REVIEW Tamibarotene is an orally-active, synthetic retinoid, developed to overcome all-trans retinoic acid resistance, with potential antineoplastic activity. It is a retinoic acid receptor (RAR) agonist with high specificity for RARalpha and RARbeta over RARgamma that induces differentiation and apoptosis of HL-60 cells in vitro. It exhibits antiproliferative effects against a variety of human tumor cells lines and displays anticancer activity against acute promyelocytic leukemia in vivo. Temporarily and spatially specific expression of RARs suggests their pivotal roles in the adult brain. It is considered to be a promising candidate drug for treatment of Alzheimer's disease because of its transcriptional controls of multiple target genes involved in etiology and pathology of Alzheimer's disease.
Eyrolles L; Kagechika H; Kawachi E; Fukasawa H; Iijima T; Matsushima Y; Hashimoto Y; Shudo K Retinobenzoic acids. 6. Retinoid antagonists with a heterocyclic ring Journal of medicinal chemistry (1994), 37(10), 1508-17.
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