Exploratory studies on CA-15L,an anti-HIV active HIV-1 capsid fragment |
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| Institution: | 1. Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University (TMDU), 2-3-10 Kandasurugadai, Chiyoda-ku, Tokyo 101-0062, Japan;2. Graduate School of Medical and Dental Sciences, Tokyo Medical and Dental University (TMDU), 1-5-45 Yushima, Bunkyo-ku, Tokyo 113-8150, Japan;3. AIDS Research Center, National Institute of Infectious Diseases, 1-23-1 Toyama, Shinjuku-ku, Tokyo 162-8640, Japan;4. Yong Loo Lin School of Medicine, National University of Singapore, Singapore 117597, Singapore;3. National Center for Global Health and Medicine Research Institute, Tokyo 162-8655, Japan;4. Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, Tokyo, 101-0062, Japan;5. AIDS Clinical Center, National Center for Global Health and Medicine, Tokyo 162-8655, Japan;6. AIDS Research Centre, National Institute of Infectious Diseases, Tokyo 162-8640, Japan;12. Faculty of Pharmaceutical Sciences, Tohoku Medical and Pharmaceutical University, Sendai 981-8558, Japan;8. Experimental Retrovirology Section, HIV and AIDS Malignancy Branch, NCI, National Institutes of Health, Bethesda, Maryland 20892-1868;1. Center for Drug Design, College of Pharmacy, University of Minnesota, Minneapolis, MN, 55455, USA;2. Department of Molecular Microbiology and Immunology, University of Missouri School of Medicine, Christopher S. Bond Life Sciences Center, Columbia, MO, 65211, USA;3. Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA, 30322, USA;4. Clinical Research Center, Nagoya Medical Center, National Hospital Organization, Nagoya, Aichi, 460-0001, Japan;1. Center for Drug Design, College of Pharmacy, University of Minnesota, Minneapolis, MN, 55455, USA;2. Department of Molecular Microbiology and Immunology, University of Missouri School of Medicine, Christopher S. Bond Life Sciences Center, Columbia, MO, 65211, USA;3. Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA, 30322, USA;4. Clinical Research Center, Nagoya Medical Center, National Hospital Organization, Nagoya, Aichi, 460-0001, Japan;1. Nano Medical Engineering Laboratory, RIKEN Cluster for Pioneering Research, 2-1 Hirosawa, Wako, Saitama 3510198, Japan;2. Viral Infectious Diseases Unit, RIKEN, 2-1 Hirosawa, Wako, Saitama 3510198, Japan;3. Biotechnology Research Center, The University of Tokyo, Tokyo, Japan;4. Laboratory of Viral Infectious Diseases, Department of Medical Genome Sciences, Graduate School of Frontier Sciences, The University of Tokyo, Saitama, Japan;5. Laboratory of Viral Genomics, Pathogen Genomics Center, National Institute of Infectious Diseases, Tokyo, Japan;6. AIDS Research Center, National Institute of Infectious Diseases, Tokyo, Japan;7. Division of Infectious Diseases, International Institute of Disaster Science, and Tohoku Medical Megabank Organization, Tohoku University, Miyagi, Japan;8. Nihon University School of Medicine, Tokyo, Japan |
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| Abstract: | Utilizing overlapping fragment peptide libraries covering the whole sequence of an HIV-1 capsid (CA) protein with the addition of an octa-arginyl moiety, we had previously found several peptides with anti-HIV-1 activity. Herein, among these potent CA fragment peptides, CA-15L was examined because this peptide sequence overlaps with Helix 7, a helix region of the CA protein, which may be important for oligomerization of the CA proteins. A CA-15L surrogate with hydrophilic residues, and its derivatives, in which amino acid sequences are shifted toward the C-terminus by one or more residues, were synthesized and their anti-HIV activity was evaluated. In addition, its derivatives with substitution for the Ser149 residue were synthesized and their anti-HIV activity was evaluated because Ser149 might be phosphorylated in the step of degradation of CA protein oligomers. Several active compounds were found and might become new anti-HIV agents and new tools for elucidation of CA functions. |
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| Keywords: | Anti-HIV-1 activity Capsid protein Hydrophilic residue Octa-arginyl group |
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