Target Information

Target General Infomation
Target ID
T64410
Former ID
TTDS00182
Target Name
D-alanyl-D-alanine carboxypeptidase
Gene Name
vanYB
Synonyms
D-alanyl-D-alanine carboxypeptidase-transpeptidase; DD-carboxypeptidase; DD-peptidase; vanYB
Target Type
Successful
Disease Bacterial infections [ICD9: 001-009, 010-018, 020-027, 030-041, 080-088, 090-099, 100-104; ICD10: A00-B99]
Gram-positive bacterial infection [ICD9: 001-009, 010-018, 020-027, 030-041, 080-088, 090-099, 100-104]
Function
Vancomycin-inducible, penicillin-resistant, DD- carboxypeptidase that hydrolyzes depsipeptide- and D-alanyl-D- alanine-containing peptidoglycan precursors. Insensitive to beta- lactams.
BioChemical Class
Peptidase
Target Validation
T64410
UniProt ID
Q47746
EC Number
EC 3.4.16.4
Sequence
MEKSNYHSNVNHHKRHMKQSGEKRAFLWAFIISFTVCTLFLGWRLVSVLEATQLPPIPAT
HTGSGTGVAENPEENTLATAKEQGDEQEWSLILVNRQNPIPAQYDVELEQLSNGERIDIR
ISPYLQDLFDAARADGVYPIVASGYRTTEKQQEIMDEKVAEYKAKGYTSAQAKAEAETWV
AVPGTSEHQLGLAVDINADGIHSTGNEVYRWLDENSYRFGFIRRYPPDKTEITGVSNEPW
HYRYVGIEAATKIYHQGLCLEEYLNTEK
Drugs and Mode of Action
Drug(s) B-Lactams Drug Info Approved Bacterial infections [536854]
Cefalotin Drug Info Approved Bacterial infections [549818]
Cefotaxime Drug Info Approved Bacterial infections [538212]
Cephalosporin Drug Info Approved Bacterial infections [550623]
TD-1792 Drug Info Phase 2 Gram-positive bacterial infection [521976]
Inhibitor 2-[(Dioxidophosphino)Oxy]Benzoate Drug Info [551393]
3-boronobenzoic acid Drug Info [530358]
5-boronothiophene-2-carboxylic acid Drug Info [530358]
B-Lactams Drug Info [536854]
Benzo[c][1,2]oxaborol-1(3H)-ol Drug Info [530358]
Cefalotin Drug Info [537844]
Cefotaxime Drug Info [536459], [537844]
Cephalosporin C Drug Info [551391]
D-Alanine Drug Info [551393]
Formaldehyde Drug Info [551393]
Glycyl-L-Alpha-Amino-Epsilon-Pimelyl-D-Alanine Drug Info [551393]
NITROCEFIN Drug Info [551374]
Phenyl Boronic acid Drug Info [530358]
TD-1792 Drug Info [536773]
Binder Cephalosporin Drug Info [535110]
References
Ref 521976ClinicalTrials.gov (NCT00442832) TD-1792 in Gram-positive Complicated Skin and Skin Structure Infection. U.S. National Institutes of Health.
Ref 536854Has nature already identified all useful antibacterial targets? Curr Opin Microbiol. 2008 Oct;11(5):387-92. Epub 2008 Oct 6.
Ref 538212FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 064200.
Ref 549818Cefalotin - FDA approved drug information (drug label) from DailyMed.
Ref 550623The Cephalosporin Antimicrobial Agents: A Comprehensive Review. J Vet Pharmacol Ther 11 (1):1-32. 1988.
Ref 530358J Med Chem. 2009 Oct 8;52(19):6097-106.Synthesis and evaluation of 3-(dihydroxyboryl)benzoic acids as D,D-carboxypeptidase R39 inhibitors.
Ref 535110A 1.2-A snapshot of the final step of bacterial cell wall biosynthesis. Proc Natl Acad Sci U S A. 2001 Feb 13;98(4):1427-31.
Ref 536459Extended-spectrum cephalosporinases: structure, detection and epidemiology. Future Microbiol. 2007 Jun;2:297-307.
Ref 536773How many modes of action should an antibiotic have? Curr Opin Pharmacol. 2008 Oct;8(5):564-73. Epub 2008 Jul 30.
Ref 536854Has nature already identified all useful antibacterial targets? Curr Opin Microbiol. 2008 Oct;11(5):387-92. Epub 2008 Oct 6.
Ref 537844Binding of cephalothin and cefotaxime to D-ala-D-ala-peptidase reveals a functional basis of a natural mutation in a low-affinity penicillin-binding protein and in extended-spectrum beta-lactamases. Biochemistry. 1995 Jul 25;34(29):9532-40.
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
Ref 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.

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