Antimicrobial Peptide AP00144

     
 

APD ID:

AP00144

 
 

Name/Class:

Magainin 2 (Magainin II, PGS; Hebrew word for "shield"; UCLL1; frog, amphibians, animals. Derivatives: MSI-78, = pexiganan, pexiganan acetate, or cytolex, loxilex; clinical trials; MSI-594; MSI-99.

 
 

Source:

skin; Stomach, African clawed frog, Xenopus laevis, Africa

 
 

Sequence:

GIGKFLHSAKKFGKAFVGEIMNS

 
 

Length:

23

 
 

Net charge:

3

 
 

Hydrophobic residue%:

43%

 
 

Boman Index:

0.41 kcal/mol

 
 

3D Structure:

Helix

 
 

Method:

NMR

 
 

SwissProt ID:

PDB ID: 2MAG   Go to PDB

 
 

Activity:

Anti-Gram+ & Gram-, Antiviral, Antifungal, Antiparasitic, Insecticidal, Spermicidal, Antimalarial, Wound healing, Anticancer

 
 

Additional info:

Discovery: The same peptide sequence was also reproted by Giovannini MG et al in 1987 as PGS without antibacterial data.

Activity description: Active against E. coli D31 (MIC 5 ug/ml), K. pneumoniae, P. putida, S. epidermidis (MIC 10 ug/ml), C. freundii (MIC 30 ug/ml), E. cloacae, E. coli, S. aureus (MIC 50 ug/ml), C. albicans (MIC 80 ug/ml), P. aeruginosa, and S. marcescens (MIC 100 ug/ml). Also S. pyogenes, and S. cerevisiae. Also active against P. falciparum, protozoan P. caudatum, A. castellani and T. pyriformis. Magainin II shows a synergistic effect with cecropin A (J Antimicrob Chemother. 2008; 62:1332-8). MOA: it kills bacteria by targeting membranes and forming a pore (forms D=L). It also inhibits Herpes Simplex Virus type 1 (HSV-1) and HSV-2 (PubMed2004). Magainin II only showed a weak activity against channel catfish virus (ref) as well as P388 leukemia, S180 ascites, and a spontaneous ovarian tumor (Baker et al., 1993). It is also insecticidal (EC50 123 pmol/mg fly).

Structure: Alpha helix: residues 4-21 in TFE, SDS, DPC (for the ref., go to PDB website below). You can rotate, zoom, and view the 3D structure here in the PDB .

Derivative 1: MSI-78 (provided by Ed Ezell) (sequence GIGKFLKKAKKFGKAFVKILKK-NH2) is active against bacteria such as E. coli, S. aureus, and P. aeruginosa and fungi. Pexiganan has wound healing activity. It was subjecte to clinical trials but was not approved by FDA due to the cytotoxicity issue. Derivative 2: MSI-594 (provided by Ed Ezell) (sequence GIGKFLKKAKKGIGAVLKVLTTGL-NH2) is engineered based on magainin and melittin. Derivative 3: NSI-99: transgenic plants: expression of a magainin analog (MSI-99, sequence GIGKFLKSAKKFGKAFVKIKNS-NH2, 22mer, more basic) in tomato and banana reduced bacterial speck disease (Planta. 2003 Feb;216(4):587-96).

Surface immobilization: Magainin has also been covalently immobilized 1995 S L Haynie et al. to a water insoluble resin. Edited 4/2017; updated 9/2017; 8/2019.

 
       
 

Title:

Magainins, a class of antimicrobial peptides from Xenopus skin: isolation, characterization of two active forms, and partial cDNA sequence of a precursor.

 
 

Author:

Zasloff M.1987

 
 

Reference:

Proc Natl Acad Sci U S A. 1987 Aug;84(15):5449-53. PubMed.

 
       

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