Significant reduction of activity retention in the kidneys via optimized linker sequences in radiohybrid-based minigastrin analogs

Autor: Nadine Holzleitner, Sebastian Fischer, Isabel Maniyankerikalam, Roswitha Beck, Constantin Lapa, Hans-Jürgen Wester, Thomas Günther

Publikováno v: EJNMMI Research, Vol 14, Iss 1, Pp 1-12 (2024)

Abstract Background We recently introduced radiohybrid (rh)-based minigastrin analogs e.g., DOTA-rhCCK-18 (DOTA-D-Dap(p-SiFA)-(D-γ-Glu)8-Ala-Tyr-Gly-Trp-Nle-Asp-Phe-NH2), that revealed substantially increased activity retention in the tumor. However

Externí odkaz: https://doaj.org/article/793c094f567543f6a4050d4c4b105f85

Investigation of the structure-activity relationship at the N-terminal part of minigastrin analogs

Autor: Nadine Holzleitner, Thomas Günther, Amira Daoud-Gadieh, Constantin Lapa, Hans-Jürgen Wester

Publikováno v: EJNMMI Research, Vol 13, Iss 1, Pp 1-8 (2023)

Abstract Background Over the last years, several strategies have been reported to improve the metabolic stability of minigastrin analogs. However, currently applied compounds still reveal limited in vitro and in vivo stability. We thus performed a gl

Externí odkaz: https://doaj.org/article/b2cf2f4f6b9c494c9c68d658fa804ed7

Preclinical evaluation of ²²⁵ Ac-labeled minigastrin analog DOTA-CCK-66 for Targeted Alpha Therapy.

Autor: Holzleitner N; Chair of Pharmaceutical Radiochemistry, Department of Chemistry, School of Natural Sciences, Technical University of Munich, Walther-Meissner-Str. 3, 85748, Garching, Germany. nadine.holzleitner@tum.de., Vilangattil M; Department of Molecular and Medical Pharmacology, Biomedical Cyclotron Facility, University of California Los Angeles, 780 Westwood Plaza, Los Angeles, CA, 90024, USA., Swaidan A; Department of Molecular and Medical Pharmacology, Biomedical Cyclotron Facility, University of California Los Angeles, 780 Westwood Plaza, Los Angeles, CA, 90024, USA., Garcia-Prada CD; Department of Molecular and Medical Pharmacology, Biomedical Cyclotron Facility, University of California Los Angeles, 780 Westwood Plaza, Los Angeles, CA, 90024, USA., Taddio MF; Department of Molecular and Medical Pharmacology, Biomedical Cyclotron Facility, University of California Los Angeles, 780 Westwood Plaza, Los Angeles, CA, 90024, USA., Jeanjean P; Department of Molecular and Medical Pharmacology, Biomedical Cyclotron Facility, University of California Los Angeles, 780 Westwood Plaza, Los Angeles, CA, 90024, USA., Mona CE; Department of Molecular and Medical Pharmacology, Biomedical Cyclotron Facility, University of California Los Angeles, 780 Westwood Plaza, Los Angeles, CA, 90024, USA., Lapa C; Nuclear Medicine, Faculty of Medicine, University of Augsburg, Augsburg, Germany., Casini A; Chair of Pharmaceutical Radiochemistry, Department of Chemistry, School of Natural Sciences, Technical University of Munich, Walther-Meissner-Str. 3, 85748, Garching, Germany.; Chair of Medicinal and Bioinorganic Chemistry, Department of Chemistry, School of Natural Sciences, Technical University of Munich, Garching, Germany., Günther T; Chair of Pharmaceutical Radiochemistry, Department of Chemistry, School of Natural Sciences, Technical University of Munich, Walther-Meissner-Str. 3, 85748, Garching, Germany.; Molecular Imaging Program at Stanford (MIPS), Department of Radiology, School of Medicine, Stanford University, Stanford, CA, USA., Carlucci G; Department of Molecular and Medical Pharmacology, Biomedical Cyclotron Facility, University of California Los Angeles, 780 Westwood Plaza, Los Angeles, CA, 90024, USA. GCarlucci@mednet.ucla.edu.

Publikováno v: European journal of nuclear medicine and molecular imaging [Eur J Nucl Med Mol Imaging] 2024 Oct 11. Date of Electronic Publication: 2024 Oct 11.

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