Amity Institute of Virology and Immunology, Sector-125, Amity University, Noida, 201313, Uttar Pradesh, India.
University Clinic of Cologne, Clinic of Nuclear Medicine, Cologne, Germany.
Org Biomol Chem. 2021 Nov 25;19(45):9849-9854. doi: 10.1039/d1ob01812d.
In this work, we describe the synthesis, stability, and preliminary biological evaluation of [Lu]Lu-DOTA-p160 peptide-based radiopharmaceuticals. Our findings highlight that all DOTA-p160-peptide radioconjugates exhibit favorable proteolytic and enzymatic stability with a prolonged half-life in human plasma and serum. Cell uptake studies carried out on MCF-7 cell line revealed saturable binding of the radioconjugates in the nanomolar range, thereby demonstrating their promising potential in the imaging and therapy of breast tumors.
在这项工作中,我们描述了 [Lu]Lu-DOTA-p160 肽类放射性药物的合成、稳定性和初步的生物学评价。我们的研究结果表明,所有的 DOTA-p160-肽放射性缀合物都表现出良好的蛋白水解和酶稳定性,在人血浆和血清中的半衰期延长。在 MCF-7 细胞系上进行的细胞摄取研究表明,放射性缀合物在纳摩尔范围内具有可饱和的结合,从而证明了它们在乳腺癌的成像和治疗方面具有广阔的应用前景。