Details of the Drug-Related molecule(s) Interaction Atlas

General Information of DTT (ID: TTUWYEA)

• DTT Name: Bacterial 50S ribosomal RNA (Bact 50S rRNA) DTT Info
• Gene Name: Bact 50S rRNA

Molecule-Related Drug & Molecule List

13 Approved Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Clarithromycin	DM4M1SG	Acute maxillary sinusitis		Approved	[1]
Clindamycin	DM15HL8	Acne vulgaris	ED80	Approved	[1]
Dalfopristin	DM4LTKV	Bacterial infection	1A00-1C4Z	Approved	[2]
Dirithromycin	DM0D9YJ	Bacterial infection	1A00-1C4Z	Approved	[3]
Erythromycin	DM4K7GQ	Acne vulgaris	ED80	Approved	[4]
Gentamicine sulfate	DMBT7MI	Bacterial infection	1A00-1C4Z	Approved	[5]
Josamycin	DMKJ8LB	Bacterial infection	1A00-1C4Z	Approved	[6]
Lincomycin	DMVTHER	Gram-positive bacterial infection	1B74-1G40	Approved	[7]
Retapamulin	DM9JXB7	Impetigo	1B72	Approved	[8]
Tedizolid	DMG2SKR	Skin infection	1F28-1G0Z	Approved	[9]
Telithromycin	DMZ4P3A	Bacterial infection	1A00-1C4Z	Approved	[10]
Troleandomycin	DMUZNIG	Bacterial infection	1A00-1C4Z	Approved	[11]
Zithromax	DMN4H2O	Syphilis infection	1A6Z	Approved	[12]

5 Clinical Trial Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
DARE-BV1	DM1C95G	Bacterial vaginosis	MF3A	Phase 3	[13]
Solithromycin	DM6QZIA	Bacillus anthracis infection	1G40	Phase 3	[14]
BC-7013	DMMKCJ6	Skin infection	1F28-1G0Z	Phase 2	[15]
GSK-1399686	DM6HBGN	Inflammatory bowel disease	DD72	Phase 2	[16]
BC-3205	DMGFABM	Respiratory tract infection	CA45	Phase 1	[17]

5 Discontinued Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Roxithromycin	DMVMIK2	Bacterial infection	1A00-1C4Z	Withdrawn from market	[18]
Eperezolid	DMCU1WO	Bacterial infection	1A00-1C4Z	Discontinued in Phase 3	[19]
Evernimicin	DM159U2	Bacterial infection	1A00-1C4Z	Discontinued in Phase 3	[20]
HMR-3562	DMKA612	Bacterial infection	1A00-1C4Z	Discontinued in Phase 1	[21]
HMR-3787	DMCHFIT	Bacterial infection	1A00-1C4Z	Terminated	[21]

2 Preclinical Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
RANBEZOLID HYDROCHLORIDE	DMRZBM7	Bacterial infection	1A00-1C4Z	Preclinical	[22]
RX-01-423	DM3AIQO	Bacterial infection	1A00-1C4Z	Preclinical	[23]

1 Investigative Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Erythromycin salnacedin	DM0PHEW	Discovery agent	N.A.	Investigative	[12]

References

• [1] Structural basis for the interaction of antibiotics with the peptidyl transferase centre in eubacteria. Nature. 2001 Oct 25;413(6858):814-21.
• [2] The streptogramin antibiotics: update on their mechanism of action. Expert Opin Investig Drugs. 1998 Apr;7(4):591-9.
• [3] Review of macrolides and ketolides: focus on respiratory tract infections. Drugs. 2001;61(4):443-98.
• [4] 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.
• [5] The protein synthesis inhibitors, oxazolidinones and chloramphenicol, cause extensive translational inaccuracy in vivo. J Mol Biol. 2002 Sep 13;322(2):273-9.
• [6] 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.
• [7] 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.
• [8] Retapamulin inhibition of translation and 50S ribosomal subunit formation in Staphylococcus aureus cells. Antimicrob Agents Chemother. 2007 Sep;51(9):3385-7.
• [9] 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
• [10] 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.
• [11] Depression of colony formation by human thymus-derived lymphocytes with rifampin and other antimicrobial agents. J Infect Dis. 1981 Jun;143(6):832-5.
• [12] The ChEMBL database in 2017. Nucleic Acids Res. 2017 Jan 4;45(D1):D945-D954.
• [13] Characterization of Escherichia coli 50S ribosomal protein L31. FEMS Microbiol Lett. 1999 Nov 15;180(2):345-9.
• [14] Company report (cempra)
• [15] Company report (briva)
• [16] 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.
• [17] 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.
• [18] Molecular insights into 14-membered macrolides using the MM-PBSA method. J Chem Inf Model. 2009 Jun;49(6):1558-67.
• [19] The oxazolidinone eperezolid binds to the 50S ribosomal subunit and competes with binding of chloramphenicol and lincomycin.
• [20] 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.
• [21] Structure-activity relationships for six ketolide antibiotics. Curr Microbiol. 2001 Mar;42(3):203-10.
• [22] 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.
• [23] DOI: 10.1038/nrd2202