Preparation and Biological Evaluation of Copper-64–Labeled Tyr3-Octreotate Using a Cross-Bridged Macrocyclic Chelator
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چکیده
منابع مشابه
Octreotate Using a Cross-Bridged Macrocyclic Chelator
Purpose: Somatostatin receptors (SSTr) are expressed on many neuroendocrine tumors, and several radiotracers have been developed for imaging these types of tumors. For this reason, peptide analogues of somatostatin have been well characterized. Copper-64 (t1/2 12.7 hours), a positron emitter suitable for positron emission tomography (PET) imaging, was shown recently to have improved in vivo cle...
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The bifunctional chelator and radiometal have been shown to have a direct effect on the pharmacokinetics of somatostatin receptor (SSTR)-targeted imaging agents. We evaluated three Y3-TATE analogues conjugated to NOTA-based chelators for radiolabeling with 64Cu and 68Ga for small-animal positron emission tomographic/computed tomograhic (PET/CT) imaging. Two commercially available NOTA analogues...
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BACKGROUND Ge/(68)Ga generators provide an inexpensive source of a PET isotope to hospitals without cyclotron facilities. The development of new (68)Ga-based molecular imaging agents and subsequent clinical translation would be greatly facilitated by simplification of radiochemical syntheses. We report the properties of a tris(hydroxypyridinone) conjugate of the SSTR2-targeted peptide, Tyr(3)-o...
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A phosphonate pendant-armed cross-bridged cyclam chelator has been synthesized, complexed to Cu(ii), radiolabeled with (64)Cu under mild conditions, and its biodistribution studied.
متن کاملNew cross-bridged cyclam derivative CB-TE1K1P, an improved bifunctional chelator for copper radionuclides.
A new cross-bridged cyclam chelator, CB-TE1K1P, was developed for copper-based radiopharmaceuticals, and this chelator can be labelled with (64)Cu under mild conditions in high specific activity. DBCO-PEG4-CB-TE1K1P was synthesized for conjugation to proteins, while Dde-CB-TE1K1P((t)Bu2)-OH was synthesized for solid-phase peptide synthesis. Examples of the conjugation chemistry, radiolabelling ...
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ژورنال
عنوان ژورنال: Clinical Cancer Research
سال: 2004
ISSN: 1078-0432,1557-3265
DOI: 10.1158/1078-0432.ccr-04-1084