Preparation and evaluation of 186/188Re-labeled antibody (A7) for radioimmunotherapy with rhenium(I) tricarbonyl core as a chelate site

Ogawa, Kenji; Kawashima, Hidekazu; Kinuya, Seigo; Shiba, Kazuhiro; Onoguchi, Masahisa; Kimura, Hiroyuki; Hashimoto, Kazuhito; Odani, Akira; Saji, Hideo

doi:10.1007/s12149-009-0319-4

Cited by 13 publications

(9 citation statements)

References 20 publications

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“…Rhenium-188 has another advantage: It is conveniently produced from a transportable, alumina-based 188 W/ 188 Re generator, similar to a 99 Mo/ 99m Tc generator. 37,70 Despite its attractive decay properties for targeted radiotherapy, 188 Re has rarely been used for the development of targeted therapeutics for HER2-expressing tumors. In a recent study, Luo et al showed that 188 Re-HYNIC-trastuzumab enhanced the cytotoxicity to tumor tissues to a level nearly 100-fold higher than that of the treatment with trastuzumab alone.…”

Section: Targeting Of Her2 For Radionuclide Therapymentioning

confidence: 99%

Targeting HER2 in Nuclear Medicine for Imaging and Therapy

2018

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Since its discovery, the human epidermal growth factor 2 (HER2) has been extensively studied. Presently, there are 2 standard diagnostic techniques to assess HER2 status in biopsies: immunohistochemistry and fluorescence in situ hybridization. While these techniques have played an important role in the treatment of patients with HER2-positive cancer, they both require invasive biopsies for analysis. Moreover, the expression of HER2 is heterogeneous in breast cancer and can change over the course of the disease. Thus, the degree of HER2 expression in the small sample size of biopsied tumors at the time of analysis may not represent the overall status of HER2 expression in the whole tumor and in between tumor foci in the metastatic setting as the disease progresses. Unlike biopsy, molecular imaging using probes against HER2 allows for a noninvasive, whole-body assessment of HER2 status in real time. This technique could potentially select patients who may benefit from HER2-directed therapy and offer alternative treatments to those who may not benefit. Several antibodies and small molecules against HER2 have been labeled with different radioisotopes for nuclear imaging and/or therapy. This review presents the most recent advances in HER2 targeting in nuclear medicine focusing on preclinical and clinical studies.

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Section: Targeting Of Her2 For Radionuclide Therapymentioning

confidence: 99%

Targeting HER2 in Nuclear Medicine for Imaging and Therapy

2018

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“…Moreover, as mentioned earlier, efforts are made to use the potential of Re(CO) 3 complexes as luminescent probes, and to develop isostructural nuclear and optical probes based on 99m Tc and Re, respectively [22,43,88,90,91]. In addition, 186 Re and 188 Re isotopes can be used for radiotherapy, and 186/188 Re tricarbonyl complexes have been designed for that purpose [92][93][94]. Generally, these complexes, luminescent or not, may be inspirational for further development of Re(CO) 3 complexes as multimodal imaging probes.…”

Section: Re(co) 3 As Surrogates For 99mmentioning

confidence: 99%

Re(I) carbonyl complexes: Multimodal platforms for inorganic chemical biology

Hostachy

Policar

Delsuc

2017

Coordination Chemistry Reviews

113

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Bio-imaging, by enabling the visualization of biomolecules of interest, has proved to be highly informative in the study of biological processes. Although fluorescence microscopy is probably one of the most used techniques, alternative methods of imaging, providing complementary information, are emerging. In this context, metal complexes represent valuable platforms for multimodal imaging, since they may combine interesting spectroscopic features and biologically relevant functionalization on a single molecular core. In particular, d6 low-spin rhenium tri-carbonyl complexes display unique luminescence and vibrational properties, and can be readily functionalized. Here we review their applications and potential as probes or drugs relying on their photophysical properties, before focusing on their use as multimodal probes for the labelling and imaging of peptides and proteins.

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“…+ in proteins are histidine residues and this has been particularly useful for labelling recombinant proteins that incorporate histidine tags (a sequence of typically six consecutive histidine residues) as a purification tool. Proteins without histidines, or with only isolated histidines, label poorly [75] whereas those with oligohistidine sequences can be labelled relatively efficiently [76]. Studies aimed at identifying optimal histidine-containing sequences for labelling with [Re(CO) 3 ] + have shown that as well as multiple histidines, incorporation of cysteine [77] or methionine [70,78] residues into the sequence can enhance labeling efficiency and stability, and incorporation of positively charged amino acids (arginine, lysine) is particularly effective, with the potential to improve specific activity and avoid the need for post-labelling purification steps [78].…”

Section: Stable Well-defined Chelated Derivative With the Square Pyrmentioning

confidence: 99%

Rhenium-188 Radiochemistry: Challenges and Prospects

Blower¹

2017

Int. J. Nucl. Medi. Res.

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After a lull in development of new chemistry for rhenium-188 and technetium-99m since 2000, there has been new investment in production facilities for Mo-99/Tc-99m coupled with increasing interest in rhenium-188 radionuclide therapy, particularly in developing countries. Much of the chemistry developed in the 1990s is not readily amenable to supporting modern radiopharmaceutical development, which places increased emphasis on molecular targeted radiopharmaceuticals. Consequently there is a need for new radiolabelling chemistry to incorporate these radionuclides into biomolecules using simple, kit-based methodology. This review provides an update on progress towards simple rhenium-188 labelling methods since 2000.

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Preparation and evaluation of 186/188Re-labeled antibody (A7) for radioimmunotherapy with rhenium(I) tricarbonyl core as a chelate site

Cited by 13 publications

References 20 publications

Targeting HER2 in Nuclear Medicine for Imaging and Therapy

Targeting HER2 in Nuclear Medicine for Imaging and Therapy

Re(I) carbonyl complexes: Multimodal platforms for inorganic chemical biology

Rhenium-188 Radiochemistry: Challenges and Prospects

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