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

General Information of Drug (ID: DMGFPU2)

• Drug Name: Linezolid Drug Info
• Synonyms: Linezlid; ZLD; Zyvox; Zyvoxa; Zyvoxam; Zyvoxid; PNU 100766; U 100766; Linezolid & VRC3375; Linezolid [USAN:INN]; PNU-100766; U-100766; Zyvox (TN); Zyvoxam (TN); Zyvoxid (TN); NDA 21-130 Zyvox (linezolid tablets); NDA 21-131 Zyvox for injection (linezolid injection); NDA 21-132 Zyvox oral suspension (linzolid oral suspension); Linezolid (JAN/USAN/INN); PNU-100766, U-100766, Zyvoxid, Zyvoxam, Linezolid; N-((3-(3-fluoro-4-morpholinylphenyl)-2-oxo-5-oxazolidinyl)methyl)acetamide; N-(((S)-3-(3-Fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl)methyl)acetamide; N-[[(5S)-3-(3-fluoro-4-morpholin-4-ylphenyl)-2-oxo-1,3-oxazolidin-5-yl]methyl]acetamide; N-({5S)-3-[3-Fluoro-4-(4-morpholinyl)phenyl]-2-oxo-1,3-oxazolidin-5-yl}methyl)acetamide, N-[[(S)-3-(3-Fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl]methyl]acetamide; (S)-N-[[3-(3-fluoro-4-morpholinylphenyl)-2-oxo-5-oxazolidinyl]methyl]acetamide; 111GE017

Indication

Disease Entry	ICD 11	Status	REF
Bacteremia	1A73	Approved	[1]
Bacterial infection	1A00-1C4Z	Approved	[2]
Staphylococcal pneumonia		Approved	[1]
Staphylococcus aureus infection		Approved	[1]
Coronavirus Disease 2019 (COVID-19)	1D6Y	Investigative	[3]
Skin infection	1F28-1G0Z	Investigative	[1]

• Therapeutic Class: Antibiotics
• Cross-matching ID:
  PubChem CID: 441401
  ChEBI ID: CHEBI:63607
  CAS Number: CAS 165800-03-3
  TTD Drug ID: DMGFPU2
  VARIDT Drug ID: DR00748
  ACDINA Drug ID: D00367

Molecule-Related Drug Atlas

Drug(s) Targeting Bacterial 23S ribosomal RNA (Bact 23S rRNA)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Lopinavir	DMITQS0	Human immunodeficiency virus infection	1C62	Approved	[6]
Chloramphenicol	DMFXEWT	Bacterial infection	1A00-1C4Z	Approved	[7]
Thiamphenicol	DMDRKH2	Bacterial infection	1A00-1C4Z	Approved	[8]
Lefamulin	DME6G97	Community-acquired pneumonia	CA40.Z	Approved	[9]
Spiramycin	DM20R5F	Bacterial infection	1A00-1C4Z	Approved	[10]
Macrolides	DM3BS97	Bacterial infection	1A00-1C4Z	Approved	[11]
Cethromycin	DMIGX84	Bacterial infection	1A00-1C4Z	Phase 3	[12]
Oxazolidinones	DMBM47Z	Gram-positive bacterial infection	1B74-1G40	Phase 2	[13]
EDP-420	DM5WZ0O	Bacterial infection	1A00-1C4Z	Phase 2	[14]
Micrococcin	DMJ4D1P	Discovery agent	N.A.	Investigative	[10]

Drug(s) Affected By Amine oxidase A (MAOA)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[15]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[16]
Troglitazone	DM3VFPD	Diabetic complication	5A2Y	Approved	[17]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[18]
Cyclophosphamide	DM4O2Z7	Advanced cancer	2A00-2F9Z	Approved	[19]
Selegiline	DM6034S	Major depressive disorder	6A70.3	Approved	[20]
Arsenic trioxide	DM61TA4	Acute lymphoblastic leukaemia	2A85	Approved	[21]
Ciclosporin	DMAZJFX	Graft-versus-host disease	4B24	Approved	[22]
Clorgyline	DMCEUJD	Parkinson disease	8A00.0	Approved	[23]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[24]

Drug(s) Affected By Amine oxidase B (MAOB)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Dopamine	DMPGUCF	Acromegaly	5A60.0	Approved	[25]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[15]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[16]
Troglitazone	DM3VFPD	Diabetic complication	5A2Y	Approved	[26]
Selegiline	DM6034S	Major depressive disorder	6A70.3	Approved	[27]
Calcitriol	DM8ZVJ7	Congenital alopecia	LC30	Approved	[28]
Ciclosporin	DMAZJFX	Graft-versus-host disease	4B24	Approved	[22]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[24]
BENZYL BENZOATE	DMDPYI5	Infestations of lice and scabies	1G00.Z	Approved	[29]
Rosiglitazone	DMILWZR	Chronic kidney disease	GB61	Approved	[26]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Bacterial 23S ribosomal RNA (Bact 23S rRNA)	TTLFGBV	NOUNIPROTAC	Binder	[4]

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Amine oxidase A (MAOA)	OT8NIWMQ	AOFA_HUMAN	Gene/Protein Processing	[5]
Amine oxidase B (MAOB)	OTTDFM1O	AOFB_HUMAN	Gene/Protein Processing	[5]

