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Synthesis and Preclinical Evaluation of Novel ⁶⁸Ga-Labeled (R)-Pyrrolidin-2-yl-boronic Acid-Based PET Tracers for Fibroblast Activation Protein-Targeted Cancer Imaging.

ABSTRACT: Fibroblast activation protein (FAP) is a membrane-tethered serine protease overexpressed in the reactive stromal fibroblasts of >90% human carcinomas, which makes it a promising target for developing radiopharmaceuticals for the imaging and therapy of carcinomas. Here, we synthesized two novel (R)-pyrrolidin-2-yl-boronic acid-based FAP-targeted ligands: SB02055 (DOTA-conjugated (R)-(1-((6-(3-(piperazin-1-yl)propoxy)quinoline-4-carbonyl)glycyl)pyrrolidin-2-yl)boronic acid) and SB04028 (DOTA-conjugated ((R)-1-((6-(3-(piperazin-1-yl)propoxy)quinoline-4-carbonyl)-D-alanyl)pyrrolidin-2-yl)boronic acid). ^natGa- and ⁶⁸Ga-complexes of both ligands were evaluated in preclinical studies and compared to previously reported ^natGa/⁶⁸Ga-co

SUBMITTER: Bendre S

PROVIDER: S-EPMC10303363 | biostudies-literature | 2023 May

REPOSITORIES: biostudies-literature

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Dataset Information

Synthesis and Preclinical Evaluation of Novel ⁶⁸Ga-Labeled (R)-Pyrrolidin-2-yl-boronic Acid-Based PET Tracers for Fibroblast Activation Protein-Targeted Cancer Imaging.

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Dataset Information

Synthesis and Preclinical Evaluation of Novel 68Ga-Labeled (R)-Pyrrolidin-2-yl-boronic Acid-Based PET Tracers for Fibroblast Activation Protein-Targeted Cancer Imaging.

OmicsDI is part of the ELIXIR infrastructure

Tweets

Synthesis and Preclinical Evaluation of Novel ⁶⁸Ga-Labeled (R)-Pyrrolidin-2-yl-boronic Acid-Based PET Tracers for Fibroblast Activation Protein-Targeted Cancer Imaging.