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3
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The construction and use of a human-mouse myeloma analogue suitable for the routine production of hybridomas secreting human monoclonal antibodies.一种适用于常规生产分泌人单克隆抗体杂交瘤的人-鼠骨髓瘤类似物的构建与应用。
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Effects of a novel vitamin D analogue MC903 on cell proliferation and differentiation in vitro and on calcium metabolism in vivo.
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Novel vitamin D analogs that modulate leukemic cell growth and differentiation with little effect on either intestinal calcium absorption or bone mobilization.新型维生素D类似物可调节白血病细胞的生长和分化，而对肠道钙吸收或骨动员几乎没有影响。
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1,25(OH)2维生素D3类似物对人慢性粒细胞白血病细胞系RWLeu-4增殖和分化的影响

Effects of analogs of 1,25(OH)2 vitamin D3 on the proliferation and differentiation of the human chronic myelogenous leukemia cell line, RWLeu-4.

作者信息

Clark J W, Posner M R, Marsella J M, Santos A, Uskokovic M, Eil C, Lasky S R

机构信息

Division of Hematology/Oncology Roger Williams General Hospital, Providence, Rhode Island 02908.

出版信息

J Cancer Res Clin Oncol. 1992;118(3):190-4. doi: 10.1007/BF01410133.

DOI:10.1007/BF01410133
PMID:1372318
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12201323/
Abstract

We evaluated the proliferative and differentiative effects of analogs of 1,25(OH)2 vitamin D3 [1,25(OH)2D3] on a chronic myelogenous leukemia cell line, RWLeu-4, which is growth-inhibited and differentiates in response to 1,25(OH)2D3 (ED50 = 3-10 nM). Side-chain-fluorinated analogs were more potent (ED50 = 0.7-2 nM) while most of those with altered saturation of the D ring or side-chain carbon-carbon bonds were equally or less effective than 1,25(OH)2D3. However, the two analogs with either two additional double bonds or an extra double and triple bond in the D ring had greater antiproliferative activity [1,25(OH)2-16,23-diene D3 (ED50 = 2.7 nM) and 1,25(OH)2-16-ene-23-yne D3 (ED50 = 0.7 nM)]. Since the latter of these has been reported to be less potent at mobilizing calcium than 1,25(OH)2D3, it (or a similar compound) may be a candidate for clinical use as an antineoplastic agent.

摘要

我们评估了1,25(OH)2维生素D3[1,25(OH)2D3]类似物对慢性粒细胞白血病细胞系RWLeu-4的增殖和分化作用，该细胞系对1,25(OH)2D3（半数有效浓度=3-10 nM）生长受抑制并发生分化。侧链氟化类似物活性更强（半数有效浓度=0.7-2 nM），而大多数D环饱和度或侧链碳-碳键改变的类似物与1,25(OH)2D3相比效果相同或更差。然而，在D环中有两个额外双键或一个额外双键和三键的两种类似物具有更强的抗增殖活性[1,25(OH)2-16,23-二烯D3（半数有效浓度=2.7 nM）和1,25(OH)2-16-烯-23-炔D3（半数有效浓度=0.7 nM）]。由于据报道后者在动员钙方面的效力低于1,25(OH)2D3，它（或类似化合物）可能是作为抗肿瘤药物临床应用的候选物。