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- W2017121385 abstract "Selective high-affinity ligands (SHALs) were synthesized as molecular targeting agents for HLA-DR10, a cell surface receptor upregulated on malignant B-cell lymphocytes in non-Hodgkin's lymphoma and leukemia. SHALs are designed to mimic the affinity and selectivity of Lym-1, an antibody that binds to the β-subunit of HLA-DR10. To bind selectively to HLA-DR10, SHALs were constructed to bind to two adjacent pockets on the surface of the β-subunit of HLA-DR10 located within an epitope recognized by the Lym-1 antibody. A series of multivalent SHALs with molecular masses of 1500−3000 Da were synthesized using solid/polymer-supported synthesis on chlorotrityl chloride resin in 50−80% yield. To enable their use as radionuclide carriers in mouse studies, SHALs were conjugated to DOTA in a solution-phase reaction with 70−100% yield. 57Co/CoCl2 titrations revealed that 50−60% of the DOTA in the DOTA-conjugated SHALs was available for radiometal chelation. These DOTA−SHALs were labeled with 111In and used to carry out pharmacokinetic studies in mice. Radiolabeling reactions of DOTA−SHALs, with exactly one DOTA entity per targeting SHAL molecule, yielded products with greater than 90% radiochemical purity and specific activities ranging from 97 to 150 μCi/μg." @default.
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- W2017121385 date "2007-03-21" @default.
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- W2017121385 title "Synthesis and Radiolabeling of Selective High-Affinity Ligands Designed to Target Non-Hodgkin's Lymphoma and Leukemia" @default.
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- W2017121385 doi "https://doi.org/10.1021/bc060305o" @default.
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