Antimicrobial Peptide AP00708

     
 

APD ID:

AP00708

 
 

Name/Class:

GF-17 (GF17; XXA; ZZHs, synthetic; Other derivatives: FK-16; GI-20, FK-13, retro-FK13, or LLAA; GF17d3; GF-17d3; 17BIPHE2; merecidin)

 
 

Source:

NMR-based discovery

 
 

Sequence:

GFKRIVQRIKDFLRNLV

 
 

Length:

17

 
 

Net charge:

5

 
 

Hydrophobic residue%:

47%

 
 

Boman Index:

2.47 kcal/mol

 
 

3D Structure:

Helix

 
 

Method:

NMR

 
 

SwissProt ID:

PDB ID: 2L5M   Go to PDB

 
 

Activity:

Anti-Gram+ & Gram-, Antiviral, Anti-HIV, Anticancer

 
 

Crucial residues:

F17 is critical for inhibiting HIV-1.

 
 

Additional info:

GF-17= G + FK-16: mol. wt 2102.5. The major antimicrobial region of human cathelicidin LL-37 discovered by the NMR method. Active against E. coli ATCC 25922, K. pneumonia ATCC 13883, P. aeruginosa PAO1, and S. aureus USA300 (MIC 3.1-6.2 uM). In complex with membrane-mimetic micelles, GF-17 has a helical structure and interfacial R23 and K25 were found to be essential for antibacterial activity as well as membrane penetration, primarily against G- bacteria (Wang G et al. 2012). You can rotate, zoom, and view the 3D structure of GF-17 bound to SDS micelleshere in the PDB.

FK-16 was demonstrated to have anticancer activity in vitro in 2006 (see the ref) and in vivo in 2013 against colon cancer cells (Ren SX et al. 2013). FK-16 shows antimicrobial and antibiofilm activities against a variety of pathogens after covalently immobilized to the titanium surface (Mishra and Wang, 2017).

FK-13 is the core antimicrobial peptide corresponding to residues 17-29 (sequence: FKRIVQRIKDFLR) of LL-37. Reversal of the sequence of FK-13 led to an LL-37-derived aurein 1.2 analog (LLAA, i.e retro-FK13; sequence RLFDKIRQVIRKF), which remained active against E. coli (Li X et al. 2006 Biochim Biophys Acta 1758: 1203-1214). While FK-13 is also active against HIV-1, retro-FK13 is not (Wang G et al. 2008 Antimicrob Agents Chemother 52: 3438-3440). However, anti-HIV GI-20, corresponding to residues 13-32 of LL-37 with the positions of I13 and G14 swapped (GIKEFKRIVQRIKDFLRNLV), showed the highest therapeutic index.

17BIPHE2 was designed based on the 3D structure of GF17d3 (Wang et al., 2014). 17BIPHE2 is active against the ESKAPE pathogens (MIC 3.1-6.2 uM), including E. faecium, S. aureus, K. pneumoniae, A. baumannii, P. aeruginosa, and Enterobacter species. Updated 4/2013; 10/2013; Jan2014; 4/2016; 4/2017;3/2018; 6/2019.

Go to PubChem for additional information.

 
       
 

Title:

Solution structures of Human LL-37 fragments and NMR-based identification of a minimal membrane-targeting antimicrobial and anticancer region

 
 

Author:

Li X et al. Wang G

 
 

Reference:

J Am Chem Soc. 2006 May 3;128(17):5776-85. PubMed.

 
       

Close this window