Abstract
T22 ([Tyr5,12, 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.
Publication types
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Comparative Study
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Research Support, Non-U.S. Gov't
MeSH terms
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Amino Acid Sequence
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Anti-HIV Agents / pharmacology*
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Anti-HIV Agents / toxicity
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Antimicrobial Cationic Peptides*
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Benzylamines
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Cells, Cultured
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Chemokine CXCL12
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Chemokines, CXC / pharmacology
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Circular Dichroism
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Cyclams
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DNA-Binding Proteins / chemistry
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HIV-1 / drug effects*
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Heterocyclic Compounds / pharmacology
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Molecular Sequence Data
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Oligopeptides / chemistry
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Oligopeptides / pharmacology*
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Oligopeptides / toxicity
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Peptides / chemistry
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Peptides / pharmacology
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Peptides, Cyclic / chemistry
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Receptors, CXCR4 / antagonists & inhibitors*
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T-Lymphocytes / virology*
Substances
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Anti-HIV Agents
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Antimicrobial Cationic Peptides
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Benzylamines
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Chemokine CXCL12
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Chemokines, CXC
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Cyclams
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DNA-Binding Proteins
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Heterocyclic Compounds
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N-alpha-acetyl-nona-D-arginine amide acetate
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Oligopeptides
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Peptides
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Peptides, Cyclic
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Receptors, CXCR4
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T134 peptide
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TW 70
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tachyplesin peptide, Tachypleus tridentatus
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polyphemusin II
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T22 protein, synthetic
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T140 peptide
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plerixafor