0000000000870899

AUTHOR

Helmut R. Maecke

showing 2 related works from this author

(R)-NODAGA-PSMA: A Versatile Precursor for Radiometal Labeling and Nuclear Imaging of PSMA-Positive Tumors

2015

Purpose The present study aims at developing and evaluating an urea-based prostate specific membrane antigen (PSMA) inhibitor suitable for labeling with 111In for SPECT and intraoperative applications as well as 68Ga and 64Cu for PET imaging. Methods The PSMA-based inhibitor-lysine-urea-glutamate-coupled to the spacer Phe-Phe-D-Lys(suberoyl) and functionalized with the enantiomerically pure prochelator (R)-1-(1-carboxy-3-carbotertbutoxypropyl)-4,7-carbotartbutoxymethyl)-1,4,7-triazacyclononane ((R)-NODAGA(tBu)3), to obtain (R)-NODAGA-Phe-Phe-D-Lys(suberoyl)-Lys-urea-Glu (CC34). CC34 was labeled with 111In, 68Ga and 64Cu. The radioconjugates were further evaluated in vitro and in vivo in LNC…

Glutamate Carboxypeptidase IIMaleBiodistributionPathologymedicine.medical_specialtylcsh:MedicineGallium RadioisotopesAcetatesurologic and male genital diseasesHeterocyclic Compounds 1-RingMicechemistry.chemical_compoundPharmacokineticsIn vivoLNCaPImage Processing Computer-AssistedTumor Cells CulturedGlutamate carboxypeptidase IImedicineAnimalsHumansTissue Distributionlcsh:ScienceIncubationMice Inbred BALB CMultidisciplinaryChemistrylcsh:RProstatic NeoplasmsXenograft Model Antitumor AssaysMolecular biologyIn vitroPositron-Emission TomographyAntigens SurfaceUreaFemalelcsh:QRadiopharmaceuticalsResearch ArticlePLOS ONE
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AMD3100: A Versatile Platform for CXCR4 Targeting 68 Ga-Based Radiopharmaceuticals

2016

International audience; CXCR4 is a G protein-coupled receptor (GPCR), which is overexpressed in numerous diseases, particularly in multiple cancers. Therefore, this receptor represents a valuable target for imaging and therapeutic purposes. Among the different approaches, which were developed for CXCR4 imaging, a CXCR4 antagonist biscyclam system (AMD3100, also called Mozobil), currently used in the clinic for the mobilization of hematopoietic stem cells, was radiolabeled with different radiometals such as 62Zn, 64Cu, 67Ga, or 99mTc. However, cyclam is not an ideal chelator for most of these radiometals, and could lead to the release of the radionuclide in vivo. In the current study, a new …

0301 basic medicineBenzylaminesReceptors CXCR4Biomedical EngineeringPharmaceutical ScienceGallium Radioisotopes[SDV.CAN]Life Sciences [q-bio]/CancerBioengineeringPharmacologyCyclamsCXCR4[ CHIM ] Chemical Sciences[ SDV.CAN ] Life Sciences [q-bio]/Cancer03 medical and health scienceschemistry.chemical_compound0302 clinical medicineHeterocyclic CompoundsIn vivoCyclamHumans[CHIM]Chemical SciencesMoietyReceptorG protein-coupled receptorPharmacologyCXCR4CXCR4 antagonistChemistryOrganic Chemistry3. Good health030104 developmental biology030220 oncology & carcinogenesisCancer researchStem cellBiotechnology
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