Department of Hematology, Amgen Inc, Thousand Oaks, CA, USA.
Blood. 2010 May 27;115(21):4264-72. doi: 10.1182/blood-2009-10-248666. Epub 2010 Feb 2.
Erythropoiesis stimulating agents (ESAs) have been reported to activate erythropoietin receptors (EpoR) on cell types, including endothelial, neuronal, renal tubule, and cardiac cells. ESAs have also been reported to promote angiogenesis. However, those findings are controversial and confounded by methodologic issues. We show that EpoR mRNA was detected in essentially all cell types examined, including primary human endothelial, renal, cardiac, and neuronal cells but 10- to 100-fold lower than Epo-responsive cells using quantitative reverse-transcribed polymerase chain reaction. Total endothelial EpoR protein examined using a new monoclonal antibody was low to undetectable. Surface EpoR on endothelial cells was not detected using [(125)I]-rHuEpo surface-binding studies. There was no evidence of ESA-induced intracellular signaling in endothelial cells. There was a similar lack of EpoR expression and signaling in other cell types examined. Experiments were performed examining ESA function on these cells. An in vivo rat corneal angiogenesis assay demonstrated neo-vessel formation in response to recombinant human vascular endothelial growth factor (rHuVEGF). However, recombinant mouse Epo did not induce vessel formation. Similarly, ESAs did not reproducibly provide cytoprotection to neuronal, renal, or cardiac cells. Taken together, our data challenge the notion of presence or function of EpoR on nonhematopoietic cells, and call into question the preclinical basis for clinical studies exploring direct, "pleiotropic" actions of ESAs.
促红细胞生成素刺激剂(ESAs)已被报道能激活细胞类型上的促红细胞生成素受体(EpoR),包括内皮细胞、神经元、肾小管和心肌细胞。ESA 也被报道能促进血管生成。然而,这些发现存在争议,并且受到方法学问题的困扰。我们表明,EpoR mRNA 存在于几乎所有检查的细胞类型中,包括原代人内皮细胞、肾细胞、心肌细胞和神经元细胞,但使用定量逆转录聚合酶链反应时,其水平比促红细胞生成素反应性细胞低 10-100 倍。使用新的单克隆抗体检查的总内皮 EpoR 蛋白水平较低或无法检测到。通过[(125)I]-rHuEpo 表面结合研究,未检测到内皮细胞上的 EpoR。在内皮细胞中没有发现 ESA 诱导的细胞内信号。在其他检查的细胞类型中也没有发现 EpoR 表达和信号。进行了检查这些细胞上 ESA 功能的实验。体内大鼠角膜血管生成试验表明,重组人血管内皮生长因子(rHuVEGF)能引起新血管形成。然而,重组鼠 Epo 不能诱导血管形成。同样,ESA 也不能重复为神经元、肾或心肌细胞提供细胞保护。综上所述,我们的数据对非造血细胞上存在或发挥功能的 EpoR 提出质疑,并对探索 ESA 的直接、“多效性”作用的临床前研究基础提出质疑。
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