Side-Chain Modified [^99mTc]Tc-DT1 Mimics: A Comparative Study in NTS₁R-Positive Models.

ABSTRACT: Radiolabeled neurotensin analogs have been developed as candidates for theranostic use against neurotensin subtype 1 receptor (NTS₁R)-expressing cancer. However, their fast degradation by two major peptidases, neprilysin (NEP) and angiotensin-converting enzyme (ACE), has hitherto limited clinical success. We have recently shown that palmitoylation at the ε-amine of Lys⁷ in [^99mTc]Tc-[Lys⁷]DT1 (DT1, N₄-Gly-Arg-Arg-Pro-Tyr-Ile-Leu-OH, N₄ = 6-(carboxy)-1,4,8,11-tetraazaundecane) led to the fully stabilized [^99mTc]Tc-DT9 analog, displaying high uptake in human pancreatic cancer AsPC-1 xenografts but unfavorable pharmacokinetics in mice. Aiming to improve the in vivo stability of [^99mTc]Tc-DT1 without

SUBMITTER: Kanellopoulos P 

PROVIDER: S-EPMC10647616 | biostudies-literature | 2023 Oct

REPOSITORIES: biostudies-literature