Structure-antiviral activity relationships of cecropin A-magainin 2 hybrid peptide and its analogues.
In order to elucidate the structure-antiviral activity relationship of cecropin A (1-8)-magainin 2 (1-12) (termed CA-MA) hybrid peptide, several analogues with amino acid substitutions were synthesized. In a previous study, it was shown that serine at position 16 in CA-MA hybrid peptide was very important for antimicrobial activity. Analogues were designed to increase the hydrophobic property by substituting a hydrophobic amino acid residue (S --> A, V, F or W, position 16) in the CA-MA hybrid peptide. In this study, the structure-antiviral activity relationships of CA-MA and its analogues were investigated. In particular, substitution of Ser with a hydrophobic amino acid, Val, Phe or Trp at position 16 caused a dramatic increase in the virus-cell fusion inhibitory activity. These results suggested that the hydrophobicity at position 16 in the hydrophobic region of CA-MA is important for potent antiviral activity.
Lee
Dong Gun
DG
School of Life Science and Biotechnology, College of Natural Sciences, Kyungpook National University, 1370 Sankyuk-dong, Puk-ku, Taegu 702-701, Korea.
Park
Yoonkyung
Y
Jin
Ingnyol
I
Hahm
Kyung-Soo
KS
Lee
Hyang-Hee
HH
Moon
Young-Hee
YH
Woo
Eun-Rhan
ER
D000818:Animals; D000890:Anti-Infective Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D023181:Antimicrobial Cationic Peptides / Q000138:chemical synthesis / Q000494:pharmacology*; D015704:CD4 Antigens / Q000235:genetics / Q000378:metabolism; D002522:Chlorocebus aethiops; D015726:Giant Cells / Q000187:drug effects; D015699:HIV Envelope Protein gp120 / Q000235:genetics / Q000378:metabolism*; D015700:HIV Envelope Protein gp41 / Q000235:genetics / Q000378:metabolism*; D015497:HIV-1 / Q000235:genetics / Q000378:metabolism*; D006367:HeLa Cells; D006801:Humans; D054806:Magainins; D011993:Recombinant Fusion Proteins / Q000138:chemical synthesis / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014616:Vaccinia virus / Q000235:genetics; D014709:Vero Cells; D029867:Xenopus Proteins / Q000138:chemical synthesis / Q000494:pharmacology*
D000890:Anti-Infective Agents; D023181:Antimicrobial Cationic Peptides; D015704:CD4 Antigens; D015699:HIV Envelope Protein gp120; D015700:HIV Envelope Protein gp41; D054806:Magainins; D011993:Recombinant Fusion Proteins; D029867:Xenopus Proteins; C053301:magainin 2 peptide, Xenopus; C031161:cecropin A