Abstract
Abstract Insulin-independent hypoglycemic agents have attracted attention, because type 2 diabetes mellitus is reported to be associated with an increased risk of cancer due to mitogenic effect of insulin. Insulin-independent antihyperglycemic effect can be obtained by LXR activation. LXR functions as heterodimers with retinoid X receptors (RXRs). RXRs also work with PPARs, which are known as targets for improvement of insulin resistance. Since LXR/RXR and PPAR/RXR can be activated by RXR agonists alone, and we are interested in RXR agonists for new hyperglycemia agents. However, well-known RXR agonists (RXR full-agonists) show significant weight gain and triglyceride elevation. Since these side effects are caused by excess activation of RXR, we hypothesized that RXR partial-agonists might be effective to decrease plasma glucose level without these problems. As a result, CBt-PMN, which has a benzotriazole structure, was discovered as an RXR partial-agonist, and significantly decreases plasma glucose level in type 2 diabetes model mice without the side effects described above. Citation Format: {Authors}. {Abstract title} [abstract]. In: Proceedings of the 103rd Annual Meeting of the American Association for Cancer Research; 2012 Mar 31-Apr 4; Chicago, IL. Philadelphia (PA): AACR; Cancer Res 2012;72(8 Suppl):Abstract nr 946. doi:1538-7445.AM2012-946
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