文章：

垂体肿瘤的分子靶点

Molecular targets in pituitary tumours

原文发布日期：2004-04-01

DOI: 10.1038/nrc1320

类型: Review Article

开放获取: 否

要点：

1. Pituitary tumours are common and cause unrestrained hormone secretion or compression of intracranial structures. Treatment aims to suppress hormone hypersecretion, ablate tumours or prevent their growth without compromising endogenous pituitary function.
2. Hypothalamic and pituitary growth factors and their receptors regulate normal and abnormal pituitary-tumour hormone secretion and cell growth.
3. Pituitary tumours express various hormone receptors and retain inhibitory responses to agonistic and antagonistic ligands. Recent efforts have enabled the development of safe and potent anti-hormonal and anti-proliferative compounds aimed at specific pituitary-tumour-cell molecular targets and, potentially, other cancers.
4. First-generation dopamine-receptor agonists have been superceded by potent compounds with long-lasting effects and improved side-effect profiles. Treatment with somatostatin analogues is poised to broaden in application with the development of somatostatin-receptor subtype-specific and universal somatostatin analogues. Newer chimeric agonists that encompass dopaminergic actions as well as somatostatin-like actions are in development.
5. Peripheral growth-hormone-receptor antagonists (for example, pegvisomant) specifically block insulin-like growth factor 1 production. Retinoic-acid receptor and peroxisome-proliferator-activated receptor-γ also represent new approaches for treating pituitary tumours.

要点翻译：

1. 垂体瘤较为常见，可导致激素分泌失控或压迫颅内结构。治疗目标在于抑制激素过度分泌、消除肿瘤或阻止其生长，同时不影响正常垂体功能。
2. 下丘脑和垂体生长因子及其受体调控正常与异常的垂体肿瘤激素分泌及细胞生长。
3. 垂体瘤表达多种激素受体，并保留对激动剂和拮抗剂配体的抑制反应。近期研究促使安全有效的抗激素和抗增殖化合物得以开发，这些药物针对特定垂体肿瘤细胞分子靶点，并可能应用于其他癌症。
4. 第一代多巴胺受体激动剂已被长效强效、副作用更少的新型化合物取代。随着生长抑素受体亚型特异性及广谱生长抑素类似物的研发，生长抑素类似物的治疗应用范围正在扩大。兼具多巴胺能作用和生长抑素样作用的新型嵌合激动剂正在开发中。
5. 外周生长激素受体拮抗剂（如培维索孟）可特异性阻断胰岛素样生长因子1的产生。视黄酸受体和过氧化物酶体增殖物激活受体-γ也为垂体瘤治疗提供了新途径。

英文摘要：

Pituitary tumours are associated with unrestrained secretion and subsequent action of trophic hormones. One approach to therapy involves suppressing pituitary-hormone hypersecretion without compromising endogenous pituitary function. Identification of novel neuroendocrine-receptor targets has enabled the development of safe and effective receptor ligands that can be used to treat pituitary tumours and associated hormonal excess. Some of these agents, such as somatostatin analogues and a growth-hormone-receptor antagonist, will also have broader applications in treating other cancers and metabolic disorders.

摘要翻译： 

垂体瘤与促激素的过度分泌及其后续作用有关。一种治疗方法是在不损害内源性垂体功能的前提下，抑制垂体激素的过度分泌。新型神经内分泌受体的发现，推动了安全有效的受体配体的开发，这些配体可用于治疗垂体瘤及相关激素过量。其中一些药物，如生长抑素类似物和生长激素受体拮抗剂，还将在治疗其他癌症和代谢性疾病中具有更广泛的应用。

原文链接：

Molecular targets in pituitary tumours