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令人痛苦的整合素拮抗剂?

Agonizing integrin antagonists?

作者信息

Weis Sara M, Stupack Dwayne G, Cheresh David A

机构信息

Moores UCSD Cancer Center and Department of Pathology, University of California, San Diego, La Jolla, CA 92093, USA.

出版信息

Cancer Cell. 2009 May 5;15(5):359-61. doi: 10.1016/j.ccr.2009.04.005.

DOI:10.1016/j.ccr.2009.04.005
PMID:19411065
Abstract

A recent study published in Nature Medicine reports that low-dose treatment with RGD-mimetic integrin inhibitors may paradoxically enhance angiogenesis and tumor growth. This work implies that delivery of these agents should be redesigned in order to avoid nanomolar plasma concentrations and to improve their efficacy to treat human cancers.

摘要

最近发表在《自然·医学》上的一项研究报告称,用模拟RGD的整合素抑制剂进行低剂量治疗可能会反常地促进血管生成和肿瘤生长。这项研究表明,应该重新设计这些药物的给药方式,以避免纳摩尔级别的血浆浓度,并提高其治疗人类癌症的疗效。

相似文献

1
Agonizing integrin antagonists?令人痛苦的整合素拮抗剂?
Cancer Cell. 2009 May 5;15(5):359-61. doi: 10.1016/j.ccr.2009.04.005.
2
Blockade of alpha v beta3 and alpha v beta5 integrins by RGD mimetics induces anoikis and not integrin-mediated death in human endothelial cells.RGD模拟物对αvβ3和αvβ5整合素的阻断可诱导人内皮细胞发生失巢凋亡,而非整合素介导的细胞死亡。
Blood. 2006 Nov 1;108(9):3035-44. doi: 10.1182/blood-2006-05-023580. Epub 2006 Jul 11.
3
Roles of integrin in tumor development and the target inhibitors.整合素在肿瘤发生发展中的作用及其靶向抑制剂。
Chin J Nat Med. 2019 Apr;17(4):241-251. doi: 10.1016/S1875-5364(19)30028-7.
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The biology of integrins.整合素的生物学
Oncology (Williston Park). 2007 Aug;21(9 Suppl 3):6-12.
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Suppression of tumor angiogenesis through the inhibition of integrin function and signaling in endothelial cells: which side to target?通过抑制内皮细胞中的整合素功能和信号传导来抑制肿瘤血管生成:该靶向哪一方?
Endothelium. 2002;9(3):151-60. doi: 10.1080/10623320213635.
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Biological and molecular properties of a new alpha(v)beta3/alpha(v)beta5 integrin antagonist.一种新型α(v)β3/α(v)β5整合素拮抗剂的生物学和分子特性
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Endothelial cell integrins and COX-2: mediators and therapeutic targets of tumor angiogenesis.内皮细胞整合素与环氧化酶-2:肿瘤血管生成的介质与治疗靶点
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Integrins and cancer.整合素与癌症
Oncology (Williston Park). 2007 Aug;21(9 Suppl 3):13-20.
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[Inhibition of angiogenesis by proteins, peptides and "small molecules"].蛋白质、肽类及“小分子”对血管生成的抑制作用
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Inhibitors of integrins.整合素抑制剂
Curr Opin Pharmacol. 2002 Aug;2(4):394-402. doi: 10.1016/s1471-4892(02)00175-3.

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Focal adhesion in the tumour metastasis: from molecular mechanisms to therapeutic targets.肿瘤转移中的粘着斑:从分子机制到治疗靶点
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Emerging therapeutic opportunities for integrin inhibitors.整合素抑制剂的新兴治疗机会。
Nat Rev Drug Discov. 2022 Jan;21(1):60-78. doi: 10.1038/s41573-021-00284-4. Epub 2021 Sep 17.
3
Side chain effect in the modulation of αβ/αβ integrin activity via clickable isoxazoline-RGD-mimetics: development of molecular delivery systems.
通过可点击异恶唑啉-RGD模拟物调节αβ/αβ整合素活性中的侧链效应:分子递送系统的开发
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Progesterone Treatment Attenuates Glycolytic Metabolism and Induces Senescence in Glioblastoma.孕酮治疗可减弱脑胶质瘤的糖酵解代谢并诱导其衰老。
Sci Rep. 2019 Jan 30;9(1):988. doi: 10.1038/s41598-018-37399-5.
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Thyroid hormones derivatives reduce proliferation and induce cell death and DNA damage in ovarian cancer.甲状腺激素衍生物可降低卵巢癌细胞增殖并诱导其死亡和 DNA 损伤。
Sci Rep. 2017 Nov 28;7(1):16475. doi: 10.1038/s41598-017-16593-x.
6
Thyroid hormone regulates adhesion, migration and matrix metalloproteinase 9 activity via αvβ3 integrin in myeloma cells.甲状腺激素通过αvβ3整合素调节骨髓瘤细胞的黏附、迁移及基质金属蛋白酶9的活性。
Oncotarget. 2014 Aug 15;5(15):6312-22. doi: 10.18632/oncotarget.2205.
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An in vivo neovascularization assay for screening regulators of angiogenesis and assessing their effects on pre-existing vessels.一种用于筛选血管生成调节剂和评估其对已有血管影响的体内血管新生检测方法。
Angiogenesis. 2012 Dec;15(4):643-55. doi: 10.1007/s10456-012-9287-8. Epub 2012 Aug 24.
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Vinculin activators target integrins from within the cell to increase melanoma sensitivity to chemotherapy.衔接蛋白激活剂从细胞内部靶向整合素,从而提高黑色素瘤对化疗的敏感性。
Mol Cancer Res. 2011 Jun;9(6):712-23. doi: 10.1158/1541-7786.MCR-10-0599. Epub 2011 Apr 1.
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Integrins as therapeutic targets: lessons and opportunities.整合素作为治疗靶点:经验与机遇。
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Potential relevance of bell-shaped and u-shaped dose-responses for the therapeutic targeting of angiogenesis in cancer.潜在的钟形和 U 形剂量反应与癌症中血管生成的治疗靶向相关。
Dose Response. 2010 Apr 23;8(3):253-84. doi: 10.2203/dose-response.09-049.Reynolds.