Antimicrobial Peptide AP00172

     
 

APD ID:

AP00172

 
 

Name/Class:

Drosocin (glycopeptide, XXG; Pro-rich; insects, arthropods, invertebrates, animals; BBL; BBPP; BBribo; VIHNN; Derivatives: Dros)

 
 

Source:

Fruit fly, Drosophila melanogaster

 
 

Sequence:

GKPRPYSPRPTSHPRPIRV

 
 

Length:

19

 
 

Net charge:

5

 
 

Hydrophobic residue%:

10%

 
 

Boman Index:

3.65 kcal/mol

 
 

3D Structure:

NonHelixBeta

 
 

Method:

NMR

 
 

SwissProt ID:

PDB ID: 4EZR   Go to PDB

 
 

Activity:

Anti-Gram+ & Gram-, Antiparasitic, Antimalarial,

 
 

Crucial residues:

Glycosylation.

 
 

Additional info:

Activity against F. graminearum (IC50 1 uM), P. indica and R. solani (IC50 <20 uM). It is induced via the IMD pathway. Position T11 is o-glycosylated and important for full activity. Subsequent analysis showed that S7 may also be glycosylated. Turn elements occur near residues 4-7, 10-13, 17, and 18. At modorate concentrations, this peptide, as well as pyrrhocoricin (AP170), is also active against a few bacteria such as B. megaterium (44% homology to E. coli DnaK D-E helix) and M. luteus, E. coli D31 (MIC 0.5-1.0 uM) (Hoffmann R et al. 1999 Biochim Biophys Acta 1426:459-67). You can rotate, zoom, and view the 3D structure of Cterminal fragment in complex with E. coli DnaKhere in the PDB. Mechanism of Action (MOA): It binds to an internal protein target DnaK (Eur J Biochem 2002; 269: 4226-4237). Note that all D-drosocin is inactive (so a non-membrane target) and the L form kills bacteria in hours not in minutes. Recently, it is demonstrated that this apidaecin-type peptide and its analog Dros (sequence: GKPRPYSPRPTSHPRPIRV) blocks the assembly of the large (50S) subunit of the ribosome, thereby inhibiting protein synthesis (Krizsan A et al., 2015). Substituting Pro at positions 3,5,10, and 14 with a hydroxylated Pro residues improved non-glycosylated drosocin activity against E. coli and K. pneumoniae. Modification of Pro at positions 3 and 5 increased peptide stability in mouse serum. The new peptides are not toxic to human cells tested at least 600 ug/ml. Updated 12/2012; 12/2015; 4/2018; 4/2019 GW.

 
       
 

Title:

A novel inducible antibacterial peptide of Drosophila carries an O-glycosylated substitution

 
 

Author:

Bulet P, Dimarcq JL, Hetru C, Lagueux M, Charlet M, Hegy G, Van Dorsselaer A, Hoffmann JA.1993

 
 

Reference:

J Biol Chem. 1993 Jul 15;268(20):14893-7. PubMed.

 
       

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