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

General Information of Drug (ID: DMGS6YH)

• Drug Name: PCNOTAXIME GROUP Drug Info
• Synonyms: open; hydrolyzed; C3'-cleaved; (2r)-2-[(R)-{[(2z)-2-(2-Amino-1,3-Thiazol-4-Yl)-2-(Methoxyimino)acetyl]amino}(Carboxy)methyl]-5-Methylidene-5,6-Dihydro-2h-1,3-Thiazine-4-Carboxylic Acid; AC1O43RR; (2R)-2-[(R)-[(2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetamido](carboxy)methyl]-5-methylidene-2,6-dihydro-1,3-thiazine-4-carboxylic acid; (2R)-2-[(1R)-1-[[(2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-methoxyiminoacetyl]amino]-2-hydroxy-2-oxoethyl]-5-methylidene-2H-1,3-thiazine-4-carboxylic acid

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 101666160
  TTD Drug ID: DMGS6YH

Molecule-Related Drug Atlas

Drug(s) Targeting Bacterial Penicillin binding protein 3 (Bact mrcA)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Aztreonam	DMDNJHG	Bacterial infection	1A00-1C4Z	Approved	[2]
Cefmetazole	DM42W1B	Bacterial infection	1A00-1C4Z	Approved	[3]
Cefotiam	DMF5HU6	Respiratory tract infection	CA45	Approved	[4]
Latamoxef	DMANL0D	Bacterial infection	1A00-1C4Z	Approved	[3]
Mezlocillin	DMY5JEP	Acute gonococcal cervicitis		Approved	[5]
Moxalactam Disodium	DMYKUNR	Bacterial infection	1A00-1C4Z	Approved	[6]
Cefmenoxime	DMPLY7B	Bacterial infection	1A00-1C4Z	Approved	[7]
Benzylpenicillin	DMS9503	Actinomycosis		Phase 3	[8]
LYS228	DM23Y6K	Urinary tract infection	GC08	Phase 2	[9]
Cephalosporin C	DMYW3ZG	Discovery agent	N.A.	Investigative	[10]

Drug(s) Targeting Staphylococcus Beta-lactamase (Stap-coc blaZ)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Tazobactam	DM3XNUI	Appendicitis	DB10	Approved	[11]
Clavulanate	DM2FGRT	Bacteremia	1A73	Approved	[12]
CAZ AVI	DMPG4OM	Serious infection	1H0Z	Phase 3	[13]
Enmetazobactam	DMZKTYJ	Urinary tract infection	GC08	Phase 3	[14]
Vaborbactam	DMDCFXJ	Urinary tract infection	GC08	Phase 3	[15]
MK-7655	DMLMV0O	Bacterial infection	1A00-1C4Z	Phase 2	[16]
CXL	DM3JFZ2	Methicillin-resistant staphylococci infection	1A00-1A09	Phase 2	[17]
RASV-Sp	DM4VTX6	Streptococcus infection	1B53	Phase 1	[18]
ME-1071	DMEMQ5J	Bacterial infection	1A00-1C4Z	Phase 1	[19]
OP-0595	DMECVP9	Bacterial infection	1A00-1C4Z	Phase 1	[20]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Bacterial Penicillin binding protein 3 (Bact mrcA)	TT85JMW	FTSI_ECOLI	Inhibitor	[1]
Staphylococcus Beta-lactamase (Stap-coc blaZ)	TTHI19T	BLAC_STAAU	Inhibitor	[1]

References

• [1] The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
• [2] Penicillin-binding protein PBP2 of Escherichia coli localizes preferentially in the lateral wall and at mid-cell in comparison with the old cell pole. Mol Microbiol. 2003 Jan;47(2):539-47.
• [3] Clinical relevance of antibiotic-induced endotoxin release in patients undergoing hepatic resection. World J Surg. 1999 Jan;23(1):75-9.
• [4] Genetic analyses of beta-lactamase negative ampicillin-resistant strains of Haemophilus influenzae isolated in Okinawa, Japan. Jpn J Infect Dis. 2006 Feb;59(1):36-41.
• [5] Bactericidal effect of piperacillin alone and combined. Presse Med. 1986 Dec 20;15(46):2297-302.
• [6] Moxalactam (6059-S), a new 1-oxa-beta-lactam: binding affinity for penicillin-binding proteins of Escherichia coli K-12.
• [7] In vitro evaluation of E1040, a new cephalosporin with potent antipseudomonal activity. Antimicrob Agents Chemother. 1988 May;32(5):693-701.
• [8] Association of amino acid substitutions in penicillin-binding protein 3 with beta-lactam resistance in beta-lactamase-negative ampicillin-resistant Haemophilus influenzae. Antimicrob Agents Chemother. 2001 Jun;45(6):1693-9.
• [9] Mode of Action of the Monobactam LYS228 and Mechanisms Decreasing In Vitro Susceptibility in Escherichia coli and Klebsiella pneumoniae. Antimicrob Agents Chemother. 2018 Sep 24;62(10):e01200-18.
• [10] DrugBank 3.0: a comprehensive resource for 'omics' research on drugs. Nucleic Acids Res. 2011 Jan;39(Database issue):D1035-41.
• [11] Selection of TNF-alpha binding affibody molecules using a beta-lactamase protein fragment complementation assay. N Biotechnol. 2009 Nov 30;26(5):251-9.
• [12] A sensitive coupled HPLC/electrospray mass spectrometry assay for SPM-1 metallo-beta-lactamase inhibitors. Assay Drug Dev Technol. 2009 Apr;7(2):170-9.
• [13] NXL104 irreversibly inhibits the -lactamase from Mycobacterium tuberculosis. Biochemistry. 2012 Jun 5;51(22):4551-7.
• [14] Pharmacodynamics of Cefepime Combined with the Novel Extended-Spectrum--Lactamase (ESBL) Inhibitor Enmetazobactam for Murine Pneumonia Caused by ESBL-Producing Klebsiella pneumoniae. Antimicrob Agents Chemother. 2020 May 21;64(6):e00180-20.
• [15] Vaborbactam: Spectrum of Beta-Lactamase Inhibition and Impact of Resistance Mechanisms on Activity in Enterobacteriaceae. Antimicrob Agents Chemother. 2017 Oct 24;61(11):e01443-17.
• [16] Discovery of MK-7655, a beta-lactamase inhibitor for combination with Primaxin . Bioorg Med Chem Lett. 2014 Feb 1;24(3):780-5.
• [17] Beta-Lactam Antibiotics Renaissance. Antibiotics. 2014, 3(2), 193-215.
• [18] WO patent application no. 2010,0456,20, Recombinant bacterium capable of eliciting an immune response against streptococcus pneumoniae.
• [19] Multidrug-resistant Gram-negative bacterial infections: are you ready for the challenge. Curr Clin Pharmacol. 2014 Feb;9(1):27-38.
• [20] OP0595, a new diazabicyclooctane: mode of action as a serine -lactamase inhibitor, antibiotic and -lactam 'enhancer'. J Antimicrob Chemother. 2015 Oct;70(10):2779-86.