The DOI matches its Crossref record; 1 of the 1 references it cites were found in a registry or an index.
68Ga-Complex Lipophilicity and the Targeting Property of a Urea-Based PSMA Inhibitor for PET Imaging
Abstract
Urea-based inhibitors of the prostate-specific membrane antigen (PSMA) represent low-molecular-weight pepidomimetics showing the ability to image PSMA-expressing prostate tumors. The highly efficient, acyclic Ga(III) chelator N,N'-bis [2-hydroxy-5-(carboxyethyl)benzyl] ethylenediamine-N,N'- diacetic acid (HBED-CC) was introduced as a lipophilic side chain into the hydrophilic pharmacophore Glu-NH-CO-NH-Lys which was found favorable to interact with the PSMA "active binding site". This report describes the syntheses, in vitro binding analyses, and biodistribution data of the radiogallium labeled PSMA inhibitor Glu-NH-CO-NH-Lys(Ahx)-HBED-CC in comparison to the corresponding DOTA conjugate. The binding properties were analyzed using competitive cell binding and enzyme-based assays followed by internalization experiments. Compared to the DOTA-conjugate, the HBED-CC derivative showed reduced unspecific binding and considerable higher specific internalization in LNCaP cells. The (68)Ga complex of the HBED-CC ligand exhibited higher specificity for PSMA expressing tumor cells resulting in improved in vivo properties. (68)Ga labeled Glu-NH-CO-NH-Lys(Ahx)-HBED-CC showed fast blood and organ clearances, low liver accumulation, and high specific uptake in PSMA expressing organs and tumor. It could be demonstrated that the PET-imaging property of a urea-based PSMA inhibitor could significantly be improved with HBED-CC.
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Rajasekaran, S. A., Anilkumar, G., Oshima, E., Bowie, J. U., Liu, H., Heston, W., Bander, N. H., & Rajasekaran, A. K. (2003) · Molecular Biology of the Cell · doi:10.1091/mbc.e02-11-0731 · Cited by 226
Cited by
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Self-citationAfshar-Oromieh, A., Malcher, A., Eder, M., Eisenhut, M., Linhart, H. G., Hadaschik, B. A., Holland-Letz, T., Giesel, F. L., Kratochwil, C., Haufe, S., et al. (2013) · European Journal of Nuclear Medicine and Molecular Imaging · doi:10.1007/s00259-012-2298-2 · Cited by 915
Self-citation68Ga-PSMA PET/CT: Joint EANM and SNMMI procedure guideline for prostate cancer imaging: version 1.0
Fendler, W. P., Eiber, M., Beheshti, M., Bomanji, J., Ceci, F., Cho, S., Giesel, F., Haberkorn, U., Hope, T. A., Kopka, K., et al. (2017) · European Journal of Nuclear Medicine and Molecular Imaging · doi:10.1007/s00259-017-3670-z · Cited by 750
Self-citationE-PSMA: the EANM standardized reporting guidelines v1.0 for PSMA-PET
Ceci, F., Oprea-Lager, D. E., Emmett, L., Adam, J. A., Bomanji, J., Czernin, J., Eiber, M., Haberkorn, U., Hofman, M. S., Hope, T. A., et al. (2021) · European Journal of Nuclear Medicine and Molecular Imaging · doi:10.1007/s00259-021-05245-y · Cited by 368
Self-citationKabasakal, L., AbuQbeitah, M., Aygün, A., Yeyin, N., Ocak, M., Demirci, E., & Toklu, T. (2015) · European Journal of Nuclear Medicine and Molecular Imaging · doi:10.1007/s00259-015-3125-3 · Cited by 208
Biological determinants of PSMA expression, regulation and heterogeneity in prostate cancer
Bakht, M. K., & Beltran, H. (2025) · Nature Reviews Urology · doi:10.1038/s41585-024-00900-z · Cited by 158
Fendler, W. P., Calais, J., Allen-Auerbach, M., Bluemel, C., Eberhardt, N., Emmett, L., Gupta, P., Hartenbach, M., Hope, T. A., Okamoto, S., et al. (2017) · Journal of Nuclear Medicine · doi:10.2967/jnumed.117.190827 · Cited by 141
Nuclear medicine and molecular imaging advances in the 21st century
Vaz, S. C., Oliveira, F., Herrmann, K., & Veit-Haibach, P. (2020) · The British Journal of Radiology · doi:10.1259/bjr.20200095 · Cited by 86
Ringheim, A., Campos Neto, G. D. C., Anazodo, U., Cui, L., da Cunha, M. L., Vitor, T., Martins, K. M., Miranda, A. C. C., de Barboza, M. F., Fuscaldi, L. L., et al. (2020) · EJNMMI Research · doi:10.1186/s13550-020-0594-6 · Cited by 34
Demirci, E., Akyel, R., Caner, B., Alan-Selçuk, N., Güven-Meşe, Ş., Ocak, M., & Kabasakal, L. (2020) · Nuclear Medicine Communications · doi:10.1097/mnm.0000000000001219 · Cited by 26
Kaittanis, C., Bolaender, A., Yoo, B., Shah, N., Ouerfelli, O., & Grimm, J. (2017) · Nano Letters · doi:10.1021/acs.nanolett.7b04209 · Cited by 19
Metadata
- Authors
- Eder, M., Schäfer, M., Bauder-Wüst, U., Hull, W.-E., Wängler, C., Mier, W., Haberkorn, U., & Eisenhut, M.
- Venue
- Bioconjugate Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2012-03-13
- Volume
- 23
- Issue
- 4
- Pages
- 688-697
- ISSN
- 1043-1802 (ISSN-L)
- 1520-4812
- OpenAlex
- W2125363072
- Cited by
- 843
- References
- 1
- FWCI
- 18.25
- Type
- journal article
- Language
- en
- Open access
- closed
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