Guo Man, Qu Xiangping, Qin Xiao-Qun
Department of Physiology, Xiangya School of Medicine, Central South University, Changsha, Hunan, P.R. China.
Curr Opin Endocrinol Diabetes Obes. 2015 Feb;22(1):3-8. doi: 10.1097/MED.0000000000000126.
To highlight the research progress of roles of bombesin-like peptides and their receptors in pharmacology and physiology.
Several new bombesin-derived radioactive or nonradioactive compounds were designed for the diagnosis and therapy of tumors that are overexpressing bombesin receptors. Both gastrin-releasing peptide receptor and neuromedin B receptor activation were shown to induce membrane depolarization and excite neurons in brain. Bombesin receptor subtype-3 was found to be downregulated in the muscle cells and myocytes from obese and type 2 diabetes patients, and its relevant cell signaling events in glucose homeostasis were also investigated. The molecular events triggered by bombesin receptors activation in different types of malignancies is being explored recently and new clues were provided for a better understanding of the biological roles of abnormal expression of bombesin receptors in tumors. Novel cross-talk between gastrin-releasing peptide receptor cell signaling and Sonic hedgehog pathways was identified in small-cell lung carcinoma.
Increasing evidence shows bombesin-like peptides and their receptors play important roles in both physiological state and diseases. More specific and safe tumor targeting Bombesin derivatives are being developed for tumor diagnosis and therapy.
强调蛙皮素样肽及其受体在药理学和生理学中的作用的研究进展。
设计了几种新的蛙皮素衍生的放射性或非放射性化合物，用于诊断和治疗过表达蛙皮素受体的肿瘤。胃泌素释放肽受体和神经介素B受体的激活均显示可诱导膜去极化并兴奋脑中的神经元。发现蛙皮素受体亚型3在肥胖和2型糖尿病患者的肌肉细胞和心肌细胞中下调，并对其在葡萄糖稳态中的相关细胞信号事件进行了研究。最近正在探索蛙皮素受体激活在不同类型恶性肿瘤中引发的分子事件，并为更好地理解蛙皮素受体异常表达在肿瘤中的生物学作用提供了新线索。在小细胞肺癌中发现了胃泌素释放肽受体细胞信号与音猬因子信号通路之间的新型相互作用。
越来越多的证据表明，蛙皮素样肽及其受体在生理状态和疾病中均起重要作用。正在开发更具特异性和安全性的靶向肿瘤的蛙皮素衍生物用于肿瘤诊断和治疗。
