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

Van Hai Nguyen; Haruhisa Kikuchi; Yuzuru Kubohara; Katsunori Takahashi; Yasuhiro Katou; Yoshiteru Oshima

doi:10.1016/j.bmc.2015.06.027

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

Van Hai Nguyen, Haruhisa Kikuchi, Yuzuru Kubohara, Katsunori Takahashi, Yasuhiro Katou, Yoshiteru Oshima

Research output: Contribution to journal › Article › peer-review

5 Citations (Scopus)

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.

Original language	English
Pages (from-to)	4311-4315
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry
Volume	23
Issue number	15
DOIs	https://doi.org/10.1016/j.bmc.2015.06.027
Publication status	Published - 2015 Jul 23
Externally published	Yes

Keywords

Cellular slime mold
Drosophila
Immunosuppressor
Innate immunity
Structure-activity relationship

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/j.bmc.2015.06.027

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title = "Development of novel DIF-1 derivatives that selectively suppress innate immune responses",

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",

author = "Nguyen, {Van Hai} and Haruhisa Kikuchi and Yuzuru Kubohara and Katsunori Takahashi and Yasuhiro Katou and Yoshiteru Oshima",

note = "Funding Information: We thank Dr. J.L. Imler for att-luc reporter construct. This work was supported in part by Grant-in-Aid for Scientific Research (Nos. 23710247 , 24590110 and 25350959 ) from the Ministry of Education, Culture, Sports, Science, and Technology, Japan ; Drug Discovery, Informatics, and Structural Life Science from the Ministry of Education, Culture, Sports, Science, and Technology, Japan; Kobayashi International Scholarship Foundation ; the SUNBOR GRANT from the Suntory Institute for Bioorganic Research ; and the Astellas Foundation for Research on Metabolic Disorders . Publisher Copyright: {\textcopyright} 2015 Elsevier Ltd . All rights reserved.",

year = "2015",

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doi = "10.1016/j.bmc.2015.06.027",

language = "English",

volume = "23",

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AU - Nguyen, Van Hai

AU - Kikuchi, Haruhisa

AU - Kubohara, Yuzuru

AU - Takahashi, Katsunori

AU - Katou, Yasuhiro

AU - Oshima, Yoshiteru

N1 - Funding Information: We thank Dr. J.L. Imler for att-luc reporter construct. This work was supported in part by Grant-in-Aid for Scientific Research (Nos. 23710247 , 24590110 and 25350959 ) from the Ministry of Education, Culture, Sports, Science, and Technology, Japan ; Drug Discovery, Informatics, and Structural Life Science from the Ministry of Education, Culture, Sports, Science, and Technology, Japan; Kobayashi International Scholarship Foundation ; the SUNBOR GRANT from the Suntory Institute for Bioorganic Research ; and the Astellas Foundation for Research on Metabolic Disorders . Publisher Copyright: © 2015 Elsevier Ltd . All rights reserved.

PY - 2015/7/23

Y1 - 2015/7/23

N2 - 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.

AB - 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.

KW - Cellular slime mold

KW - Drosophila

KW - Immunosuppressor

KW - Innate immunity

KW - Structure-activity relationship

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JO - Bioorganic and Medicinal Chemistry

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

Abstract

Keywords

ASJC Scopus subject areas

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