| Project/Area Number |
05671832
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| Research Category |
Grant-in-Aid for General Scientific Research (C)
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| Allocation Type | Single-year Grants |
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| Research Field |
Biological pharmacy
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| Research Institution | Kumamoto University |
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Principal Investigator |
SHOJI Shozo Kumamoto Univ., Pharmaceutical Sciences, Researcher, 薬学部, 教授 (60040317)
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| Co-Investigator(Kenkyū-buntansha) |
HATTORI Toshio Kyoto Univ., Virus Insutitute, Associate Professor, ウイルス研, 助教授 (30172935)
FURUISHI Kazuchika Kumamoto Univ., Pharmaceutical Sciences, Professor, 薬学部, 助手 (40238663)
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| Project Period (FY) |
1993 – 1994
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| Project Status |
Completed (Fiscal Year 1994)
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| Budget Amount *help |
¥2,100,000 (Direct Cost: ¥2,100,000)
Fiscal Year 1994: ¥1,000,000 (Direct Cost: ¥1,000,000)
Fiscal Year 1993: ¥1,100,000 (Direct Cost: ¥1,100,000)
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| Keywords | AIDS / HIV-1 / HIV-1 RT / AZT / Virus / transcriptase / LAV |
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| Research Abstract |
Attempts to overcome HIV-1 infection have been made on the basis of the points of attack of the HIV-1 life cycle. HIV-1 reverse transcriptase (RT) plays a central role in the HOV-1 life cycle, copying the genetic information in the genomic RNA into a double-stranded DNA form.
Azidothymidine (AZT), an inhibitor of HIV-RT,is being used to treat AIDS.As in vitro and in vivo HIV-1 resistance to a number of RT inhibitors has been reported, RT inhibitors are shown to be no longer chemotherapy for AIDS.
A kind of diketopiperazine derivatives is found to be a good or pure substrate, which is not a HIV-1 RT inhibitor, for HIV-1 RT in vitro. These results suggest that the diketopiperazine derivative is metabolically converted to a mimic nucleotide derivative in cell, transcripted to HIV-1 cDNA,and incorporated into host DNA.
The mechanism of the anti-HIV action with the derivative is not understood so far, however, the new compound may be very important for AIDS chemotherapy.
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