Department of Chemistry, Purdue University, West Lafayette, Indiana, USA.
Institute for Drug Discovery, Purdue University, West Lafayette, Indiana, USA.
FASEB J. 2022 Jun;36(6):e22360. doi: 10.1096/fj.202100809RR.
Although both protein tyrosine phosphatases and kinases are constitutively active in healthy human red blood cells (RBCs), the preponderance of phosphatase activities maintains the membrane proteins in a predominantly unphosphorylated state. We report here that unlike healthy RBCs, proteins in sickle cells are heavily tyrosine phosphorylated, raising the question regarding the mechanism underpinning this tyrosine phosphorylation. Upon investigating possible causes, we observe that protein tyrosine phosphatase 1B (PTP1B), the major erythrocyte tyrosine phosphatase, is largely digested to a lower molecular weight fragment in sickle cells. We further find that the resulting truncated form of PTP1B is significantly less active than its intact counterpart, probably accounting for the intense tyrosine phosphorylation of Band 3 in sickle erythrocytes. Because this tyrosine phosphorylation of Band 3 promotes erythrocyte membrane weakening that causes release of both membrane vesicles and cell free hemoglobin that in turn initiates vaso-occlusive events, we conclude that cleavage of PTP1B could contribute to the symptoms of sickle cell disease. We further posit that methods to inhibit proteolysis of PTP1B could mitigate symptoms of the disease.
尽管蛋白酪氨酸磷酸酶和激酶在健康的人类红细胞(RBC)中都是持续激活的,但磷酸酶活性的优势使膜蛋白主要处于未磷酸化状态。我们在这里报告说,与健康的 RBC 不同,镰状细胞中的蛋白质被大量酪氨酸磷酸化,这就提出了一个问题,即这种酪氨酸磷酸化的机制是什么。在研究可能的原因时,我们观察到蛋白酪氨酸磷酸酶 1B(PTP1B),即主要的红细胞酪氨酸磷酸酶,在镰状细胞中被大量消化成较低分子量的片段。我们进一步发现,PTP1B 的这种截短形式的活性明显低于其完整形式,这可能是导致 Band 3 在镰状红细胞中强烈酪氨酸磷酸化的原因。由于 Band 3 的这种酪氨酸磷酸化促进了红细胞膜的弱化,导致膜囊泡和无细胞血红蛋白的释放,进而引发血管阻塞事件,因此我们得出结论,PTP1B 的裂解可能导致镰状细胞病的症状。我们进一步假设抑制 PTP1B 蛋白水解的方法可以减轻该疾病的症状。