Journal
BIOSCIENCE BIOTECHNOLOGY AND BIOCHEMISTRY
Volume 76, Issue 6, Pages 1055-1067Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1271/bbb.120072
Keywords
CD1d; glycosphingolipid; KRN7000; natural killer T-cell; T-cell receptor
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Funding
- Mizutani Foundation for Glycoscience
- Ministry of Education, Culture, Sports, Science and Technology (MEXT) of Japan
- Japan Society for Bioscience, Biotechnology, and Agrochemistry
- Grants-in-Aid for Scientific Research [23790148] Funding Source: KAKEN
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KRN7000, an anticancer drug candidate developed by Kirin Brewery Co. in 1995, is an alpha-galactosyl ceramide. It is a ligand making a complex with CD1d protein, and it stimulates invariant natural killer T (NKT) cells, which are one of the lineages of immunocytes. NKT cells activated by recognition of the CD1d/KRN7000 complex with its invariant T-cell receptor (TCR) can induce both protective and regulatory immune responses. To determine the recognition and activation mechanisms of NKT cells and to develop drug candidates more effective than KRN7000, a large number of analogs of KRN7000 have been synthesized. Some of them show potent bioactivities and have the potential of being utilized as therapeutic agents. In this review, structure-activity relationship studies of novel glycolipids which stimulate NKT cells efficiently are summarized.
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