AI Article Synopsis
- α-Galactosylceramide (α-GalCer) interacts with CD1d proteins to stimulate immune responses, but repeated injections can lead to immune suppression, limiting its anti-cancer use.
- To address this issue, researchers created photochromic azobenzene-based analogues to control exposure and enhance binding to CD1d.
- FACS analyses showed that some analogues increased binding affinity to CD1d by about 20% upon photo-irradiation, while simulations indicated that a bulkier photochromic structure may improve the toggle between active and inactive states.
Article Abstract
α-Galactosylceramide (α-GalCer) is recognized by the CD1d proteins on antigen-presenting cells at the ceramide moiety and the galactose moiety is presented to iNKT cells, which stimulates the immune responses. However, the immune suppression by repeated injections of α-GalCer has discouraged its development as an anti-cancer agent. To overcome the shortcoming by spatiotemporal restriction of its exposure, we synthesized the photochromic azobenzene-incorporated analogues and tested the photo-immunoregulation effect in its binding to CD1d. FACS analyses indicated that some of these analogues enhanced the affinity to CD1d on photo-irradiation by about 20%. A docking simulation suggests that the photochromic molecule should be bulkier for a clearer discrimination between on and off states.
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| http://dx.doi.org/10.1016/j.bmcl.2020.126960 | DOI Listing |
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Photo effect on the CD1d-binding ability of azobenzene-attached analogues of α-GalCer.
Bioorg Med Chem Lett
March 2020
School of Life Science and Technology, Tokyo Institute of Technology, 4259 J2-10 Nagatsuta-cho, Midori-ku, Yokohama, Kanagawa 226-8501, Japan. Electronic address:
Article Synopsis
- α-Galactosylceramide (α-GalCer) interacts with CD1d proteins to stimulate immune responses, but repeated injections can lead to immune suppression, limiting its anti-cancer use.
- To address this issue, researchers created photochromic azobenzene-based analogues to control exposure and enhance binding to CD1d.
- FACS analyses showed that some analogues increased binding affinity to CD1d by about 20% upon photo-irradiation, while simulations indicated that a bulkier photochromic structure may improve the toggle between active and inactive states.
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