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[111In]-Ethylenedicysteine-murine anti-phosphotyrosine antibody.


Chopra A1.


Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004-2013.
2009 Mar 12 [updated 2009 Apr 06].

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National Center for Biotechnology Information, NLM, NIH, Bethesda, MD 20894


The overexpression or constitutive activation of non-receptor tyrosine kinase (TK) such as Src- and Bcr-Abl is one of the several mechanisms known to initiate and participate in the progression and metastasis of cancer (1, 2). Because of their role in the development of different neoplasms, small-molecule drugs such as imatinib, dasatinib, and others that block TK activity by inhibiting ATP binding to the enzyme are often used to treat patients suffering from this disease (3, 4). Because several different TK blockers are either under development or are being evaluated in clinical trials to treat cancers, it is important to be able to screen patients to determine which TK inhibitor is likely to result in a good prognosis for an individual (5). Although invasive procedures such as biopsies are routinely used to determine the efficacy of an anti-cancer treatment, a noninvasive technique such as imaging would probably be preferred to evaluate drug activity during early stages of the treatment. Wu et al. envisioned that antibodies labeled with a radionuclide and directed toward an intracellular non-receptor TK could be used for the noninvasive determination of drug efficacy (5). The investigators evaluated an ethylenedicysteine (EC)-murine anti-phosphotyrosine (APT) antibody labeled with radioactive indium (111In) (111In-EC-APT) to image the Bcr-Abl TK, which is known to be upregulated and to promote chronic myeloid leukemia (6), in a mouse xenograft tumor model. The radiolabeled antibody (Ab) was also used to investigate tumor imaging changes in the animals after treatment with imatinib.

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