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- W2418258604 abstract "N1,N1-diethyl-N4-(7-[125I]iodoquinolin-4-yl)pentane-1,4-diamine, abbreviated as 125I IQ, is a compound synthesized by Chin et al. for imaging cancer stem cells (CSCs) by targeting aldehyde dehydrogenase 1A1 (ALDH1) (1).CSCs, also known as tumor-initiating cells, have been defined as a minor population of quiescent cells that possess the capacity for self-renewal, can generate heterogeneous lineages of cancer cells, and are resistant to conventional treatment (2, 3). Currently, there are two conflicting models proposed for cancer development: the stochastic model, which proposes that all cells have an equal possibility of acquiring mutations and initiating a tumor; and the hierarchy model, which proposes that only a distinct and small subset of cancer cells serve as CSCs and give rise to tumors (2, 4). The latter is becoming more popular in the field of tumor biology, and the focus of treatment is shifting from cytotoxic therapy that indiscriminately kills tumor cells to CSC-targeted therapy (5). A key issue to establish CSC-targeted imaging and therapy is the identification of biomarkers that can be used to identify and isolate CSCs from diverse cell populations (1, 3).The cytosolic activity of the enzyme ALDH1 has been shown to be a reliable marker for CSCs in various types of solid tumors (6, 7). Evidence shows that tumor cells with highly expressed ALDH1 are highly tumorigenic, and the high activity of ALDH1 is associated with poor prognosis of many types of tumors. Growing evidence further suggests that ALDH1 is not only a putative stem cell marker but may actually play multiple roles that contribute to stem cell self-protection, differentiation, and self-renewal (4). Chin et al. tested the feasibility of iodoquine (IQ) to localize CSCs by targeting the high ALDH1 activity in tumors (1). IQ is structurally identical to chloroquine (6) with the exception of the halogen substitution of iodine for chlorine. CQ is known as a weak base anti-malarial drug, which accumulates within the digestive vacuoles of parasites as well as within the lysosomes of tumor cells (8). CQ is simply metabolized by the hepatic cytochrome P450 to N-desethylchloroquine and then excreted from kidneys. Recently, Graves et al. used proteomics techniques to determine that ALDH1 is a selective target for CQ (9, 10). These characteristics make CQ an attractive candidate for high-contrast tumor imaging. Chin et al. hypothesized that the structural similarity of IQ to CQ could confer the biochemical behavior and properties similar to the CQ (1). The studies by Chin et al. supported the hypothesis and suggested that IQ is a potential radiotracer for identifying CSCs with high ALDH1 expression (1)." @default.
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- W2418258604 date "2012-05-02" @default.
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- W2418258604 title "N1,N1-diethyl-N4-(7-[125I]iodoquinolin-4-yl)pentane-1,4-diamine" @default.
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