Neamine derivatives having a nucleobase with a lysine or an arginine as a linker, their synthesis and evaluation as potential inhibitors for HIV TAR-Tat.
Neamine derivatives bearing a nucleobase, adenine, cytosine, guanine or thymine with a lysine or an arginine as a linker have been synthesized and its potential as the inhibitor for HIV TAR-Tat interaction examined. Among them, modified neamine having an arginine-nucleobase showed a higher inhibition than that of the one having a lysine-nucleobase. The difference of the nucleobase anchor did not characterize inhibition specificity. Also, stereochemistry of the amino acid in the compounds causes no difference in the inhibition for TAR-Tat.
Yajima
Saki
S
Department of Applied Chemistry, Shibaura Institute of Technology, 3-4-9 Shibaura, Tokyo 108-8548, Japan.
Shionoya
Hirohito
H
Akagi
Takashi
T
Hamasaki
Keita
K
D000595:Amino Acid Sequence; D000617:Aminoglycosides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001120:Arginine / Q000737:chemistry*; D005601:Framycetin / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015696:Gene Products, tat / Q000037:antagonists & inhibitors*; D008239:Lysine / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D008969:Molecular Sequence Data; D013050:Spectrometry, Fluorescence
D000617:Aminoglycosides; D019380:Anti-HIV Agents; D015696:Gene Products, tat; D005601:Framycetin; C488396:neamine; D001120:Arginine; D008239:Lysine