Antimicrobial Peptide AP00195

     
 

APD ID:

AP00195

 
 

Name/Class:

Protegrin 1 (Protegrin-1, PG-1, IB-200; UCSS1a; cathelicidin, pigs, mammals; animals; XXA, ZZHa, BBBm; Derivatives: Iseganan, protegrin IB 367 (IB-367); Clinical; BBL; JJsn; 2S=S)

 
 

Source:

leukocytes; Pig, Sus scrofa

 
 

Sequence:

RGGRLCYCRRRFCVCVGR

 
 

Length:

18

 
 

Net charge:

7

 
 

Hydrophobic residue%:

44%

 
 

Boman Index:

3.65 kcal/mol

 
 

3D Structure:

Beta

 
 

Method:

NMR

 
 

SwissProt ID:

PDB ID: 1PG1   Go to PDB

 
 

Activity:

Anti-Gram+, Antiviral, Antifungal, Anti-HIV, Anti-MRSA, Antibiofilm,

 
 

Crucial residues:

Disulfide bond for antifungal activity.

 
 

Additional info:

Activity against E. coli 004(MIC 0.12ug/ml), VREF 032 (MIC 0.25ug/ml), P. aeruginosa ATCC 9027 (MIC 0.5ug/ml), MRSA ATCC 33591 (MIC 2ug/ml) and C. albicans ATCC 10231 (MIC 8ug/ml). Active against C. albicans (Cho Y et al., 1998); HSV-1, HSV-2 (Yasin et al., 2000); porcine reproductive and respiratory syndrome virus in vitro (Guo C et al., 2014). Two disulfide bridges: 6,15; 8,13. You can rotate, zoom, and view the 3D structure here in the PDB . The first 4 residues are not esential for antibacterial activity but important for antifungal activity. It probably forms a dimer in membranes. Larger oligomers are possible. The mechanism of action involves "pore" formation (ref). Simulation based on ssNMR work suggests an octomer in membranes (ref). The sequence of IB-367 is RGGLCYCRGRFCVCVGR and the peptide is active against bacteria and fungi. For other IB-peptides derived from PG-1, please refer to Che J et al (2000) Biopolymers 55:88-98. Chen et al. also found that the D- and L-forms of three derivatives showed similar activity (D=L). This peptide showed synergistic effect with LL-37 against P. aeruginosa and E. coli (Yan H & Hancock REW 2001 Antimicrob Agents Chemother 45: 1558-60). PG-1 derivatives were subjected to clinical trials. Animal model:mouse: IB-367 also affects Gram-positive biofilms in vivo of S. aureus and E. faecalis, thereby having the potential of being used as adjuvant agent to linezolid treatment (Ghiselli R et al., 2007). Updated 11/2014; 11/2015; 6/2018.

 
       
 

Title:

Synthesis of protegrin-related peptides and their antibacterial and anti-human immunodeficiency virus activity

 
 

Author:

Tamamura H, Murakami T, Horiuchi S, Sugihara K, Otaka A, Takada W, Ibuka T, Waki M, Yamamoto N, Fujii N.1995

 
 

Reference:

Chem Pharm Bull (Tokyo). 1995 May;43(5):853-8

 
       

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