Design and synthesis of biotin- or alkyne-conjugated photoaffinity probes for studying the target molecules of PD 404182
| Autor: | Kazuya Shimura, Masao Matsuoka, Hiroaki Ohno, Nobutaka Fujii, Tsukasa Mizuhara, Shinya Oishi |
|---|---|
| Rok vydání: | 2013 |
| Předmět: |
Anti-HIV Agents
Clinical Biochemistry Biotin Pharmaceutical Science Alkyne HIV Infections Photoaffinity Labels Conjugated system Biochemistry Cell Line Viral Proteins chemistry.chemical_compound Drug Discovery medicine Humans Molecule Molecular Biology chemistry.chemical_classification Photoaffinity labeling Organic Chemistry Combinatorial chemistry chemistry Mechanism of action Alkynes HIV-1 Molecular Medicine medicine.symptom Protein Binding |
| Zdroj: | Bioorganic & Medicinal Chemistry. 21:2079-2087 |
| ISSN: | 0968-0896 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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