Antimicrobial Peptide AP02203

     
 

APD ID:

AP02203

 
 

Name/Class:

Natural form A21978C1 (XXL; XXD3; XXM; lactone, XXJ; UCSB1b; Gram-positive bacteria, prokaryotes; BBII, BBW; derivatives: Daptomycin, cubicin, LY146032; LY 146032; lipopeptides)

 
 

Source:

Streptomyces roseosporus

 
 

Sequence:

WNDTGKDADGSEY

 
 

Length:

13

 
 

Net charge:

-3

 
 

Hydrophobic residue%:

15%

 
 

Boman Index:

3.48 kcal/mol

 
 

3D Structure:

nonhelixbeta

 
 

Method:

NMR

 
 

SwissProt ID:

Reference ID: Ref  

 
 

Activity:

Anti-Gram+,

 
 

Crucial residues:

Ca2+, lipid tail, and the ring structure

 
 

Additional info:

Drug/AMPs in use: Daptomycin was approved by FDA in 2003 to treat soft-tissue infections, and in 2006 to treat S. aureus bacteremia and right-sided endocarditis.

Warning: the sequence is a close mimic of the natural counterpart. The natural form is cyclic due to the ester bond between the hydroxyl of T4 and the carboxyl of kynurenine-13 (represented by Y here). In daptomycin, the N-terminus is lipidated with n-decanoyl fatty acid chain to repalce the C11 branched fatty acid in the natural form of A21978C1 (Eliopoulos GM et al., 1985). Other nonstandard amino acids include ornithine-6 (represented with K), (2S,3R)-3-methyl-glutamic acid-12 (represented with E), and three D-amino acids at positions N2, A8, and S11.

Activity: Natural form is active against various Gram-positive bacteria S. aureus, S. faecalis, S. epidermidis (MIC 0.125-0.5 ug/ml), L. monocytogenes (MIC 4-16 ug/ml), S. pyogenes (MIC <0.06 ug/ml), S. agalactiae (MIC 0.25-0.5 ug/ml), group G. streptococci (MIC <0.06 ug/ml), V. streptococci (MIC <0.06-4 ug/ml), S. pneumoniae (MIC <0.06-0.125 ug/ml). This is another anionic peptide that is distinct from many of the cationic AMPs. Its activity requires the presence of Ca2+ (calcium) that causes the aggregation of the peptide. Updated 5/2019; Jan2020

 
       
 

Title:

In vitro and in vivo activity of LY 146032, a new cyclic lipopeptide antibiotic.

 
 

Author:

Eliopoulos GM, Willey S, Reiszner E, Spitzer PG, Caputo G, Moellering RC Jr. 1986

 
 

Reference:

Antimicrob Agents Chemother. 1986 Oct;30(4):532-5.Pub-Med.

 
       

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