Radiotheranostics with radiolanthanides: Design, development strategies, and medical applications
TL;DR: This review discusses radiotheranostics with radiolanthanides, focusing on the design, development strategies, and medical applications of radiolAnthanide-labeled probes.
About: This article is published in Coordination Chemistry Reviews.The article was published on 2019-03-15. It has received 27 citations till now.
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TL;DR: The background of the interactions of BPs with bone cells that form the basis of the classical treatment are described and another example of the pleiotropic function of BPS which involves targeting the imaging agents to bone tissues accompanied by pain reduction is presented.
48 citations
TL;DR: A series of thorium(IV)-imido complexes was synthesized and characterized, providing unique experimental evidence for the larger covalent character of 4f05d0 Ce(IV) multiple bonds compared to its 5f06d0 Th( IV) actinide congener.
Abstract: A series of thorium(IV)-imido complexes was synthesized and characterized. Extensive experimental and computational comparisons with the isostructural cerium(IV)-imido complexes revealed a notably more covalent bonding arrangement for the Ce═N bond compared with the more ionic Th═N bond. The thorium-imido moieties were observed to be 3 orders of magnitude more basic than their cerium congeners. More generally, these results provide unique experimental evidence for the larger covalent character of 4f05d0 Ce(IV) multiple bonds compared to its 5f06d0 Th(IV) actinide congener.
46 citations
TL;DR: DFT calculations suggest that a key factor in the enhanced selectivity of this ligand for the large f-block ions is its rigid macrocyclic core, which cannot adequately distort to interact effectively with small ions.
Abstract: The f-block elements, which comprise both the lanthanide and actinide series, possess interesting spectroscopic, magnetic, and nuclear properties that make them uniquely suited for a range of biome...
46 citations
01 Mar 2019
TL;DR: A novel 211At-labeling method is demonstrated using the RGD peptide as a model peptide for direct labeling of proteins or peptides into the tyrosine residue with 211At, showing high accumulation in the tumor and similar biodistribution.
Abstract: Alpha particle-emitting radionuclides have gained considerable attention for radionuclide therapy. Astatine-211 (211At) is a promising alpha particle-emitting radionuclide. 211At is a halogen that has similar chemical properties to iodine and exhibits a half-life of 7.2 h. However, direct labeling of proteins or peptides into the tyrosine residue with 211At was shown to be impractical. Herein, we demonstrate a novel 211At-labeling method using the RGD peptide as a model peptide. An 211At-labeled RGD peptide, [211At]c[RGDf(4-At)K], was prepared from a precursor with a tributylstannyl group on the phenylalanine residue in c(RGDfK) with a radiochemical yield of 63% and a radiochemical purity of >96%, and its potential for targeted radionuclide therapy was evaluated. Based on the results of biodistribution experiments, [125I]c[RGDf(4-I)K] and [211At]c[RGDf(4-At)K] showed high accumulation in the tumor and similar biodistribution. This study provides useful information for radiotheranostics between an 211At-la...
25 citations
TL;DR: In this paper, the authors provide some perspectives of using the TRIUMF ISOL facility (ISAC) to produce medical radionuclides for targeted radiation therapy application and highlight the current effort to collect of 165Er and 155Tb for Auger Therapy and SPECT imaging, respectively.
14 citations
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TL;DR: The effective ionic radii of Shannon & Prewitt [Acta Cryst. (1969), B25, 925-945] are revised to include more unusual oxidation states and coordinations as mentioned in this paper.
Abstract: The effective ionic radii of Shannon & Prewitt [Acta Cryst. (1969), B25, 925-945] are revised to include more unusual oxidation states and coordinations. Revisions are based on new structural data, empirical bond strength-bond length relationships, and plots of (1) radii vs volume, (2) radii vs coordination number, and (3) radii vs oxidation state. Factors which affect radii additivity are polyhedral distortion, partial occupancy of cation sites, covalence, and metallic character. Mean Nb5+-O and Mo6+-O octahedral distances are linearly dependent on distortion. A decrease in cation occupancy increases mean Li+-O, Na+-O, and Ag+-O distances in a predictable manner. Covalence strongly shortens Fe2+-X, Co2+-X, Ni2+-X, Mn2+-X, Cu+-X, Ag+-X, and M-H- bonds as the electronegativity of X or M decreases. Smaller effects are seen for Zn2+-X, Cd2+-X, In2+-X, pb2+-X, and TI+-X. Bonds with delocalized electrons and therefore metallic character, e.g. Sm-S, V-S, and Re-O, are significantly shorter than similar bonds with localized electrons.
