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Can I read One Step Closer to Clinical Translation: Enhanced Tumor Targeting of [99mTc]Tc-DB4 and [111In]In-SG4 in Mice Treated with Entresto on EtoBox?
One Step Closer to Clinical Translation: Enhanced Tumor Targeting of [99mTc]Tc-DB4 and [111In]In-SG4 in Mice Treated with Entresto by Kanellopoulos, Panagiotis; Kaloudi, Aikaterini; Rouchota, Maritina; Loudos, George; de Jong, Marion; Krenning, Eric P.; Nock, Berthold A.; Maina, Theodosia is a Pharmacology, Toxicology and Pharmaceutics article available to read on EtoBox.
What is One Step Closer to Clinical Translation: Enhanced Tumor Targeting of [99mTc]Tc-DB4 and [111In]In-SG4 in Mice Treated with Entresto about?
Background: Peptide radioligands may serve as radionuclide carriers to tumor sites overexpressing their cognate receptor for diagnostic or therapeutic purposes. Treatment of mice with the neprilysin (NEP)-inhibitor phosphoramidon was previously shown to improve the metabolic stability and tumor uptake of biodegradable radiopeptides. Aiming to clinical translation of this methodology, we herein investigated the impact of the approved pill Entresto, releasing the potent NEP-inhibitor LBQ657 in vivo, on the stability and tumor uptake of two radiopeptides. Methods: The metabolic stability of [99mTc]Tc-DB4 (DB4, N4-Pro-Gln-Arg-Tyr-Gly-Asn-Gln-Trp-Ala-Val-Gly-His-Leu-Nle-NH2) and [111In]In-SG4 (SG4, DOTA-DGlu-Ala-Tyr-Gly-Trp-Nle-Asp-Phe-NH2) was tested in LBQ657/Entresto-treated mice vs. untreated controls. The uptake in gastrin-releasing peptide receptor (GRPR)-, or cholecystokinin subtype 2 receptor (CCK2R)-positive tumors respectively, was compared between LBQ657/Entresto-treated mice and untreated controls. Results: LBQ657/Entresto treatment induced marked stabilization of [99mTc] Tc-DB4 and [111In]In-SG4 in peripheral mice blood, resulting in equally enhanced tumor uptake at 4 h pos
Who reads One Step Closer to Clinical Translation: Enhanced Tumor Targeting of [99mTc]Tc-DB4 and [111In]In-SG4 in Mice Treated with Entresto?
It is typically read by researchers, students, and practitioners in Pharmacology, Toxicology and Pharmaceutics.
- Author
- Kanellopoulos, Panagiotis; Kaloudi, Aikaterini; Rouchota, Maritina; Loudos, George; de Jong, Marion; Krenning, Eric P.; Nock, Berthold A.; Maina, Theodosia
- Publisher
- MDPI AG; Multidisciplinary Digital Publishing Institute (MDPI); Basel: MDPI, 2009- (ISSN 1999-4923)
- Published
- 2020
- Language
- EN
- Field
- Pharmacology, Toxicology and Pharmaceutics (Life Sciences)