857892-34-3Relevant academic research and scientific papers
Optimization of IEDDA bioorthogonal system: Efficient process to improve trans-cyclooctene/tetrazine interaction
Béquignat, Jean-Baptiste,Boucheix, Claude,Canitrot, Damien,Chezal, Jean-Michel,Degoul, Fran?oise,Miot-Noirault, Elisabeth,Moreau, Emmanuel,Navarro-Teulon, Isabelle,Quintana, Mercedes,Rondon, Aurélie,Taiariol, Ludivine,Ty, Nancy
, (2020/07/21)
The antibody pretargeting approach for radioimmunotherapy (RIT) using inverse electron demand Diels-Alder cycloaddition (IEDDA) constitutes an emerging theranostic approach for solid cancers. However, IEDDA pretargeting has not reached clinical trial. The major limitation of the IEDDA strategy depends largely on trans-cyclooctene (TCO) stability. Indeed, TCO may isomerize into the more stable but unreactive cis-cyclooctene (CCO), leading to a drastic decrease of IEDDA efficiency. We have thus developed both efficient and reproducible synthetic pathways and analytical follow up for (PEGylated) TCO derivatives, providing high TCO isomeric purity for antibody modification. We have set up an original process to limit the isomerization of TCO to CCO before the mAbs’ functionalization to allow high TCO/tetrazine cycloaddition.
Novel 19F activatable probe for the detection of matrix metalloprotease-2 activity by MRI/MRS
Yue, Xuyi,Wang, Zhe,Zhu, Lei,Wang, Yu,Qian, Chunqi,Ma, Ying,Kiesewetter, Dale O.,Niu, Gang,Chen, Xiaoyuan
, p. 4208 - 4217 (2016/10/13)
Matrix metalloproteases (MMPs) have been found to be highly expressed in a variety of malignant tumor tissues. Noninvasive visualization of MMP activity may play an important role in the diagnosis of MMP associated diseases. Here we report the design and
METHODS AND COMPOSITIONS FOR PROTEIN LABELLING
-
, (2010/09/07)
A modular platform is provided for rapid preparation of various water-soluble prosthetic groups capable to efficiently introduce 18F into proteins with 18F labelling reagents.
A modular platform for the rapid site-specific radiolabeling of proteins with 18F exemplified by quantitative positron emission tomography of human epidermal growth factor receptor 2
Gill, Herman S.,Tinianow, Jeff N.,Ogasawara, Annie,Flores, Judith E.,Vanderbilt, Alexander N.,Raab, Helga,Scheer, Justin M.,Vandlen, Richard,Williams, Simon-P.,Marik, Jan
experimental part, p. 5816 - 5825 (2010/03/24)
Receptor-specific proteins produced by genetic engineering are attractive as PET imaging agents, but labeling with conventional 18F-based prosthetic groups is problematic due to long synthesis times, poor radiochemical yields, and low specific activities. Therefore, we developed a modular platform for the rapid preparation of water-soluble prosthetic groups capable of efficiently introducing 18F into proteins. The utility of this platform is demonstrated by the thiol-specific prosthetic group, [ 18F]FPEGMA, which was used to produce site-specifically 18F-labeled protein (18F-trastuzumab-ThioFab) in 82 min with a total radiochemical yield of 13 ± 3% and a specific activity of 2.2 ( 0.2 Ci/μmol. 18F-trastuzumab-ThioFab retained the biological activity of native protein and was successfully validated in vivo with microPET imaging of Her2 expression in a xenograft tumor-bearing murine model modulated by the Hsp90 inhibitor, 17-(allylamino)-17-demethoxygeldanamycin. 2009 American Chemical Society.
