Fei Bei, Yu Shuai, Geahlen Robert L
Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN 47907, USA.
Biochim Biophys Acta. 2013 Oct;1833(10):2153-64. doi: 10.1016/j.bbamcr.2013.05.010. Epub 2013 May 16.
Syk is a 72kDa non-receptor tyrosine kinase that is best characterized in hematopoietic cells. While Syk is pro-tumorigenic in some cancer cell types, it also has been reported as a negative regulator of metastatic cell growth in others. An examination of the RelA (p65) subunit of NF-κB expressed in MCF7 breast cancer cells indicated that either treatment with pervanadate or stable expression of Syk protected RelA from calpain-mediated proteolysis. Similar results were observed with the tyrosine phosphatase, PTP1B, another sensitive calpain substrate. The activity of calpain in MCF7 cell lysates was inhibited by both treatment with hydrogen peroxide and expression of Syk, the former due to oxidative inactivation of calpain and the latter to enhanced expression of calpastatin (CAST), the endogenous calpain inhibitor. The level of CAST was elevated in the cytosolic fraction of Syk-positive breast cancer cells resulting in more CAST present in complex with calpain in cell lysates. The high levels of CAST coincided with elevated basal levels of calcium-and of intracellular calpain activity-in Syk-expressing cells resulting from decreased levels of Bcl-2, an inhibitor of IP3-receptor-mediated calcium release. The inhibition of cellular calpain stimulated the Syk-mediated enhancement of NF-κB induced by TNF-α, enhanced tyrosine phosphorylation resulting from integrin crosslinking, and increased the localization of Syk to the plasma membrane.
Syk是一种72kDa的非受体酪氨酸激酶,在造血细胞中表现最为显著。虽然Syk在某些癌细胞类型中具有促肿瘤作用,但也有报道称它在其他细胞中是转移细胞生长的负调节因子。对MCF7乳腺癌细胞中表达的NF-κB的RelA(p65)亚基进行检测表明,用过氧钒酸盐处理或Syk的稳定表达均可保护RelA免受钙蛋白酶介导的蛋白水解作用。酪氨酸磷酸酶PTP1B(另一种敏感的钙蛋白酶底物)也观察到了类似结果。用过氧化氢处理和Syk的表达均能抑制MCF7细胞裂解物中钙蛋白酶的活性,前者是由于钙蛋白酶的氧化失活,后者是由于内源性钙蛋白酶抑制剂钙蛋白酶抑制蛋白(CAST)的表达增强。在Syk阳性乳腺癌细胞的胞质部分中,CAST水平升高,导致细胞裂解物中与钙蛋白酶结合的CAST增多。高水平的CAST与Syk表达细胞中钙和细胞内钙蛋白酶活性的基础水平升高相一致,这是由于IP3受体介导的钙释放抑制剂Bcl-2水平降低所致。细胞钙蛋白酶的抑制刺激了Syk介导的由TNF-α诱导的NF-κB增强、整合素交联导致的酪氨酸磷酸化增强,并增加了Syk在质膜上的定位。