Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 21, Issue 7, Pages 2079-2087Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2013.01.016
Keywords
Anti-HIV agents; PD 404182; Photoaffinity labeling; Pyrimidobenzothiazine
Funding
- MEXT
- Health and Labor Science Research Grants (Research on HIV/AIDS, Japan)
- JSPS
- Grants-in-Aid for Scientific Research [10J01895, 24791021, 23390025] Funding Source: KAKEN
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To investigate the mechanism of action of the potent antiviral compound PD 404182, three novel photo-affinity probes equipped with a biotin or alkyne indicator were designed and synthesized based on previous structure-activity relationship studies. These probes retained the potent anti-HIV activity of the original pyrimidobenzothiazine derivatives. In photoaffinity labeling studies using HIV-1-infected H9 cells (H9IIIB), eight potential proteins were observed to bind PD 404182. (C) 2013 Elsevier Ltd. All rights reserved.
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