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A New, Second Generation Trithiol Bifunctional Chelate for 72,77As: Trithiol(b)-(Ser)2-RM2
Bioconjugate Chemistry ( IF 4.0 ) Pub Date : 2021-01-10 , DOI: 10.1021/acs.bioconjchem.0c00658
Firouzeh Najafi Khosroshahi , Yutian Feng , Li Ma , Simon Manring , Tammy L Rold 1 , Fabio A Gallazzi , Steven P Kelley , Mary F Embree , Heather M Hennkens , Timothy J Hoffman 1 , Silvia S Jurisson
Affiliation  

Trithiol chelates are suitable for labeling radioarsenic (72As: 2.49 MeV β+, 26 h; 77As: 0.683 MeV β, 38.8 h) to form potential theranostic radiopharmaceuticals for positron emission tomography (PET) imaging and therapy. A trithiol(b)-(Ser)2-RM2 bioconjugate and its arsenic complex were synthesized and characterized. The trithiol(b)-(Ser)2-RM2 bioconjugate was radiolabeled with no-carrier-added 77As in over 95% radiochemical yield and was stable for over 48 h, and in vitro IC50 cell binding studies of [77As]As-trithiol(b)-(Ser)2-RM2 in PC-3 cells demonstrated high affinity for the gastrin-releasing peptide (GRP) receptor (low nanomolar range). Limited biodistribution studies in normal mice were performed with HPLC purified 77As-trithiol(b)-(Ser)2-RM2 demonstrating both pancreatic uptake and hepatobiliary clearance.

中文翻译:


72,77As 的新型第二代三硫醇双功能螯合物:三硫醇(b)-(Ser)2-RM2



三硫醇螯合物适合标记放射性砷( 72 As:2.49 MeV β + ,26 h; 77 As:0.683 MeV β ,38.8 h),形成用于正电子发射断层扫描(PET)成像和治疗的潜在治疗诊断放射性药物。合成并表征了三硫醇(b)-(Ser) 2 -RM2生物缀合物及其砷配合物。三硫醇(b)-(Ser) 2 -RM2 生物缀合物用未添加载体的77 As 进行放射性标记,放射化学产率超过 95%,并且稳定超过 48 小时,并且 [ 77 As] 的体外IC 50细胞结合研究PC-3 细胞中的 As-三硫醇(b)-(Ser) 2 -RM2 表现出对胃泌素释放肽 (GRP) 受体的高亲和力(低纳摩尔范围)。使用 HPLC 纯化的77 As-三硫醇(b)-(Ser) 2 -RM2 在正常小鼠中进行了有限的生物分布研究,证明了胰腺摄取和肝胆清除。
更新日期:2021-01-10
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