Stronger anti-HIV-1 activity of C-peptide derived from HIV-1 89.6 gp41 C-terminal heptad repeated sequence.
C34-LAI containing amino acids 118 to 151 of the HIV-1(LAI) gp41 ectodomain exhibits potent anti-HIV-1 activity. However, the N-terminal halves of C34 peptides vary more according to the HIV-1 strain than the C-terminal halves. Therefore, an analysis was conducted on the anti-HIV-1 activities of the C34 peptides derived from various HIV-1 strains. C34-89.6 exhibited the strongest anti-HIV-1 activity among the C34 peptides tested. Interestingly, its N-terminal half was more acidic than those of the other C34 peptides, whereas its C-terminal half was more basic. Since the C-peptides derived from the HIV-1(LAI) strain are used extensively, the anti-HIV-1 activities of these peptides were compared between the HIV-1 strains 89.6 and LAI. When using chimeric peptides, it was found that the C-terminal basic region of C34-89.6 was more critical than its N-terminal basic region. The anti-HIV-1 activity of T20-89.6 and C28-89.6 was also stronger than that of T20-LAI and C28-LAI, respectively. The anti-HIV-1 activity of C28-89.6 was weakened when the C-terminal basic residues were changed to the corresponding residues of C28-LAI. However, no conformational differences were found among the C28 peptides. Accordingly, these results imply that introducing the C-terminal basic residues of the HIV-1 89.6 C-peptide may be useful for developing potent anti-HIV-1 drugs.
Seo
Jeong Kon
JK
Systemic Proteomics Research Center, Korea Research Institute of Bioscience and Biotechnology, P.O. Box 115, Yusong, Daejon 305-600, Republic of Korea.
Kim
Hee Kyung
HK
Lee
Tae Young
TY
Hahm
Kyung-Soo
KS
Kim
Kil Lyong
KL
Lee
Myung Kyu
MK
D000595:Amino Acid Sequence; D044966:Anti-Retroviral Agents / Q000737:chemistry* / Q000494:pharmacology; D002460:Cell Line; D015700:HIV Envelope Protein gp41 / Q000737:chemistry* / Q000494:pharmacology; D015658:HIV Infections / Q000188:drug therapy*; D015497:HIV-1 / Q000737:chemistry* / Q000187:drug effects / Q000254:growth & development; D008969:Molecular Sequence Data; D010455:Peptides / Q000737:chemistry* / Q000494:pharmacology
D044966:Anti-Retroviral Agents; D015700:HIV Envelope Protein gp41; D010455:Peptides