Výsledky vyhledávání - "Renzo Cescato"

Switch from antagonist to agonist after addition of a DOTA chelator to a somatostatin analog

Autor: Judit Erchegyi, Jean Claude Reubi, Renzo Cescato, Beatrice Waser, Jean Rivier

Publikováno v: Reubi, Jean Claude; Erchegyi, Judit; Cescato, Renzo; Waser, Beatrice; Rivier, Jean E (2010). Switch from antagonist to agonist after addition of a DOTA chelator to a somatostatin analog. European journal of nuclear medicine and molecular imaging, 37(8), pp. 1551-8. Berlin: Springer-Verlag 10.1007/s00259-010-1445-x

Purpose: Peptide receptor targeting has become an increasingly attractive method to target tumors diagnostically and radiotherapeutically. Peptides linked to a variety of chelators have been developed for this purpose. They have, however, rarely been

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1253f28031df30c384bd99ba65a7821f
http://doc.rero.ch/record/319191/files/259_2010_Article_1445.pdf

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Syntheses, Receptor Bindings,in vitroandin vivoStabilities and Biodistributions of DOTA-Neurotensin(8-13) Derivatives Containingβ-Amino Acid Residues - A Lesson about the Importance of Animal Experiments

Autor: Renzo Cescato, Christof Sparr, Harald Hübner, Beata Kolesinska, Beatrice Waser, Simone Maschauer, Dieter Seebach, Peter Gmeiner, Nirupam Purkayastha, Tomohiro Yoshinari, Jean Claude Reubi, Olaf Prante

Publikováno v: Chemistry & Biodiversity. 10:2101-2121

Neurotensin(8-13) (NTS(8-13)) analogs with C- and/or N-terminal β-amino acid residues and three DOTA derivatives thereof have been synthesized (i.e., 1-6). A virtual docking experiment showed almost perfect fit of one of the 1,4,7,10-tetraazacyclodo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::51126a0cfbd69f74d6c25bb80795f737
https://doi.org/10.1002/cbdv.201300331

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[99mTc]Demomedin C, a Radioligand Based on Human Gastrin Releasing Peptide(18-27): Synthesis and Preclinical Evaluation in Gastrin Releasing Peptide Receptor-Expressing Models

Autor: Eleni Ketani, Renzo Cescato, Berthold A. Nock, Beatrice Waser, Jean Claude Reubi, Theodosia Maina

Publikováno v: Journal of Medicinal Chemistry. 55:8364-8374

The synthesis and preclinical evaluation of [(99m)Tc]Demomedin C in GRPR-expressing models are reported. Demomedin C resulted by coupling a Boc-protected N(4)-chelator to neuromedin C (human GRP(18-27)), which, after (99m)Tc-labeling, afforded [(99m)

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1c49f6007dd71d1a63bf0afd8994c018
https://doi.org/10.1021/jm300741f

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Unexpected Sensitivity of sst2 Antagonists to N-Terminal Radiometal Modifications

Autor: Renzo Cescato, Helmut R. Maecke, Friederike Braun, Melpomeni Fani, Karin Beetschen, Judit Erchegyi, Jean Claude Reubi, Wolfgang Weber, Beatrice Waser, Jean Rivier

Publikováno v: Journal of Nuclear Medicine. 53:1481-1489

Chelated somatostatin agonists have been shown to be sensitive to N-terminal radiometal modifications, with Ga-DOTA agonists having significantly higher binding affinity than their Lu-, In-, and Y-DOTA correlates. Recently, somatostatin antagonists h

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0b9e7e7ded9e38b5156c30415b46997f
https://doi.org/10.2967/jnumed.112.102764

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Bombesin Antagonist–Based Radioligands for Translational Nuclear Imaging of Gastrin-Releasing Peptide Receptor–Positive Tumors

Autor: Rosalba Mansi, Maria-Luisa Tamma, Renzo Cescato, Jean Claude Reubi, Keelara Abiraj, Flavio Forrer, Melpomeni Fani, Helmut R. Maecke, Guillaume Nicolas

