- 作者: Peter K. Chiang; Peter P. McCann; James R. Lane; Marvin C. Pankaskie; Donald S. Burke; Douglas L. Mayers
- 作者服務機構: a Division of Retrovirology,Walter Reed Army Institute of Research,Washington, D.C., ; b British Biotech Inc., Annapolis, Md., c SRA Technologies, Rockville, Md., d University of Nebraska Medical Center,Omaha, Nebr., USA
- 中文摘要: --
- 英文摘要: Four inhibitors of polyamine biosynthetic pathways were tested for their effect on HIV-1 replication in phytohemagglutinin-stimulated human peripheral blood mononuclear cells. Methyl acetylenic putrescine (MAP) and a-mono-fluoromethyldehydroornithine methyl ester, irreversible inhibitors of ornithine decarboxylase, inhibited the production of p24 antigen in phytohemagglutinin-stimulated peripheral blood mononuclear cells by clinical HIV-1 strains isolated from HIV-infected patients with IC50 values of about 1-2 μM 5'-{(Z)-4-amino-2-butenyl]methylamino}-5'-deoxyadenosine (MDL 73811), an enzyme-activated irreversible inhibitor of S-adenosyl-L-methionine (AdoMet) decarboxylase, also inhibited the production of p24 antigen by HIV-1 strains in peripheral blood mononuclear cells with IC50 values of 1-2 μM The least potent was 1-aminoxyethylamine which is another inhibitor of AdoMet decarboxylase. MAP showed the best therapeutic index of 500-1,000.
- 中文關鍵字: --
- 英文關鍵字: HIV-1 ; Polyamines ; Inhibitors ; p24; S-adenosylmethionine