gentamicin

Drug Info

[14]

Tobramycin

Drug Info

[15]

Inhibitor

[+] 7 Inhibitor drugs

Nitrofurazone

Drug Info

[1]

Omadacycline

Drug Info

[6]

Sarecycline

Drug Info

[7]

TP-434

Drug Info

[8]

ME1100

Drug Info

[16]

Wetimicin

Drug Info

[17]

DACTIMICIN

Drug Info

[18]

Drug Property Profile of Target

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(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

References

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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

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 (NCT03691584) Phase 1, Safety and Bronchopulmonary PK Study in Healthy Volunteers (BAL). U.S. National Institutes of Health.

REF 10

ClinicalTrials.gov (NCT03234738) A Phase 1 Safety and PK Study of IV TP-271. U.S. National Institutes of Health.

REF 11

ClinicalTrials.gov (NCT01907776) Pharmacokinetics and Safety Study of ME1100 in Healthy Volunteers. 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

Cross susceptibility of ototoxicity about aminoglycoside antibiotics. Lin Chuang Er Bi Yan Hou Ke Za Zhi. 1997 Jan;11(1):9-10.

REF 18

Aminoglycosides: Activity and Resistance. Antimicrob Agents Chemother. 1999 April; 43(4): 727-737.

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