Publikováno v: Journal of Nuclear Medicine. 52:1970-1978

Bombesin receptors are overexpressed on a variety of human tumors. In particular, the gastrin-releasing peptide receptor (GRPr) has been identified on prostate and breast cancers and on gastrointestinal stromal tumors. The current study aims at devel

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cad4b25e457763e7157dbf0fbf3fc4d9
https://doi.org/10.2967/jnumed.111.094375

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Evaluation of 177Lu-DOTA-sst2 Antagonist Versus 177Lu-DOTA-sst2 Agonist Binding in Human Cancers In Vitro

Autor: Beatrice Waser, Renzo Cescato, Melpomeni Fani, Jean Claude Reubi

Publikováno v: Journal of Nuclear Medicine. 52:1886-1890

Somatostatin receptor targeting of neuroendocrine tumors using radiolabeled somatostatin agonists is today an established method to image and treat cancer patients. However, in a study using an animal tumor model, somatostatin receptor antagonists we

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0bd29364ed89b65f4f10d94e2014f546
https://doi.org/10.2967/jnumed.111.095778

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PET of Somatostatin Receptor–Positive Tumors Using 64Cu- and 68Ga-Somatostatin Antagonists: The Chelate Makes the Difference

Autor: Rosalba Mansi, Melpomeni Fani, Wolfgang Weber, Keelara Abiraj, Luigi Del Pozzo, Maria Luisa Tamma, Renzo Cescato, Helmut R. Maecke, Beatrice Waser, Jean Claude Reubi

Publikováno v: Journal of Nuclear Medicine. 52:1110-1118

Somatostatin-based radiolabeled peptides have been successfully introduced into the clinic for targeted imaging and radionuclide therapy of somatostatin receptor (sst)-positive tumors, especially of subtype 2 (sst2). The clinically used peptides are

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9c1857e823c27938e26952a9ca07c75a
https://doi.org/10.2967/jnumed.111.087999

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Radiolabeled Bicyclic Somatostatin-Based Analogs: A Novel Class of Potential Radiotracers for SPECT/PET of Neuroendocrine Tumors

Autor: Renzo Cescato, Maria-Luisa Tamma, Guillaume Nicolas, Helmut R. Maecke, Andreas Mueller, Melpomeni Fani, Jean Claude Reubi, Hans R. Rink

Publikováno v: Journal of Nuclear Medicine. 51:1771-1779

A variety of radiolabeled somatostatin analogs have been developed for targeting of somatostatin receptor (sst)-positive tumors. Bicyclic somatostatin-based radiopeptides have not been studied yet. Hypothesizing that the introduction of conformationa

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::944bc14052eb685520557a2f857a8ffd
https://doi.org/10.2967/jnumed.110.076695

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Development of a potent DOTA-conjugated bombesin antagonist for targeting GRPr-positive tumours

Autor: Flavio Forrer, Rosalba Mansi, Renzo Cescato, Xuejuan Wang, Keith Graham, Helmut R. Maecke, Beatrice Waser, Sandra Borkowski, Jean Claude Reubi

Publikováno v: Mansi, Rosalba; Wang, Xuejuan; Forrer, Flavio; Waser, Beatrice; Cescato, Renzo; Graham, Keith; Borkowski, Sandra; Reubi, Jean-Claude; Maecke, Helmut R (2011). Development of a potent DOTA-conjugated bombesin antagonist for targeting GRPr-positive tumours. European journal of nuclear medicine and molecular imaging, 38(1), pp. 97-107. Berlin: Springer 10.1007/s00259-010-1596-9

Radiolabelled somatostatin-based antagonists show a higher uptake in tumour-bearing mouse models than agonists of similar or even distinctly higher receptor affinity. Very similar results were obtained with another family of G protein-coupled recepto

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::57865ad0f64b6ab7f69a71bdb48b1050
https://doi.org/10.1007/s00259-010-1596-9

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