Department of Pharmacology, Emory University, Atlanta, Georgia (C.-m.L., B.-s.L., E.T.M.); and Department of Pharmaceutics, University of Washington, Seattle, Washington (S.L.A., N.I.).
J Pharmacol Exp Ther. 2014 Jan;348(1):141-52. doi: 10.1124/jpet.113.209841. Epub 2013 Oct 21.
CYP2C22 was recently described as a retinoic acid-metabolizing cytochrome P450 enzyme whose transcription is induced by all-trans-retinoic acid (atRA) in hepatoma cells (Qian L, Zolfaghari R, and Ross AC (2010) J Lipid Res 51:1781-1792). We identified CYP2C22 as a putative nitric oxide (NO)-regulated protein in a proteomic screen and raised specific polyclonal antibodies to CYP2C22 to study its protein expression. We found that CYP2C22 is a liver-specific protein that was not significantly induced by activators of the pregnane X receptor, constitutive androstane receptor, or peroxisome proliferator-activated receptor-α, but was downregulated to <25% of control by the aryl hydrocarbon receptor agonist β-naphthoflavone in cultured rat hepatocytes. CYP2C22 protein and its mRNA both were induced by atRA in hepatocytes, with EC50 of 100-300 nM, whereas the maximal extent of mRNA induction was twice that of the protein. CYP2C22 protein, but not its mRNA, was rapidly downregulated in hepatocytes by interleukin-1 (IL-1) or NO-donating compounds, and the downregulation by IL-1 was blocked by inhibition of NO synthases. The NO donor (Z)-1-[N-(3-aminopropyl)-N-(3-ammoniopropyl)amino]diazen-1-ium-1,2-diolate reduced the half-life of CYP2C22 from 8.7 to 3.4 hours in the presence of cycloheximide, demonstrating that NO-dependent downregulation is due to stimulated proteolysis. No intermediate degradation products were detected. However, this degradation was insensitive to inhibitors of calpains or the canonical proteasomal or lysosomal pathways, indicating that NO-dependent degradation of CYP2C22 proceeds via a novel pathway.
CYP2C22 最近被描述为一种视黄酸代谢细胞色素 P450 酶,其转录在肝癌细胞中被全反式视黄酸(atRA)诱导(Qian L、Zolfaghari R 和 Ross AC(2010)J Lipid Res 51:1781-1792)。我们在蛋白质组学筛选中鉴定 CYP2C22 为一种潜在的一氧化氮(NO)调节蛋白,并制备了特异性 CYP2C22 多克隆抗体来研究其蛋白表达。我们发现 CYP2C22 是一种肝脏特异性蛋白,不受孕烷 X 受体、组成型雄烷受体或过氧化物酶体增殖物激活受体-α的激活剂显著诱导,但在培养的大鼠肝细胞中,芳基烃受体激动剂β-萘黄酮将其下调至对照的 <25%。CYP2C22 蛋白及其 mRNA 均在肝细胞中被 atRA 诱导,EC50 为 100-300 nM,而 mRNA 诱导的最大程度是蛋白的两倍。CYP2C22 蛋白,而不是其 mRNA,在肝细胞中被白细胞介素-1(IL-1)或一氧化氮供体化合物迅速下调,IL-1 的下调被一氧化氮合酶抑制剂阻断。一氧化氮供体(Z)-1-[N-(3-氨基丙基)-N-(3-氨丙基)氨基]二氮烯-1,2-二醇在存在环己酰亚胺的情况下将 CYP2C22 的半衰期从 8.7 小时缩短至 3.4 小时,表明一氧化氮依赖性下调是由于刺激的蛋白水解。未检测到中间降解产物。然而,这种降解对钙蛋白酶或经典的蛋白酶体或溶酶体途径的抑制剂不敏感,表明一氧化氮依赖性 CYP2C22 降解通过一种新途径进行。