摘要
肺癌在全球每年杀害大约130万名公民。酪氨酸激酶抑制剂(TKI)厄洛替尼和吉非替尼是有效的抗肿瘤药物尤其是肺癌 表皮生长因子受体基因突变的患者。目标是增加患野生型表皮生长因子受体肺癌患者的酪氨酸激酶抑制剂效力。G蛋白偶联受体(GPCR)反式激活野生型肺癌细胞中的表皮生长因子受体。G蛋白偶联受体可以由肽激动剂引起的磷脂酰肌醇代谢激活或受腺苷酰环化酶刺激。最近,非肽类拮抗剂被发现抑制由多肽引起的表皮生长因子受体的反式激活。蛙皮素非肽类拮抗剂(BB)、神经降压素(NTS)、胆囊收缩素(CCK)抑制肺癌的生长和提高吉非替尼毒性。结果表明,G蛋白偶联受体反式激活表皮生长因子受体可能在癌细胞的增殖发挥重要的作用。
关键词: 表皮生长因子受体,G蛋白偶联受体,肺癌,非肽受体拮抗剂,肽受体酪氨酸激酶受体激活。
图形摘要
Current Drug Targets
Title:EGFR Transactivation by Peptide G Protein-Coupled Receptors in Cancer
Volume: 17 Issue: 5
Author(s): Terry W. Moody, Bernardo Nuche-Berenguer, Taichi Nakamura and Robert T. Jensen
Affiliation:
关键词: 表皮生长因子受体,G蛋白偶联受体,肺癌,非肽受体拮抗剂,肽受体酪氨酸激酶受体激活。
摘要: Lung cancer kills approximately 1.3 million citizens in the world annually. The tyrosine kinase inhibitors (TKI) erlotinib and gefitinib are effective anti-tumor agents especially in lung cancer patients with epidermal growth factor receptor (EGFR) mutations. The goal is to increase the potency of TKI in lung cancer patients with wild type EGFR. G protein-coupled receptors (GPCR) transactivate the wild type EGFR in lung cancer cells. The GPCR can be activated by peptide agonists causing phosphatidylinositol turnover or stimulation of adenylylcyclase. Recently, nonpeptide antagonists were found to inhibit the EGFR transactivation caused by peptides. Nonpeptide antagonists for bombesin (BB), neurotensin (NTS) and cholecystokinin (CCK) inhibit lung cancer growth and increase the cytotoxicity of gefitinib. The results suggest that GPCR transactivation of the EGFR may play an important role in cancer cell proliferation.
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Cite this article as:
Terry W. Moody, Bernardo Nuche-Berenguer, Taichi Nakamura and Robert T. Jensen , EGFR Transactivation by Peptide G Protein-Coupled Receptors in Cancer, Current Drug Targets 2016; 17 (5) . https://dx.doi.org/10.2174/1389450116666150107153609
DOI https://dx.doi.org/10.2174/1389450116666150107153609 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
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