Dataset Information

Synthesis and Evaluation of ⁶⁸Ga- and ¹⁷⁷Lu-Labeled [diF-Pro¹⁴]Bombesin(6-14) Analogs for Detection and Radioligand Therapy of Gastrin-Releasing Peptide Receptor-Expressing Cancer.

ABSTRACT: Background/Objectives: Overexpressed in various solid tumors, the gastrin-releasing peptide receptor (GRPR) is a promising target for cancer diagnosis and therapy. However, the high pancreas uptake of the current clinically evaluated GRPR-targeted radiopharmaceuticals limits their applications. In this study, we replaced the Pro¹⁴ residue in our previously reported GRPR-targeted LW02056 and ProBOMB5 with 4,4-difluoroproline (diF-Pro) to obtain an agonist LW02060 (DOTA-Pip-[D-Phe⁶,Tle¹⁰,NMe-His¹²,diF-Pro¹⁴]Bombesin(6-14)) and an antagonist LW02080 (DOTA-Pip-[D-Phe⁶,NMe-Gly¹¹,Leu¹³(ψ)diF-Pro¹⁴]Bombesin(6-14)), respectively. Methods/Results: The binding affinities (K_i) o

SUBMITTER: Wang L

PROVIDER: S-EPMC11859184 | biostudies-literature | 2025 Feb

REPOSITORIES: biostudies-literature

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Dataset Information

Synthesis and Evaluation of ⁶⁸Ga- and ¹⁷⁷Lu-Labeled [diF-Pro¹⁴]Bombesin(6-14) Analogs for Detection and Radioligand Therapy of Gastrin-Releasing Peptide Receptor-Expressing Cancer.

OmicsDI is part of the ELIXIR infrastructure

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Dataset Information

Synthesis and Evaluation of 68Ga- and 177Lu-Labeled [diF-Pro14]Bombesin(6-14) Analogs for Detection and Radioligand Therapy of Gastrin-Releasing Peptide Receptor-Expressing Cancer.

OmicsDI is part of the ELIXIR infrastructure

Tweets

Synthesis and Evaluation of ⁶⁸Ga- and ¹⁷⁷Lu-Labeled [diF-Pro¹⁴]Bombesin(6-14) Analogs for Detection and Radioligand Therapy of Gastrin-Releasing Peptide Receptor-Expressing Cancer.