摘要
5-hT1A受体是一种药理特征良好的5-羟色胺受体亚型,由于其参与了多种生理病理机制和治疗,长期以来一直被研究。神经性疾病如失语症和抑郁症。5-羟色胺(5-HT)还具有许多非神经功能,如原发性高血压、胚胎发生、卵泡成熟和行为。而且它对不同类型的非肿瘤细胞具有生长因子作用,并与癌基因有关。事实上,5-羟色胺在不同的人血清中的生长刺激活性。或者细胞已经被报道。最近,结合5-HT1A受体的新化学分子被认为是用于神经保护、认知障碍、帕金森症的新的治疗实体。疾病,疼痛治疗,恶性类癌综合征和癌症。广泛的研究表明,5-HT1A受体参与了肿瘤的发生和发展,并参与了多种肿瘤类型的研究,如:前列腺,膀胱,小细胞肺,直肠结肠镜和胆管癌。此外,根据肿瘤类型的不同,5-HT1A受体拮抗剂被证明能够阻断5-羟色胺(5-ht)诱导的促肾上腺皮质激素(Incre)。ASE在肿瘤生长中的作用。在这篇综述中,我们将注意力集中在涉及5-HT1A受体的每一种肿瘤类型上,研究了这种分子靶点的作用和不同类型的F化合物已经显示了调节它的能力。这些分析可以为医学化学家开发新的分子提供线索,因为选择性的5-ht1A试剂在fart中是有用的。她阐明了这个治疗靶子的作用。
关键词: 5-羟色胺、5-HT1A受体、癌变、人肿瘤类型、5-HT1A配体、抗增殖活性。
Current Medicinal Chemistry
Title:The Role of 5-HT1A Receptor in Cancer as a New Opportunity in Medicinal Chemistry
Volume: 25 Issue: 27
关键词: 5-羟色胺、5-HT1A受体、癌变、人肿瘤类型、5-HT1A配体、抗增殖活性。
摘要: The 5-HT1A receptor is a pharmacologically well characterized serotonin receptor subtype and it has long been investigated because of its involvement in several physiopathological mechanisms and treatment of neurological diseases like ansia and depression. Serotonin (5-HT) also shows many non-neural functions such as essential hypertension, embryogenesis, follicle maturation and behavior. Moreover, it exerts a growth factor function on different types of non-tumoral cells, and it was also found to be related to oncogenes. In fact, growth-stimulatory activity of serotonin in different human tumor cells has been reported. Recently, new chemical molecules binding the 5-HT1A receptor have been described as novel therapeutic entities useful in neuroprotection, cognitive impairment, Parkinson’s Disease, pain treatment, malignant carcinoid syndrome and cancer. It was widely demonstrated that 5-HT1A receptor is involved in the carcinogenesis and consequently in many human tumor types, such as prostate, bladder, small cell lung, colonrectal and cholangiocarcinoma. Furthermore, depending on the tumor type, 5-HT1A receptor antagonists were shown to be capable of blocking the 5HT-induced increase in tumor growth. In this review, we have focused our attention on each tumor type where the 5-HT1A receptor is involved, investigating the role of this molecular target and the different classes of compounds that have shown the capability to modulate it. The analyzed aspects could represent a hint for the medical chemists to develop novel molecules as selective 5-HT1A agents are useful in further elucidating the role of this therapeutic target.
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The Role of 5-HT1A Receptor in Cancer as a New Opportunity in Medicinal Chemistry, Current Medicinal Chemistry 2018; 25 (27) . https://dx.doi.org/10.2174/0929867325666180209141650
DOI https://dx.doi.org/10.2174/0929867325666180209141650 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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