Target Information

Target General Infomation
Target ID
T33193
Former ID
TTDS00212
Target Name
Penicillin binding protein 3
Gene Name
mrcA
Synonyms
PBP 3; PBP-3; PSPB20; Penicillin-binding protein 3; Peptidoglycan glycosyltransferase 3; Peptidoglycan synthetase ftsI; mrcA
Target Type
Successful
Disease Bacterial infections [ICD9: 001-009, 010-018, 020-027, 030-041, 080-088, 090-099, 100-104; ICD10: A00-B99]
Bacterial respiratory tract infection [ICD10: J13, J15]
Urinary tract infections [ICD9: 599; ICD10: N39.0]
Function
Cell wall formation. Essential for the formation of a septum of the murein sacculus. Synthesis of cross-linked peptidoglycan from the lipid intermediates.
BioChemical Class
Hexosyltransferase
Target Validation
T33193
UniProt ID
P02918
EC Number
EC 2.4.1.129
Sequence
MKFVKYFLILAVCCILLGAGSIYGLYRYIEPQLPDVATLKDVRLQIPMQIYSADGELIAQ
YGEKRRIPVTLDQIPPEMVKAFIATEDSRFYEHHGVDPVGIFRAASVALFSGHASQGAST
ITQQLARNFFLSPERTLMRKIKEVFLAIRIEQLLTKDEILELYLNKIYLGYRAYGVGAAA
QVYFGKTVDQLTLNEMAVIAGLPKAPSTFNPLYSMDRAVARRNVVLSRMLDEGYITQQQF
DQTRTEAINANYHAPEIAFSAPYLSEMVRQEMYNRYGESAYEDGYRIYTTITRKVQQAAQ
QAVRNNVLDYDMRHGYRGPANVLWKVGESAWDNNKITDTLKALPTYGPLLPAAVTSANPQ
QATAMLADGSTVALSMEGVRWARPYRSDTQQGPTPRKVTDVLQTGQQIWVRQVGDAWWLA
QVPEVNSALVSINPQNGAVMALVGGFDFNQSKFNRATQALRQVGSNIKPFLYTAAMDKGL
TLASMLNDVPISRWDASAGSDWQPKNSPPQYAGPIRLRQGLGQSKNVVMVRAMRAMGVDY
AAEYLQRFGFPAQNIVHTESLALGSASFTPMQVARGYAVMANGGFLVDPWFISKIENDQG
GVIFEAKPKVACPECDIPVIYGDTQKSNVLENNDVEDVAISREQQNVSVPMPQLEQANQA
LVAKTGAQEYAPHVINTPLAFLIKSALNTNIFGEPGWQGTGWRAGRDLQRRDIGGKTGTT
NSSKDAWFSGYGPGVVTSVWIGFDDHRRNLGHTTASGAIKDQISGYEGGAKSAQPAWDAY
MKAVLEGVPEQPLTPPPGIVTVNIDRSTGQLANGGNSREEYFIEGTQPTQQAVHEVGTTI
IDNGEAQELF
Structure
2ZC5; 2ZC6
Drugs and Mode of Action
Drug(s) Aztreonam Drug Info Approved Bacterial infections [536361]
Cefmenoxime Drug Info Approved Bacterial infections [536361]
Cefmetazole Drug Info Approved Bacterial infections [538602]
Cefotiam Drug Info Approved Bacterial respiratory tract infection [536361], [551871]
Latamoxef Drug Info Approved Bacterial infections [538144]
Mezlocillin Drug Info Approved Urinary tract infections [538601], [551871]
Moxalactam Disodium Drug Info Approved Bacterial infections [551871]
Benzylpenicillin Drug Info Phase 3 Discovery agent [523554]
Binder Acylureido penicillin mezlocillin Drug Info [537787]
Aztreonam Drug Info [535671]
Benzylpenicillin Drug Info [535176]
Cefmenoxime Drug Info [537736]
Cefmetazole Drug Info [538144]
Cefotiam Drug Info [536184]
Latamoxef Drug Info [538144]
Mezlocillin Drug Info [537719]
Antagonist Cephalosporin C Drug Info [551391]
Modulator Moxalactam Disodium Drug Info
Inhibitor PCNOTAXIME GROUP Drug Info [551374]
References
Ref 523554ClinicalTrials.gov (NCT01399723) Amoxicillin Versus Benzyl Penicillin for Treatment of Children Hospitalised With Severe Pneumonia. U.S. National Institutes of Health.
Ref 536361Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20.
Ref 538144Clinical relevance of antibiotic-induced endotoxin release in patients undergoing hepatic resection. World J Surg. 1999 Jan;23(1):75-9.
Ref 538601FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 050549.
Ref 538602FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 050637.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 535176Association 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.
Ref 535671Penicillin-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.
Ref 536184Genetic 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.
Ref 537719Bactericidal effect of piperacillin alone and combined. Presse Med. 1986 Dec 20;15(46):2297-302.
Ref 537736In vitro evaluation of E1040, a new cephalosporin with potent antipseudomonal activity. Antimicrob Agents Chemother. 1988 May;32(5):693-701.
Ref 537787Microbiology, pharmacology, and clinical use of mezlocillin sodium. Pharmacotherapy. 1982 Nov-Dec;2(6):300-12.
Ref 538144Clinical relevance of antibiotic-induced endotoxin release in patients undergoing hepatic resection. World J Surg. 1999 Jan;23(1):75-9.
Ref 551374The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
Ref 551391DrugBank 3.0: a comprehensive resource for 'omics' research on drugs. Nucleic Acids Res. 2011 Jan;39(Database issue):D1035-4. Nucleic Acids Res. 2011 January

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