Department of Pathobiology of the Nervous System, Center for Brain Research, Medical University of Vienna, 1090 Vienna, Austria.
Biomolecules. 2024 Feb 19;14(2):244. doi: 10.3390/biom14020244.
3-hydroxy-3-methylglutaryl-CoA reductase (HMG-CoA reductase, HMGCR) is one of the rate-limiting enzymes in the mevalonate pathway required for cholesterol biosynthesis. It is an integral membrane protein of the endoplasmic reticulum (ER) but has occasionally been described in peroxisomes. By co-immunofluorescence microscopy using different HMGCR antibodies, we present evidence for a dual localization of HMGCR in the ER and peroxisomes in differentiated human monocytic THP-1 cells, primary human monocyte-derived macrophages and human primary skin fibroblasts under conditions of low cholesterol and statin treatment. Using density gradient centrifugation and Western blot analysis, we observed a truncated HMGCR variant of 76 kDa in the peroxisomal fractions, while a full-length HMGCR of 96 kDa was contained in fractions of the ER. In contrast to primary human control fibroblasts, peroxisomal HMGCR was not found in fibroblasts from patients suffering from type-1 rhizomelic chondrodysplasia punctata, who lack functional PEX7 and, thus, cannot import peroxisomal matrix proteins harboring a type-2 peroxisomal targeting signal (PTS2). Moreover, in the N-terminal region of the soluble 76 kDa C-terminal catalytic domain, we identified a PTS2-like motif, which was functional in a reporter context. We propose that under sterol-depleted conditions, part of the soluble HMGCR domain, which is released from the ER by proteolytic processing for further turnover, remains sufficiently long in the cytosol for peroxisomal import via a PTS2/PEX7-dependent mechanism. Altogether, our findings describe a dual localization of HMGCR under combined lipid depletion and statin treatment, adding another puzzle piece to the complex regulation of HMGCR.
3-羟-3-甲基戊二酰辅酶 A 还原酶(HMG-CoA 还原酶,HMGCR)是胆固醇生物合成所需甲羟戊酸途径中的限速酶之一。它是内质网(ER)的整合膜蛋白,但偶尔也在过氧化物酶体中描述。通过使用不同的 HMGCR 抗体进行共免疫荧光显微镜检查,我们提供了证据表明在分化的人单核细胞 THP-1 细胞、原代人单核细胞衍生的巨噬细胞和人原代皮肤成纤维细胞中,HMGCR 存在于 ER 和过氧化物酶体中的双重定位在低胆固醇和他汀类药物治疗的条件下。通过密度梯度离心和 Western blot 分析,我们在过氧化物酶体部分观察到 76 kDa 的截断 HMGCR 变体,而全长 HMGCR 的 96 kDa 则包含在 ER 部分。与原发性人对照成纤维细胞不同,在患有 1 型 Rhizomelic 软骨发育不良性点状营养不良的患者的成纤维细胞中未发现过氧化物酶体 HMGCR,这些患者缺乏功能性 PEX7,因此不能导入含有 2 型过氧化物酶体靶向信号(PTS2)的过氧化物酶体基质蛋白。此外,在可溶性 76 kDa C 末端催化结构域的 N 末端区域,我们鉴定出一个 PTS2 样基序,该基序在报告基因背景中具有功能。我们提出,在甾醇耗竭条件下,部分可溶性 HMGCR 结构域通过蛋白水解处理从 ER 释放出来进行进一步周转,在细胞质中保持足够长的时间,通过 PTS2/PEX7 依赖性机制进入过氧化物酶体。总之,我们的研究结果描述了在联合脂质耗竭和他汀类药物治疗下 HMGCR 的双重定位,为 HMGCR 的复杂调控增添了另一个难题。