Peretinoin (NIK333) 是一种具有维生素 A 样结构的口服无环类维生素 A，可靶向类维生素 A 核受体，如类维生素 X 受体 (RXR) 和视黄酸受体 (RAR)。
Peretinoin is an oral acyclic retinoid, inhibits HCV RNA amplification and virus release by altering lipid metabolism.Target: HCVin vitro: Peretinoin is an acyclic retinoid, improves the hepatic gene signature of chronic hepatitis C following curative therapy of hepatocellular carcinoma. Peretinoin is an oral acyclic retinoid with a vitamin A-like structure that targets retinoid nuclear receptors, such as retinoid X receptor and retinoic acid receptor. Peretinoin inhibits HCV RNA amplification and virus release by altering lipid metabolism. Peretinoin suppresses the RNA replication of H77S.3/GLuc2A most efficiently and its EC50 was 9 μM. Peretinoin may reduce the recurrence of hepatocellular carcinoma (HCC) following surgical ablation of primary tumours. Peretinoin inhibits RNA replication for all genotypes and showed the strongest antiviral effect among the retinoids tested. in vivo: In addition, Peretinoin prevents the development of hepatoma in several different hepatoma models.
[1]. Honda M, et al. Peretinoin, an acyclic retinoid, improves the hepatic gene signature of chronic hepatitis C following curative therapy of hepatocellular carcinoma. BMC Cancer. 2013 Apr 15;13:191. [2]. Shimakami T, et al. The acyclic retinoid Peretinoin inhibits hepatitis C virus replication and infectious virus release in vitro. Sci Rep. 2014 Apr 15;4:4688. doi: 10.1038/srep04688.
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