CART (cocaine- and amphetamine-regulated transcript) peptides are involved in food intake regulation, stress and other physiological functions. Although CART peptides have been known for over 25 years, their receptor(s) have not yet been characterized. In this short review, we will summarize our previous studies, where we reported specific binding of 125 I-CART(61-102) to PC12 rat pheochromocytoma cells. Competitive binding experiments performed with mono- and di-iodinated peptides and their isoforms with oxidized Met67 resulted in nanomolar binding affinity. Moreover, in our previous study, CART(61-102), as well as di-iodinated CART(61-102), have shown a strong anorexigenic effect in fasted lean mice after intracerebroventricular administration. In conclusion, from our previous studies, iodination of CART(61-102) resulted in mono- and di-iodinated analogs with or without oxidized Met67 . All analogs revealed a high affinity to binding sites at PC12 cells and preserved biological activity.

中文翻译：

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CART（61-102）肽的碘化：保留小鼠的结合和厌食活性

CART（可卡因和安非他明调节的转录物）肽参与食物摄入调节、压力和其他生理功能。尽管 CART 肽已为人所知超过 25 年，但它们的受体尚未被表征。在这篇简短的回顾中，我们将总结我们之前的研究，其中我们报告了 125 I-CART(61-102) 与 PC12 大鼠嗜铬细胞瘤细胞的特异性结合。使用单碘化和二碘化肽及其同种型与氧化的 Met67 进行的竞争性结合实验产生了纳摩尔结合亲和力。此外，在我们之前的研究中，CART(61-102) 以及二碘化 CART(61-102) 在脑室内给药后对禁食的瘦小鼠表现出强烈的厌食作用。总之，根据我们之前的研究，CART(61-102) 的碘化导致单碘化和二碘化类似物有或没有氧化的 Met67。所有类似物都显示出对 PC12 细胞结合位点的高亲和力并保留了生物活性。