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Human prostate cancer stem cells: new features unveiled 被引量:1
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作者 Yuting Sun Wei-Qiang Gao 《Asian Journal of Andrology》 SCIE CAS CSCD 2011年第3期355-356,共2页
Cancer stem cells (CSCs) are a rare subpopulation of phenotypically distinct cancer cells exhibiting stem cell characteristics. They are tumourigenic, meanwhile capable of self-renewal and forming differentiated pro... Cancer stem cells (CSCs) are a rare subpopulation of phenotypically distinct cancer cells exhibiting stem cell characteristics. They are tumourigenic, meanwhile capable of self-renewal and forming differentiated progenies. CSCs are believed to be resistant to the standard therapeutics, and provide the cell reservoir for tumour initiation.1 Understanding CSCs or in another word, tumour-initiating cells, is of critical therapeutic importance. 展开更多
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Tissue distribution and tumor uptake of folate receptor–targeted epothilone folate conjugate,BMS-753493,in CD2F1 mice after systemic administration 被引量:3
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作者 Hong Shen Lifei Wang +7 位作者 Weiqi Chen Krista Menard Yang Hong Yuan Tian Samuel J.Bonacorsi W.Griffith Humphreys Francis Y.Lee Jinping Gan 《Acta Pharmaceutica Sinica B》 SCIE CAS CSCD 2016年第5期460-467,共8页
To assess targeting of an epothilone folate conjugate(BMS-753493) to the folate receptor(FR)-overexpressed tumor in mice bearing both FRt and FR– tumors,a series of experiments were conducted by quantitative whole-bo... To assess targeting of an epothilone folate conjugate(BMS-753493) to the folate receptor(FR)-overexpressed tumor in mice bearing both FRt and FR– tumors,a series of experiments were conducted by quantitative whole-body autoradiography(QWBA) and LC–MS/MS following i.v.administration of BMS-753493 or its active moiety,BMS-748285 in mice bearing FRt(98M109) and FR–(M109) tumors.QWBA showed [3H]BMS-753493–derived radioactivity was extensively distributed to various tissues.The FR over-expressing 98M109 tumors showed consistently higher level of radioactivity than FR-negative tumors(i.e.,M109 tumors) up to 48 h post dose of [3H]BMS-753493,despite the magnitude of difference between the tumors is relatively small(generally 3 5-fold).The radioactivity level in 98M109 tumors was 2 12-fold of normal tissues except intestine/content at 48 h post dose.No selective radioactivity uptake into 98M109 tumors over M109 or normal tissues was observed after i.v.administration of the active epothilone,[3H]BMS-748285.LC–MS/MS measurements demonstrated that the concentrations of BMS-748285,presumably from hydrolysis of the folate conjugate,in 98M109 tumors were greater than those in M109 tumors after i.v.administration of BMS-753493(2–3-fold) whereas no differential uptake in the tumors following BMS-748285 administration.Those data were consistent with radioactivity determinations.Those results demonstrated that the folate conjugation in BMS-753493 enabled moderately preferential distribution of the active epothilone to FR overexpressing 98M109 tumors,thereby supporting targeted delivery of cytotoxics through the folate receptor. 展开更多
关键词 Folate RECEPTOR TUMOR selective targeting Folate receptor–expressing TUMOR EPOTHILONE folate CONJUGATE Tissue distribution TUMOR UPTAKE
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