51,997 citations
TL;DR: The adhesion receptor integrin alpha v beta 3 was identified as a marker of angiogenic vascular tissue in this paper, and it showed a fourfold increase in expression during angiogenesis on the chick chorioallantoic membrane.
Abstract: Angiogenesis depends on the adhesive interactions of vascular cells. The adhesion receptor integrin alpha v beta 3 was identified as a marker of angiogenic vascular tissue. Integrin alpha v beta 3 was expressed on blood vessels in human wound granulation tissue but not in normal skin, and it showed a fourfold increase in expression during angiogenesis on the chick chorioallantoic membrane. In the latter assay, a monoclonal antibody to alpha v beta 3 blocked angiogenesis induced by basic fibroblast growth factor, tumor necrosis factor-alpha, and human melanoma fragments but had no effect on preexisting vessels. These findings suggest that alpha v beta 3 may be a useful therapeutic target for diseases characterized by neovascularization.
2,926 citations
TL;DR: In this article, a single intravascular injection of a cyclic peptide or monoclonal antibody antagonist of integrin alpha v beta 3 disrupts ongoing angiogenesis on the chick chorioallantoic membrane (CAM).
2,318 citations
TL;DR: There is tremendous potential for all antibody fragments either as robust diagnostic reagents, or as nonimmunogenic in vivo biopharmaceuticals with superior biodistribution and blood clearance properties.
Abstract: With 18 monoclonal antibody (mAb) products currently on the market and more than 100 in clinical trials, it is clear that engineered antibodies have come of age as biopharmaceuticals. In fact, by 2008, engineered antibodies are predicted to account for >30% of all revenues in the biotechnology market. Smaller recombinant antibody fragments (for example, classic monovalent antibody fragments (Fab, scFv)) and engineered variants (diabodies, triabodies, minibodies and single-domain antibodies) are now emerging as credible alternatives. These fragments retain the targeting specificity of whole mAbs but can be produced more economically and possess other unique and superior properties for a range of diagnostic and therapeutic applications. Antibody fragments have been forged into multivalent and multispecific reagents, linked to therapeutic payloads (such as radionuclides, toxins, enzymes, liposomes and viruses) and engineered for enhanced therapeutic efficacy. Recently, single antibody domains have been engineered and selected as targeting reagents against hitherto immunosilent cavities in enzymes, receptors and infectious agents. Single-domain antibodies are anticipated to significantly expand the repertoire of antibody-based reagents against the vast range of novel biomarkers being discovered through proteomics. As this review aims to show, there is tremendous potential for all antibody fragments either as robust diagnostic reagents (for example in biosensors), or as nonimmunogenic in vivo biopharmaceuticals with superior biodistribution and blood clearance properties.
2,167 citations
University of South Florida1, University of Kentucky2, Cedars-Sinai Medical Center3, University of Texas MD Anderson Cancer Center4, Stanford University5, Harvard University6, University of Iowa7, Royal Free Hospital8, Mayo Clinic9, Katholieke Universiteit Leuven10, Northwestern University11, University of Cambridge12, Charité13, University of Barcelona14, Vanderbilt University15, Uppsala University16, Erasmus University Rotterdam17
TL;DR: Treatment with lutetium‐177 (177Lu)–Dotatate resulted in markedly longer progression‐free survival and a significantly higher response rate than high‐dose octreotide LAR among patients with advanced midgut neuroendocrine tumors.
Abstract: BackgroundPatients with advanced midgut neuroendocrine tumors who have had disease progression during first-line somatostatin analogue therapy have limited therapeutic options. This randomized, controlled trial evaluated the efficacy and safety of lutetium-177 (177Lu)–Dotatate in patients with advanced, progressive, somatostatin-receptor–positive midgut neuroendocrine tumors. MethodsWe randomly assigned 229 patients who had well-differentiated, metastatic midgut neuroendocrine tumors to receive either 177Lu-Dotatate (116 patients) at a dose of 7.4 GBq every 8 weeks (four intravenous infusions, plus best supportive care including octreotide long-acting repeatable [LAR] administered intramuscularly at a dose of 30 mg) (177Lu-Dotatate group) or octreotide LAR alone (113 patients) administered intramuscularly at a dose of 60 mg every 4 weeks (control group). The primary end point was progression-free survival. Secondary end points included the objective response rate, overall survival, safety, and the side-ef...
1,975 citations