119 0

Short peptides with induced β-turn inhibit the interaction between HIV-1 gp120 and CD4

Title
Short peptides with induced β-turn inhibit the interaction between HIV-1 gp120 and CD4
Author
원호식
Issue Date
2001-04
Publisher
AMER CHEMICAL SOC
Citation
JOURNAL OF MEDICINAL CHEMISTRY, v. 44, issue. 9, page. 1356-1363
Abstract
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 β-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 IC50 of about 50 μM. 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 IC50's of 6 and 1 μΜ, respectively. Thus, this study might provide a new insight into the development of anti-HIV-1 inhibitors.
URI
https://pubs.acs.org/doi/10.1021/jm000403%2Bhttps://repository.hanyang.ac.kr/handle/20.500.11754/158575
ISSN
0022-2623
DOI
10.1021/jm000403+
Appears in Collections:
COLLEGE OF SCIENCE AND CONVERGENCE TECHNOLOGY[E](과학기술융합대학) > CHEMICAL AND MOLECULAR ENGINEERING(화학분자공학과) > Articles
Files in This Item:
There are no files associated with this item.
Export
RIS (EndNote)
XLS (Excel)
XML


qrcode

Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.

BROWSE