Publications by authors named "P N Kanellopoulos"
Background: Gastrin releasing peptide receptor (GRPR)-directed radiopharmaceuticals for targeted radionuclide therapy may be a very promising addition in prostate and breast cancer patient management. Aiming to provide a GRPR-targeting theranostic pair, we have utilized the Tc-99m/Re-188 radiometal pair, in combination with two bombesin based antagonists, maSSS-PEG2-RM26 and maSES-PEG2-RM26. The two main aims of the current study were (i) to elucidate the influence of the radiometal-exchange on the biodistribution profile of the two peptides and (ii) to evaluate the feasibility of using the [Tc]Tc labeled counterparts for the dosimetry estimation for the [Re]Re-labeled conjugates.
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- Recent studies on growth differentiation factor 15 (GDF-15) and interleukin-6 (IL-6) in inflammatory bowel diseases (IBD) are limited, prompting this assessment of their serum levels in patients with Crohn's disease (CD) and ulcerative colitis (UC).
- The study involved 122 CD patients, 71 UC patients, and 44 healthy controls, revealing that elevated GDF-15 and IL-6 levels in active CD were significantly associated with various patient characteristics, including CRP levels and hospitalization rates.
- In UC, while both GDF-15 and IL-6 were higher in active patients compared to controls, only IL-6 showed consistent associations with disease activity,
The concept of radiotheranostics relies on the overexpression of a biomolecular target on malignant cells to direct diagnostic/therapeutic radionuclide-carriers specifically to cancer lesions. The concomitant expression of more than one target in pathological lesions may be elegantly exploited to improve diagnostic sensitivity and therapeutic efficacy. Toward this goal, we explored a first example of a combined application of [Tc]Tc-DT11 (DT11, N-Lys(MPBA-PEG4)-Arg-Arg-Pro-Tyr-Ile-Leu-OH; NTSR-specific) and [Tc]Tc-DB7(DB7, N-PEG2-DPhe-Gln-Trp-Ala-Val-Gly-His-Leu-NHEt; GRPR-specific) in prostate cancer models.
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- Targeting the gastrin-releasing peptide receptor (GRPR) using the peptide RM26 has shown promise in imaging for prostate cancer, but its quick clearance from the body limits its effectiveness as a therapeutic agent.
- To prolong the peptide's half-life, researchers have experimented with an albumin-binding domain (ABD) to create a new series of ABD-RM26 conjugates aimed at improving the stability and reducing kidney uptake.
- The second-generation construct ABD-RM26 Gen 2A demonstrated significantly lower kidney uptake—almost 6 times less—improving biodistribution, but it had reduced effectiveness in binding to GRPR, indicating potential for further development in targeted cancer therapy.
Two Novel [Ga]Ga-Labeled Radiotracers Based on Metabolically Stable [Sar]RM26 Antagonistic Peptide for Diagnostic Positron Emission Tomography Imaging of GRPR-Positive Prostate Cancer.
ACS Omega
April 2024
Gastrin releasing peptide receptor (GRPR) is overexpressed in prostate cancer (PC-3) and can be used for diagnostic purposes. We herein present the design and preclinical evaluation of two novel NOTA/NODAGA-containing peptides suitable for labeling with the positron emission tomography (PET) radionuclide Ga-68. These analogs are based on the previously reported GRPR-antagonist DOTAGA-PEG2-[Sar]RM26, developed for targeted radiotheraostic applications.
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