title: Design and synthesis of biotin- or alkyne-conjugated photoaffinity probes for studying the target molecules of PD 404182.
abstract: To investigate the mechanism of action of the potent antiviral compound PD 404182, three novel photoaffinity 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.
authors: Graduate School of Pharmaceutical Sciences, Kyoto University, Sakyo-ku, Kyoto 606-8501, Japan.
authors: Tsukasa
authors: T
authors: Mizuhara
authors: Shinya
authors: S
authors: Oishi
authors: Hiroaki
authors: H
authors: Ohno
authors: Kazuya
authors: K
authors: Shimura
authors: Masao
authors: M
authors: Matsuoka
authors: Nobutaka
authors: N
authors: Fujii
mesh_terms: D000480:Alkynes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D001710:Biotin / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D002460:Cell Line; D015658:HIV Infections / Q000188:drug therapy / Q000821:virology; D015497:HIV-1 / Q000187:drug effects* / Q000378:metabolism; D006801:Humans; D019920:Photoaffinity Labels / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D011485:Protein Binding; D014764:Viral Proteins / Q000378:metabolism*
chemical_list: D000480:Alkynes; D019380:Anti-HIV Agents; D019920:Photoaffinity Labels; D014764:Viral Proteins; D001710:Biotin