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Click-Chemistry (CuAAC) Trimerization of an αv β6 Integrin Targeting Ga-68-Peptide: Enhanced Contrast for in-Vivo PET Imaging of Human Lung Adenocarcinoma Xenografts.


ABSTRACT: αv β6 Integrin is an epithelial transmembrane protein that recognizes latency-associated peptide (LAP) and primarily activates transforming growth factor beta (TGF-β). It is overexpressed in carcinomas (most notably, pancreatic) and other conditions associated with αv β6 integrin-dependent TGF-β dysregulation, such as fibrosis. We have designed a trimeric Ga-68-labeled TRAP conjugate of the αv β6 -specific cyclic pentapeptide SDM17 (cyclo[RGD-Chg-E]-CONH2 ) to enhance αv β6 integrin affinity as well as target-specific in-vivo uptake. Ga-68-TRAP(SDM17)3 showed a 28-fold higher αv β6 affinity than the corresponding monomer Ga-68-NOTA-SDM17 (IC50 of 0.

SUBMITTER: Quigley NG 

PROVIDER: S-EPMC7586803 | biostudies-literature | 2020 Oct

REPOSITORIES: biostudies-literature