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  • Hasnowo, Lutfi A.Tomsk Polytech Univ, Sch Nucl Sci & Engn, Tomsk 634050, Russia.;Natl Res & Innovat Agcy, Polytech Inst Nucl Technol, Yogyakarta 55281, Indonesia. (author)

Synthesis, I-123-Radiolabeling Optimization, and Initial Preclinical Evaluation of Novel Urea-Based PSMA Inhibitors with a Tributylstannyl Prosthetic Group in Their Structures

  • Article/chapterEnglish2023

Publisher, publication year, extent ...

  • MDPI,2023
  • electronicrdacarrier

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  • LIBRIS-ID:oai:DiVA.org:uu-510103
  • https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-510103URI
  • https://doi.org/10.3390/ijms241512206DOI

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  • Language:English
  • Summary in:English

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  • Subject category:ref swepub-contenttype
  • Subject category:art swepub-publicationtype

Notes

  • Prostate-specific membrane antigen (PSMA) has been identified as a target for the development of theranostic agents. In our current work, we describe the design and synthesis of novel N-[N-[(S)-1,3-dicarboxypropyl]carbamoyl]-(S)-L-lysine (DCL) urea-based PSMA inhibitors with a chlorine-substituted aromatic fragment at the lysine & epsilon;-nitrogen atom, a dipeptide including two phenylalanine residues in the L-configuration as the peptide fragment of the linker, and 3- or 4-(tributylstannyl)benzoic acid as a prosthetic group in their structures for radiolabeling. The standard compounds [I-127]PSMA-m-IB and [I-127]PSMA-p-IB for comparative and characterization studies were first synthesized using two alternative synthetic approaches. An important advantage of the alternative synthetic approach, in which the prosthetic group (NHS-activated esters of compounds) is first conjugated with the polypeptide sequence followed by replacement of the Sn(Bu)(3) group with radioiodine, is that the radionuclide is introduced in the final step of synthesis, thereby minimizing operating time with iodine-123 during the radiolabeling process. The obtained DCL urea-based PSMA inhibitors were radiolabeled with iodine-123. The radiolabeling optimization results showed that the radiochemical yield of [I-123]PSMA-p-IB was higher than that of [I-123]PSMA-m-IB, which were 74.9 & PLUSMN; 1.0% and 49.4 & PLUSMN; 1.2%, respectively. The radiochemical purity of [I-123]PSMA-p-IB after purification was greater than 99.50%. The initial preclinical evaluation of [I-123]PSMA-p-IB demonstrated a considerable affinity and specific binding to PC-3 PIP (PSMA-expressing cells) in vitro. The in vivo biodistribution of this new radioligand [I-123]PSMA-p-IB showed less accumulation than [Lu-177]Lu-PSMA-617 in several normal organs (liver, kidney, and bone). These results warrant further preclinical development, including toxicology evaluation and experiments in tumor-bearing mice.

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  • Larkina, Maria S.Tomsk Polytech Univ, Res Sch Chem & Appl Biomed Sci, Res Ctr Oncotheranost, Tomsk 634050, Russia.;Siberian State Med Univ, Dept Pharmaceut Anal, Tomsk 634050, Russia. (author)
  • Plotnikov, EvgeniiTomsk Polytech Univ, Res Sch Chem & Appl Biomed Sci, Res Ctr Oncotheranost, Tomsk 634050, Russia.;Russian Acad Sci, Mental Hlth Reseach Inst, Tomsk Natl Res Med Ctr, Tomsk 634014, Russia. (author)
  • Bodenko, VitalinaTomsk Polytech Univ, Res Sch Chem & Appl Biomed Sci, Res Ctr Oncotheranost, Tomsk 634050, Russia.;Siberian State Med Univ, Dept Pharmaceut Anal, Tomsk 634050, Russia. (author)
  • Yuldasheva, FeruzaTomsk Polytech Univ, Res Sch Chem & Appl Biomed Sci, Res Ctr Oncotheranost, Tomsk 634050, Russia. (author)
  • Stasyuk, ElenaTomsk Polytech Univ, Sch Nucl Sci & Engn, Tomsk 634050, Russia. (author)
  • Petrov, Stanislav A.Moscow MV Lomonosov State Univ, Dept Chem, Leninskie Gory 1-3, Moscow 119991, Russia. (author)
  • Zyk, Nikolai Y.Moscow MV Lomonosov State Univ, Dept Chem, Leninskie Gory 1-3, Moscow 119991, Russia. (author)
  • Machulkin, Aleksei E.Moscow MV Lomonosov State Univ, Dept Chem, Leninskie Gory 1-3, Moscow 119991, Russia. (author)
  • Vorozhtsov, Nikolai I.Moscow MV Lomonosov State Univ, Dept Chem, Leninskie Gory 1-3, Moscow 119991, Russia. (author)
  • Beloglazkina, Elena K.Moscow MV Lomonosov State Univ, Dept Chem, Leninskie Gory 1-3, Moscow 119991, Russia. (author)
  • Nenajdenko, Valentine G.Moscow MV Lomonosov State Univ, Dept Chem, Leninskie Gory 1-3, Moscow 119991, Russia. (author)
  • Tolmachev, VladimirUppsala universitet,Cancerprecisionsmedicin(Swepub:uu)vladtolm (author)
  • Orlova, Anna,1960-Uppsala universitet,Theranostics(Swepub:uu)annaorlo (author)
  • Majouga, Alexander G.Dmitry Mendeleev Univ Chem Technol Russia, Fac Chem, Miusskaya sq 9, Moscow 125047, Russia. (author)
  • Yusubov, Mekhman S.Tomsk Polytech Univ, Res Sch Chem & Appl Biomed Sci, Res Ctr Oncotheranost, Tomsk 634050, Russia. (author)
  • Tomsk Polytech Univ, Sch Nucl Sci & Engn, Tomsk 634050, Russia.;Natl Res & Innovat Agcy, Polytech Inst Nucl Technol, Yogyakarta 55281, Indonesia.Tomsk Polytech Univ, Res Sch Chem & Appl Biomed Sci, Res Ctr Oncotheranost, Tomsk 634050, Russia.;Siberian State Med Univ, Dept Pharmaceut Anal, Tomsk 634050, Russia. (creator_code:org_t)

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  • In:International Journal of Molecular Sciences: MDPI24:151661-65961422-0067

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