References

• [1] Linezolid FDA Label
• [2] FDA Approved Drug Products from FDA Official Website. 2019. Application Number: (ANDA) 200222.
• [3] Therapeutic and Triage Strategies for 2019 Novel Coronavirus Disease in Fever Clinics. Lancet Respir Med. 2020 Mar;8(3):e11-e12.
• [4] Genome sequencing of linezolid-resistant Streptococcus pneumoniae mutants reveals novel mechanisms of resistance. Genome Res. 2009 Jul;19(7):1214-23.
• [5] Nonclinical Evaluation of Antibacterial Oxazolidinones Contezolid and Contezolid Acefosamil with Low Serotonergic Neurotoxicity. Chem Res Toxicol. 2021 May 17;34(5):1348-1354. doi: 10.1021/acs.chemrestox.0c00524. Epub 2021 Apr 29.
• [6] Company report (JMI Laboratories)
• [7] Inhibition of peptide bond formation by pleuromutilins: the structure of the 50S ribosomal subunit from Deinococcus radiodurans in complex with tiamulin. Mol Microbiol. 2004 Dec;54(5):1287-94.
• [8] The fused TrpEG from Streptomyces venezuelae is an anthranilate synthase, not a 2-amino-2-deoxyisochorismate [corrected] (ADIC) synthase. Ethn Dis. 2008 Spring;18(2 Suppl 2):S2-9-13.
• [9] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [10] The apicoplast as an antimalarial drug target. Drug Resist Updat. 2001 Jun;4(3):145-51.
• [11] Has nature already identified all useful antibacterial targets Curr Opin Microbiol. 2008 Oct;11(5):387-92.
• [12] How many modes of action should an antibiotic have Curr Opin Pharmacol. 2008 Oct;8(5):564-73.
• [13] Ribosomal RNA is the target for oxazolidinones, a novel class of translational inhibitors. RNA. 1999 Jul;5(7):939-46.
• [14] EDP-420, a Bicyclolide (Bridged Bicyclic Macrolide), Is Active against Mycobacterium avium. Antimicrob Agents Chemother. 2007 May; 51(5): 1666-1670.
• [15] Functional gene expression profile underlying methotrexate-induced senescence in human colon cancer cells. Tumour Biol. 2011 Oct;32(5):965-76.
• [16] Comparison of phenotypic and transcriptomic effects of false-positive genotoxins, true genotoxins and non-genotoxins using HepG2 cells. Mutagenesis. 2011 Sep;26(5):593-604.
• [17] Effects of ciglitazone and troglitazone on the proliferation of human stomach cancer cells. World J Gastroenterol. 2009 Jan 21;15(3):310-20.
• [18] Phenotypic characterization of retinoic acid differentiated SH-SY5Y cells by transcriptional profiling. PLoS One. 2013 May 28;8(5):e63862.
• [19] Comparative gene expression analysis of a chronic myelogenous leukemia cell line resistant to cyclophosphamide using oligonucleotide arrays and response to tyrosine kinase inhibitors. Leuk Res. 2007 Nov;31(11):1511-20.
• [20] Characterizing fucoxanthin as a selective dopamine D(3)/D(4) receptor agonist: Relevance to Parkinson's disease. Chem Biol Interact. 2019 Sep 1;310:108757. doi: 10.1016/j.cbi.2019.108757. Epub 2019 Jul 16.
• [21] Arsenic suppresses gene expression in promyelocytic leukemia cells partly through Sp1 oxidation. Blood. 2005 Jul 1;106(1):304-10.
• [22] Comparison of HepG2 and HepaRG by whole-genome gene expression analysis for the purpose of chemical hazard identification. Toxicol Sci. 2010 May;115(1):66-79.
• [23] Synthesis and study of a series of 3-arylcoumarins as potent and selective monoamine oxidase B inhibitors. J Med Chem. 2011 Oct 27;54(20):7127-37.
• [24] Integrative omics data analyses of repeated dose toxicity of valproic acid in vitro reveal new mechanisms of steatosis induction. Toxicology. 2018 Jan 15;393:160-170.
• [25] Inhibition potential of 3,4-methylenedioxymethamphetamine (MDMA) and its metabolites on the in vitro monoamine oxidase (MAO)-catalyzed deamination of the neurotransmitters serotonin and dopamine. Toxicol Lett. 2016 Jan 22;243:48-55.
• [26] Molecular Insights into Human Monoamine Oxidase B Inhibition by the Glitazone Anti-Diabetes Drugs. ACS Med Chem Lett. 2011 Oct 15;3(1):39-42.
• [27] Chromone, a privileged scaffold for the development of monoamine oxidase inhibitors. J Med Chem. 2011 Jul 28;54(14):5165-73.
• [28] Identification of vitamin D3 target genes in human breast cancer tissue. J Steroid Biochem Mol Biol. 2016 Nov;164:90-97.
• [29] Combining initro and in silico approaches to evaluate the multifunctional profile of rosmarinic acid from Blechnum brasiliense on targets related to neurodegeneration. Chem Biol Interact. 2016 Jul 25;254:135-45.