1. Academic Validation
  2. Synthesis of the biotinylated anti-HIV compound BMMP and the target identification study

Synthesis of the biotinylated anti-HIV compound BMMP and the target identification study

  • Bioorg Med Chem Lett. 2016 Jan 1;26(1):43-5. doi: 10.1016/j.bmcl.2015.11.036.
Masahiro Kamo 1 Hiroshi Tateishi 2 Ryoko Koga 3 Yoshinari Okamoto 4 Masami Otsuka 5 Mikako Fujita 6
Affiliations

Affiliations

  • 1 Department of Bioorganic Medicinal Chemistry, Faculty of Life Sciences, Kumamoto University, 5-1 Oe-honmachi, Chuo-ku, Kumamoto 862-0973, Japan. Electronic address: 141y1023@st.kumamoto-u.ac.jp.
  • 2 Department of Bioorganic Medicinal Chemistry, Faculty of Life Sciences, Kumamoto University, 5-1 Oe-honmachi, Chuo-ku, Kumamoto 862-0973, Japan. Electronic address: 155y2008@st.kumamoto-u.ac.jp.
  • 3 Department of Bioorganic Medicinal Chemistry, Faculty of Life Sciences, Kumamoto University, 5-1 Oe-honmachi, Chuo-ku, Kumamoto 862-0973, Japan. Electronic address: kk1205@kumamoto-u.ac.jp.
  • 4 Department of Bioorganic Medicinal Chemistry, Faculty of Life Sciences, Kumamoto University, 5-1 Oe-honmachi, Chuo-ku, Kumamoto 862-0973, Japan. Electronic address: okamoto@gpo.kumamoto-u.ac.jp.
  • 5 Department of Bioorganic Medicinal Chemistry, Faculty of Life Sciences, Kumamoto University, 5-1 Oe-honmachi, Chuo-ku, Kumamoto 862-0973, Japan. Electronic address: motsuka@gpo.kumamoto-u.ac.jp.
  • 6 Research Institute for Drug Discovery, School of Pharmacy, Kumamoto University, 5-1 Oe-honmachi, Chuo-ku, Kumamoto 862-0973, Japan. Electronic address: mfujita@kumamoto-u.ac.jp.
Abstract

BMMP [2-(benzothiazol-2-ylmethylthio)-4-methylpyrimidine], an inhibitor of HIV-1 replication, was linked to biotin to study the interaction with the presumed target, HIV-1 Pr55(Gag) or CA, by means of surface plasmon resonance. The synthesized Biotin-BMMP inhibited HIV-1 replication to a similar extent as BMMP alone, but did not interact with Pr55(Gag) or CA, suggesting that BMMP exerts its activity by a different mechanism.

Keywords

BMMP; Biotin; CA; HIV-1; Pr55(Gag).

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