2. Academic Validation
  3. Development of novel DIF-1 derivatives that selectively suppress innate immune responses

Development of novel DIF-1 derivatives that selectively suppress innate immune responses

  • Bioorg Med Chem. 2015 Aug 1;23(15):4311-4315. doi: 10.1016/j.bmc.2015.06.027.
Van Hai Nguyen 1,  Haruhisa Kikuchi 2,  Yuzuru Kubohara 3,  Katsunori Takahashi 4,  Yasuhiro Katou 1,  Yoshiteru Oshima 1
Affiliations

Affiliations

  • 1 Graduate School of Pharmaceutical Sciences, Tohoku University, Aoba-yama, Aoba-ku, Sendai 980-8578, Japan.
  • 2 Graduate School of Pharmaceutical Sciences, Tohoku University, Aoba-yama, Aoba-ku, Sendai 980-8578, Japan. Electronic address: hal@mail.pharm.tohoku.ac.jp.
  • 3 Department of Molecular and Cellular Biology, Institute for Molecular and Cellular Regulation (IMCR), Gunma University, 3-39-15 Showa-machi, Maebashi, Gunma 371-8512, Japan; Graduate School of Health and Sports Science, Juntendo University, 1-1 Hiraga-gakuendai, Inzai, Chiba 270-1695, Japan.
  • 4 Department of Medical Technology, Faculty of Health Science, Gunma Paz College, Takasaki 370-0006, Japan.
PMID: 26122773 DOI: 10.1016/j.bmc.2015.06.027
Abstract

The multiple pharmacological activities of differentiation-inducing factor-1 (DIF-1) of the cellular slime mold Dictyostelium discoideum led us to examine the use of DIF-1 as a 'drug template' to develop promising seed compounds for drug discovery. DIF-1 and its derivatives were synthesized and evaluated for their regulatory activities in innate immune responses. We found two new derivatives (4d and 5e) with highly selective inhibitory activities against production of the antimicrobial peptide attacin in Drosophila S2 cells and against production of interleukin-2 in Jurkat cells.

Keywords

Cellular slime mold; Drosophila; Immunosuppressor; Innate immunity; Structure–activity relationship.

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