TY - JOUR
T1 - A low-molecular-weight inhibitor against the chemokine receptor CXCR4
T2 - A strong anti-HIV peptide T140
AU - Tamamura, Hirokazu
AU - Xu, Younong
AU - Hattori, Toshio
AU - Zhang, Xiaoyan
AU - Arakaki, Rieko
AU - Kanbara, Kenji
AU - Omagari, Akane
AU - Otaka, Akira
AU - Ibuka, Toshiro
AU - Yamamoto, Naoki
AU - Nakashima, Hideki
AU - Fujii, Nobutaka
PY - 1998/12/30
Y1 - 1998/12/30
N2 - T22 ([Tyr(5,l2), Lys7]-polyphemusin II) is an 18-residue peptide amide, which has strong anti-HIV activity. T22 inhibits the T cell line-tropic (T-tropic) HIV-1 infection through its specific binding to a chemokine receptor CXCR4, which serves as a coreceptor for the entry of T-tropic HIV-1 strains. Herein, we report our finding of novel 14-residue CXCR4 inhibitors, T134 and T140, on the basis of the T22 structure. In the assays we examined, T140 showed the highest inhibitory activity against HIV-1 entry and the strongest inhibitory effect on the binding of an anti-CXCR4 monoclonal antibody (12G5) to CXCR4 among all the CXCR4 inhibitors that have been reported up to now.
AB - T22 ([Tyr(5,l2), Lys7]-polyphemusin II) is an 18-residue peptide amide, which has strong anti-HIV activity. T22 inhibits the T cell line-tropic (T-tropic) HIV-1 infection through its specific binding to a chemokine receptor CXCR4, which serves as a coreceptor for the entry of T-tropic HIV-1 strains. Herein, we report our finding of novel 14-residue CXCR4 inhibitors, T134 and T140, on the basis of the T22 structure. In the assays we examined, T140 showed the highest inhibitory activity against HIV-1 entry and the strongest inhibitory effect on the binding of an anti-CXCR4 monoclonal antibody (12G5) to CXCR4 among all the CXCR4 inhibitors that have been reported up to now.
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U2 - 10.1006/bbrc.1998.9871
DO - 10.1006/bbrc.1998.9871
M3 - Article
C2 - 9918823
AN - SCOPUS:0032583575
VL - 253
SP - 877
EP - 882
JO - Biochemical and Biophysical Research Communications
JF - Biochemical and Biophysical Research Communications
SN - 0006-291X
IS - 3
ER -