ArticleEJNMMI radiopharmacy and chemistry2025
Enhancing theranostic potential of anti-mesothelin sdAb through site-specific labeling at a unique conserved lysine by molecular engineering.
Article in EJNMMI radiopharmacy and chemistry, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.
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Who cites it
2 citing papers in PubMed.
- Comparative theranostic efficacy ofEuropean journal of nuclear medicine and molecular imaging · 2026Article
- Side by side comparison of NOTA and DOTA for conjugation efficiency, gallium-68 labeling, and in vivo biodistribution of anti-mesothelin sdAb A1-His.EJNMMI radiopharmacy and chemistry · 2025Article
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13 authors.
Funding
Abstract
backgroundMesothelin is a 40 kDa glycoprotein overexpressed in several cancers, including triple-negative breast cancer (TNBC). The anti-mesothelin single-domain antibody (sdAb, or nanobody) A1 can serve as a radio-theranostic agent, but random DOTA conjugation on lysines yields heterogeneous products.
resultsWe reengineered A1-His by directed mutagenesis to produce four single-lysine variants (A1K1-His, A1K2-His, A1K3-His, and A1K4-His). Each was site-specifically conjugated with p-SCN-Bn-DOTA, radiolabeled with
conclusionsFor the first time, site-specific DOTA conjugation using sdAb derivatives containing a single lysine was achieved, avoiding the production of mixed final compounds. These findings identify
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