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Validation of 125ICPCR4.3 as an investigative tool for the sensitive and specific detection of hCXCR4 and mCXCR4 expression in vitro and in vivo

机译:验证125I CPCR4.3作为在体外和体内敏感和特异性检测hCXCR4和mCXCR4表达的研究工具

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摘要

BackgroundThe development and clinical translation of [68Ga] Pentixafor has substantially promoted the relevance of non-invasive PET imaging of CXCR4 expression in a broad spectrum of diseases, including cancer and inflammation. Its pronounced selectivity for the human receptor (hCXCR4), however, precludes the use of [68Ga] Pentixafor for imaging receptor expression and dynamics in CXCR4-related diseases in endogenous mouse models. To overcome this restriction, [125I]CPCR4.3, a structurally related pentapeptide ligand, has been evaluated as a preclinical tool for efficient in vitro and in vivo targeting of hCXCR4 and mCXCR4.
机译:背景[ 68 Ga] Pentixafor的开发和临床翻译已大大促进了CXCR4表达的非侵入性PET成像在包括癌症和炎症在内的各种疾病中的相关性。但是,它对人类受体(hCXCR4)的明显选择性,使得无法使用[ 68 Ga] Pentixafor来成像内源性小鼠模型中CXCR4相关疾病的受体表达和动力学。为了克服这一限制,已经评估了结构上相关的五肽配体[ 125 I] CPCR4.3作为有效体外和体内靶向hCXCR4和mCXCR4的临床前工具。

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