Novel nastorazepide-based radioligands demonstrate effective cholecystokinin-2 receptor targeting with potential for theranostic applications
Lennart Bohrmann, Doroteja Novak, Marko Kroselj, Raghuvir H. Gaonkar, Francesca Porto, Melpomeni Fani, Petra Kolenc, Marko Anderluh, Rosalba Mansi · 2026
Read Novel nastorazepide-based radioligands demonstrate effective cholecystokinin-2 receptor targeting with potential for theranostic applications by Lennart Bohrmann, Doroteja Novak, Marko Kroselj, Raghuvir H. Gaonkar, Francesca Porto, Melpomeni Fani, Petra Kolenc, Marko Anderluh, Rosalba Mansi (2026) in the Tower of Babel, a free online library of public-domain works preserved in clean, searchable text. No sign-up. The full text is served as a plain-text file at a predictable URL, where text is present: https://antarctic-labs.com/tower-of-babel/PMC13549144.txt.
Description
Lennart Bohrmann and colleagues turn a known gut hormone blocker into radioactive tracers for tumors carrying its receptor, in a 2026 radiopharmaceutical study. Tumors such as medullary thyroid cancer display the cholecystokinin-2 receptor, and earlier tracers based on hormone mimics had drawbacks. The team built four new ligands on the antagonist drug nastorazepide, varying the linker and the metal-gripping chelator, and labeled them with two radioactive metals.
The new tracers latched onto receptor sites three to four times better than a reference tracer, with strong binding strength. One lead compound entered receptor-bearing cells at twice the rate of its siblings and, in mice, piled into tumors quickly with favorable tumor-to-organ ratios and high stability in the body. A first therapy test showed no significant tumor kill, so the authors frame the lead as a promising scaffold needing optimization.
Catalog record
| CREATOR | Lennart Bohrmann, Doroteja Novak, Marko Kroselj, Raghuvir H. Gaonkar, Francesca Porto, Melpomeni Fani, Petra Kolenc, Marko Anderluh, Rosalba Mansi |
|---|---|
| YEAR | 2026 |
| COLLECTION | PAPERS |
| FORMAT | TXT |
| FILE SIZE | 40 KB |
| LICENSE | https://creativecommons.org/licenses/by/4.0 |
| RIGHTS | CC BY |
| SOURCE | Europe PMC |