放射性核素标记胃泌素及其类似物在肿瘤显像和治疗中的研究进展

胃泌素是一种脑肠肽,在中枢神经系统中可以作为神经递质,在外周组织中尤其是胃肠道可以看作是激素。胃泌素的功能是通过与细胞胆囊收缩素-B/胃泌素受体相互作用实现的。在核医学靶向诊断和治疗中已将胆囊收缩素-B/胃泌素受体作为靶组织来研究。胆囊收缩素-B/胃泌素受体可以在甲状腺髓样癌、小细胞肺癌、卵巢癌和胃肠内分泌肿瘤等胃泌素受体阳性的肿瘤中过度表达。放射性核素标记的胃泌素可以与多种肿瘤组织的胃泌素受体特异性地结合,可诊断和治疗胃泌素受体阳性肿瘤。本文对胃泌素及类似物在肿瘤的显像和治疗的应用进行了综述。

Development of Gastrin Related Radiopharmaceuticals for Cancer Imaging and Therapy

Gastrin is a kind of braingut peptide and present in both central nervous system（CNS） where it plays the roles of neurotransmitter or neuromodulator and in some peripheral tissues,mainly in gastrointestinal tract,where it may be considered as a hormone.Some researches revealed that most of the effects of gastrin were results from the specific interaction with cell Cholecystokinin-B（CCK-B,formerly CCK-B）/gastrin receptors.CCK-B/gastrin receptors have recently found increasing interest as targets for nuclear medicine applications.A high incidence of CCK-B receptors has been found in human samples of medullary thyroid cancer（MTC）,small cell lung cancer（SCLC）,stromal ovarian cancers,and also in vivo in gastrointestinal neuroendocrine tumors.Radiolabeled gastrin analogues have high specific affinity to receptor in Cholecystokinin-B/gastrin receptors positive tumor.This article reviews about gastrin and its analogues for cancer imaging and therapy.