Relevance of coexpression of somatostatin and dopamine D2 receptors in pituitary adenomas
Relevance of coexpression of somatostatin and dopamine D2 receptors in pituitary adenomas
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DOI：
10.1016/j.mce.2007.12.008
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发表时间：
2008-05-14
影响因子：
4.1
通讯作者：
Barher, A.
中科院分区：
文献类型：
--
作者：
Aveanu, A. S.;Jaquet, P.;Barher, A.
多巴胺和生长抑素均参与正常垂体细胞的负控制。多巴胺亚型 2 受体 (D2DR) 和生长抑素受体 (sst) 激动剂（主要针对 sst2）用于治疗垂体腺瘤。然而，大多数促肾上腺皮质激素细胞和促性腺激素细胞腺瘤以及三分之一的生长激素细胞腺瘤仍然不能通过这些治疗得到充分控制。 D2DR 和 sst1、2、3 和 5 存在于大多数垂体腺瘤中。这些受体可能通过异二聚化相互作用，如 sst1-sst5、sst5-D2DR、sst2-sst3 和 sst2-D2DR 所示，表明可能存在相加效应。 D2DR 和 sst2 激动剂联合治疗对肢端肥大症中 GH 分泌的加和作用有限。此外，具有sst2、D2DR和sst5亲和力的新型嵌合化合物已显示出对细胞培养物中不同类型垂体腺瘤的分泌和/或增殖的控制增强。与最近开发的多sst配体药物一起，这些多巴胺-生长抑素配体代表了垂体腺瘤联合治疗的新机会。 (C) 2007 Elsevier Ireland Ltd. 保留所有权利。
Dopamine and somatostatin are both involved in the negative control of normal pituitary cells. Dopamine subtype 2 receptor (D2DR) and somatostatin receptor (sst) agonists, mainly directed to sst2, are used in the treatment of pituitary adenomas. Nevertheless, a majority of corticotroph and gonadotroph adenomas and a third of somatotroph adenomas are still not sufficiently controlled by these treatments. D2DR and sst1, 2, 3 and 5 are present in most pituitary adenomas. These receptors may interact by heterodimerization as shown for sst1-sst5, sst5-D2DR, sst2-sst3 and sst2-D2DR suggesting possible additive effects. D2DR and sst2 agonist cotreatment showed limited additivity on GH secretion in acromegaly. Moreover, new chimeric compounds with sst2, D2DR and sst5 affinity have shown an increased control of secretion and/or proliferation of different types of pituitary adenomas in cell culture. Together with the multi-sst ligand drugs recently developed, these dopamine-somatostatin ligands represent a new opportunity in the combinatory treatment of pituitary adenomas. (C) 2007 Elsevier Ireland Ltd. All rights reserved.