Antimicrobial Peptide AP02249

     
 

APD ID:

AP02249

 
 

Name/Class:

Teixobactin (nonribosomally synthesized peptide antibiotic, Gram-negative bacteria, prokaryotes, lactone, XXJ, XXD4; XXM; UCSB1b; BBW)

 
 

Source:

Eleftheria terrae, i-chip technology

 
 

Sequence:

FISQIISTARI

 
 

Length:

11

 
 

Net charge:

1

 
 

Hydrophobic residue%:

54%

 
 

Boman Index:

0.48 kcal/mol

 
 

3D Structure:

Unknown

 
 

SwissProt ID:

Reference ID: Ref  

 
 

Activity:

Anti-Gram+, Anti-MRSA,

 
 

Crucial residues:

 
 

Additional info:

Discovery: A new peptide antibiotic has been discovered via a multichannel device, the iChip, to simultaneously isolate and grow uncultured bacteria.

Structure: An ester bond is formed between the backbone C-terminal Ile carboxylic acid and the side chain of Thr8. In addition, the N-terminal phe is methylated (XXM). There are 4 D-amino acids and enduracididine (represented with an Arg here).

Activity: Active against primarily Gram-positive bacteria, including S. aureus (MSSA and MRSA), E. faecalis (anti-VRE), S. pneumoniae, S. pyogenes, S. agalactiae, B. anthracis, C. difficile, P. acnes, M. tuberculosis H37Rv (MIC 0.005-0.25 ug/ml) (anti-TB), H. influenzae, M. catarrhalis (MIC 2-4 ug/ml), and moderately E. coli MIC (25 ug/ml).

MOA: It seems that this peptide inhibits both peptidoglycan and teichoic acid synthesis, causing cell lysis (Homma et al. 2016).

SAR: One can only increase positive charges to 3 or 4 as an analog with 5 charges shows least activity (Abdel Monaim et al. 2017). Alanine scan reveals that positions 10 and 3 can be changed without affecting activity (Chen et al. 2017). Updated 10/2017.

 
       
 

Title:

A new antibiotic kills pathogens without detectable resistance.

 
 

Author:

Ling LL, Schneider T, Peoples AJ, Spoering AL, Engels I, Conlon BP, Mueller A, Schäberle TF, Hughes DE, Epstein S, Jones M, Lazarides L, Steadman VA, Cohen DR, Felix CR, Fetterman KA, Millett WP, Nitti AG, Zullo AM, Chen C, Lewis K. 2015

 
 

Reference:

Nature. 2015 Jan 22;517(7535):455-9. Pub-Med.

 
       

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