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Cholecystokinin and gastrin receptors targeting in gastrointestinal cancer

机译:靶向胃肠道癌的胆囊收缩素和胃泌素受体

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摘要

Cholecystokinin and Gastrin are amongst the first gastrointestinal hormone discovered. In addition to classical actions (contraction of gallbladder, growth and secretion in the stomach and pancreas), these also act as growth stimulants for gastrointestinal malignancies and cell lines. Growth of these tumours is inhibited by antagonists of the cholecystokinin and gastrin receptors. These receptors provides most promising approach in clinical oncology and several specific radiolabelled ligands have been synthesized for specific tumour targeting and therapy of tumours overexpressing these receptors. Therefore, definition of the molecular structure of the receptor involved in the autocrine/paracrine loop may contribute to novel therapies for gastrointestinal cancer. Hence, this review tries to focus on the role and distribution of these hormones and their receptors in gastrointestinal cancer with a brief talk about the clinical trial using available agonist and antagonist in gastrointestinal cancers.
机译:胆囊收缩素和胃泌素是最早发现的胃肠激素之一。除了经典作用(胆囊收缩,胃和胰腺的生长和分泌)外,这些还可以作为胃肠道恶性肿瘤和细胞系的生长刺激剂。胆囊收缩素和胃泌素受体的拮抗剂抑制了这些肿瘤的生长。这些受体在临床肿瘤学中提供了最有前途的方法,并且已经合成了几种特定的放射性标记的配体用于特异性肿瘤靶向和过表达这些受体的肿瘤的治疗。因此,参与自分泌/旁分泌环的受体的分子结构的定义可能有助于胃肠道癌的新疗法。因此,本文简要讨论了这些激素及其受体在胃肠道癌中的作用和分布,并简要介绍了在胃肠道癌中使用可用激动剂和拮抗剂的临床试验。

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