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Preclinical Evaluat...
Preclinical Evaluation of a Novel High-Affinity Radioligand [99mTc]Tc-BQ0413 Targeting Prostate-Specific Membrane Antigen (PSMA)
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- Bezverkhniaia, Ekaterina (author)
- Uppsala universitet,Theranostics,Tomsk Polytech Univ, Res Sch Chem & Appl Biomed Sci, Res Centrum Oncotheranost, Tomsk 634009, Russia.;Siberian State Med Univ, Sci & Res Lab Chem & Pharmaceut Res, Tomsk 634050, Russia.
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- Kanellopoulos, Panagiotis (author)
- Uppsala universitet,Theranostics
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- Abouzayed, Ayman (author)
- Uppsala universitet,Theranostics
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- Larkina, Mariia (author)
- Tomsk Polytech Univ, Res Sch Chem & Appl Biomed Sci, Res Centrum Oncotheranost, Tomsk 634009, Russia.;Siberian State Med Univ, Sci & Res Lab Chem & Pharmaceut Res, Tomsk 634050, Russia.
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- Oroujeni, Maryam, PhD, 1982- (author)
- Uppsala universitet,Cancerprecisionsmedicin,Affibody AB, S-17165 Solna, Sweden.
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- Vorobyeva, Anzhelika (author)
- Uppsala universitet,Cancerprecisionsmedicin
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- Rosenström, Ulrika (author)
- Uppsala universitet,Preparativ läkemedelskemi,Theranostics
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- Tolmachev, Vladimir (author)
- Uppsala universitet,Cancerprecisionsmedicin
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- Orlova, Anna, 1960- (author)
- Uppsala universitet,Theranostics,Science for Life Laboratory, SciLifeLab
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(creator_code:org_t)
- MDPI, 2023
- 2023
- English.
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In: International Journal of Molecular Sciences. - : MDPI. - 1661-6596 .- 1422-0067. ; 24:24
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https://doi.org/10.3...
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Abstract
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- Radionuclide imaging using radiolabeled inhibitors of prostate-specific membrane antigen (PSMA) can be used for the staging of prostate cancer. Previously, we optimized the Glu-urea-Lys binding moiety using a linker structure containing 2-napththyl-L-alanine and L-tyrosine. We have now designed a molecule that contains mercaptoacetyl-triglutamate chelator for labeling with Tc-99m (designated as BQ0413). The purpose of this study was to evaluate the imaging properties of [Tc-99m]Tc-BQ0413. PSMA-transfected PC3-pip cells were used to evaluate the specificity and affinity of [Tc-99m]Tc-BQ0413 binding in vitro. PC3-pip tumor-bearing BALB/C nu/nu mice were used as an in vivo model. [Tc-99m]Tc-BQ0413 bound specifically to PC3-pip cells with an affinity of 33 +/- 15 pM. In tumor-bearing mice, the tumor uptake of [Tc-99m]Tc-BQ0413 (38 +/- 6 %IA/g in PC3-pip 3 h after the injection of 40 pmol) was dependent on PSMA expression (3 +/- 2 %IA/g and 0.9 +/- 0.3 %IA/g in PSMA-negative PC-3 and SKOV-3 tumors, respectively). We show that both unlabeled BQ0413 and the commonly used binder PSMA-11 enable the blocking of [Tc-99m]Tc-BQ0413 uptake in normal PSMA-expressing tissues without blocking the uptake in tumors. This resulted in an appreciable increase in tumor-to-organ ratios. At the same injected mass (5 nmol), the use of BQ0413 was more efficient in suppressing renal uptake than the use of PSMA-11. In conclusion, [Tc-99m]Tc-BQ0413 is a promising probe for the visualization of PSMA-positive lesions using single-photon emission computed tomography (SPECT).
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Klinisk medicin -- Cancer och onkologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Clinical Medicine -- Cancer and Oncology (hsv//eng)
- MEDICIN OCH HÄLSOVETENSKAP -- Klinisk medicin -- Radiologi och bildbehandling (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Clinical Medicine -- Radiology, Nuclear Medicine and Medical Imaging (hsv//eng)
Keyword
- prostate cancer
- prostate-specific membrane antigen
- PSMA
- technetium-99m
- BQ0413
- single-photon emission computed tomography
Publication and Content Type
- ref (subject category)
- art (subject category)
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Bezverkhniaia, E ...
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Kanellopoulos, P ...
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Abouzayed, Ayman
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Larkina, Mariia
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Oroujeni, Maryam ...
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Vorobyeva, Anzhe ...
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Rosenström, Ulri ...
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Tolmachev, Vladi ...
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Orlova, Anna, 19 ...
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