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RET inhibition: Implications in cancer therapy

机译：RET抑制：在癌症治疗中的意义

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Introduction: The RET gene encodes a receptor tyrosine kinase essential for ontogenesis of the enteric nervous system and kidney. Following identification of RET, it was found that somatic rearrangements of this gene, conventionally designated as RET/PTC, are frequently present in papillary thyroid carcinoma. Subsequently, activating germ line point mutations of RET were identified as being responsible for the hereditary medullary thyroid carcinoma syndromes MEN2A, MEN2B and FMTC. RET rearrangements have recently been identified in a small fraction of lung adenocarcinomas.Area covered: The authors review the current field concerning the RET gene and protein, its involvement in cancer and the preclinical and clinical studies which highlight its role as a potentially important therapeutic target for several cancers.Expert opinion: Many multitargeted inhibitors which crossreact with RET have been developed and investigated in clinical trials targeting many cancer indications. In particular, VEGFR/PDGFR inhibitors, widely explored as antiangiogenics, have been intensively studied in thyroid carcinoma patients. Notwithstanding the efficacy observed with such agents, their common clinical activity in thyroid carcinoma is of short duration and includes frequent and severe side effects, limiting their therapeutic action. These findings are discussed and the need for improved, more specific RET-targeting drugs is highlighted.
机译：简介：RET基因编码一个受体酪氨酸激酶，对肠神经系统和肾脏的本体发育至关重要。鉴定出RET后，发现该基因的体细胞重排通常称为RET / PTC，经常出现在甲状腺乳头状癌中。随后，RET的激活种系点突变被确定为遗传性甲状腺髓样癌综合征MEN2A，MEN2B和FMTC。最近在一小部分肺腺癌中发现了RET重排。研究领域包括：作者回顾了有关RET基因和蛋白质，其在癌症中的参与以及临床前和临床研究的当前领域，这些研究突显了其作为潜在重要治疗靶点的作用专家意见：已经开发出许多与RET交叉反应的多靶点抑制剂，并已在针对许多癌症适应症的临床试验中进行了研究。特别地，已经广泛研究了作为抗血管生成剂的VEGFR / PDGFR抑制剂，已在甲状腺癌患者中进行了深入研究。尽管用这些试剂观察到了功效，但是它们在甲状腺癌中的常见临床活性持续时间短并且包括频繁和严重的副作用，从而限制了它们的治疗作用。讨论了这些发现，并强调了对改良的，更具体的RET靶向药物的需求。

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