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Titolo:
INHIBITION OF INFECTION OF T-CELLS WITH HUMAN-IMMUNODEFICIENCY-VIRUS TYPE-1 BY DIDEOXYNUCLEOSIDES CONJUGATED WITH OLIGOPEPTIDES
Autore:
SHIMIZU NS; HANDA A; SHIMIZU NG; IKEDA R; UCHIYAMA T; ACHIWA K; HOSHINO H;
Indirizzi:
GUNMA UNIV,SCH MED,DEPT HYG & VIROL,SHOWA MACHI MAEBASHI GUMMA 371 JAPAN GUNMA UNIV,SCH MED,DEPT HYG & VIROL MAEBASHI GUMMA 371 JAPAN NIPPON KAYAKU CO LTD,INFECT DIS LAB TAKASAKI GUMMA 37012 JAPAN UNIV SHIZUOKA,SCH PHARMACEUT SCI SHIZUOKA 422 JAPAN
Titolo Testata:
Antiviral chemistry & chemotherapy
fascicolo: 1, volume: 6, anno: 1995,
pagine: 17 - 24
SICI:
0956-3202(1995)6:1<17:IOIOTW>2.0.ZU;2-H
Fonte:
ISI
Lingua:
ENG
Soggetto:
AIDS-RELATED COMPLEX; PLACEBO-CONTROLLED TRIAL; RECOMBINANT SOLUBLE CD4; AZIDOTHYMIDINE AZT; DOUBLE-BLIND; THERAPY; INVITRO; RECEPTOR; BINDING; GP120;
Keywords:
ANTIVIRAL AGENTS; CD4; CYTOTOXICITY; 2',3'-DIDEOXYNUCLEOSIDE DERIVATIVE; HIV-1; OLIGOPEPTIDE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
32
Recensione:
Indirizzi per estratti:
Citazione:
N.S. Shimizu et al., "INHIBITION OF INFECTION OF T-CELLS WITH HUMAN-IMMUNODEFICIENCY-VIRUS TYPE-1 BY DIDEOXYNUCLEOSIDES CONJUGATED WITH OLIGOPEPTIDES", Antiviral chemistry & chemotherapy, 6(1), 1995, pp. 17-24

Abstract

We conjugated nucleoside derivatives that have anti-HIV-1 activities with oligopeptides that should bind to the gp120 of the HIV-1 virion, and examined their anti-HIV-1 activities. These derivates included 3'-azido-2',3'dideoxythymidine (AZT), 2',3'-dideoxyuridine (ddU), 2',3'-dideoxycytidine (ddC), 2',3'-dideoxyinosine (ddl) and 2',3'-dideoxyadenine (ddA). Dipeptides consisting of N-carbomethoxy-carbonyl-prolyl-phenylalanyl-benzyl ester (CPF) and oligopeptides derived from the complementarity-determining region 2 (CDRS) of domain 1 of CD4 were synthesized. The N-terminals of these peptides were conjugated with the 5'OH of AZT, ddU, ddC, ddl or ddA through carbonyl moieties. CPF conjugated with AZT, ddC, ddl or ddA through two-carbonyl moieties exhibited powerful anti-HIV-1 activity, which was similar to that of the respective nucleosides when compared at the same molar concentration. No complex compound connected by a one-carbonyl moiety had anti-HIV-1 activity, whereas a tetrapeptide or octapeptide of the CDR2 region combined with AZT did have such activity. The toxicity of these CPF-containing compounds to human peripheral blood lymphocytes was slightly weaker than the toxicities of the corresponding nucleosides lacking CPF. Antiviral nucleosides containing oligopeptides may be used as lead compounds in an effort to isolate more effective and less cytotoxic anti-HIV-1 agents.

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Documento generato il 01/12/20 alle ore 10:36:26