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Short Peptides with Induced β-Turn Inhibit the Interaction between HIV-1 gp120 and CD4

 Yo Han Choi  ;  Won Sang Rho  ;  Nam Doo Kim  ;  Sang Jin Park  ;  Dong Hyuk Shin  ;  Jong Woo Kim  ;  Sung Hyuk Im  ;  Ho Sik Won  ;  Chang Woo Lee  ;  Chi Bom Chae  ;  Young Chul Sung 
 Journal of Medicinal Chemistry, Vol.44(9) : 1356-1363, 2001 
Journal Title
 Journal of Medicinal Chemistry 
Issue Date
Amino Acid Sequence ; Anti-HIV Agents/chemistry* ; Anti-HIV Agents/metabolism ; Anti-HIV Agents/pharmacology ; Base Sequence ; CD4 Antigens/chemistry* ; CD4 Antigens/metabolism ; Coliphages/chemistry* ; Coliphages/genetics ; Coliphages/metabolism ; Crystallography, X-Ray ; HIV Envelope Protein gp120/chemistry* ; HIV Envelope Protein gp120/metabolism ; Magnetic Resonance Spectroscopy ; Models, Molecular ; Molecular Sequence Data ; Oligopeptides/chemistry* ; Oligopeptides/genetics ; Oligopeptides/metabolism ; Oligopeptides/pharmacology ; Peptide Library* ; Protein Structure, Secondary
To identify novel peptides that inhibit the interaction between human immunodeficiency virus type 1 (HIV-1) envelope glycoprotein gp120 and CD4, we constructed a targeted phage-displayed peptide library in which phenylalanine and proline were fixed at the fourth and sixth positions, respectively, because Phe43 and the adjacent beta-turn of CD4 are critical for interaction with gp120. Two synthetic peptides were selected after three rounds of biopanning against gp120, and one of them, G1 peptide (ARQPSFDLQCGF), exhibited specific inhibition of the interaction between gp120 and CD4 with an IC(50) of about 50 microM. Structural analysis using NMR demonstrated that G1 peptide forms a compact cyclic structure similar to the CD4 region interacting with gp120. Two derivatives of G1 peptide, a linear hexameric peptide (G1-6) and a cyclic nonameric peptide (G1-c), were synthesized based on the structure of the G1 peptide. Interestingly, they showed higher inhibitory activities than did G1 peptide with IC(50)'s of 6 and 1 microM, respectively. Thus, this study might provide a new insight into the development of anti-HIV-1 inhibitors.
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5. Research Institutes (연구소) > Liver Cirrhosis Clinical Research Center (간경변증임상연구센터) > 1. Journal Papers
Yonsei Authors
Ro, Simon Weonsang(노원상) ORCID logo https://orcid.org/0000-0003-2187-3698
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