Enzymatic rationale and preclinical support for a potent protein kinase C beta inhibitor in cancer therapy.

Teicher BA; Alvarez E; Mendelsohn LG; Ara G; Menon K; Ways DK

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Enzymatic rationale and preclinical support for a potent protein kinase C beta inhibitor in cancer therapy.

机译：在癌症治疗中有效的蛋白激酶Cβ抑制剂的酶学原理和临床前支持。

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The macrocyclic bisindolylmaleimide, LY333531, selectively inhibits protein kinase C beta 1 and beta 2 isoforms with an approximate IC50 of 5 nanomolar. The efficacy of LY333531 administered alone and in combination with cytotoxic cancer therapies in models of non-small cell lung carcinoma and brain tumors was determined in vivo. In the Lewis lung carcinoma, administration of LY333531 enhanced the activity of paclitaxel and fractionated radiation and, to a lesser degree, carboplatin and gemcitabine. In the human T98G glioblastoma multiforme xenograft, the addition of LY333531 to treatment with carmustine (BCNU) resulted in enhanced tumor response in a nodule grown subcutaneously and increased life-span in animals bearing an intracranial tumor from 37 days in the control animals to 64 days in the BCNU treated animals, and to 104 days in the LY333531 plus BCNU treated animals with 4 out of 5 animals being long-term survivors.

机译：大环双吲哚基马来酰亚胺LY333531选择性抑制蛋白激酶Cβ1和β2亚型，IC50约为5纳摩尔。在体内确定了LY333531单独给药以及与细胞毒性癌症疗法联合给药在非小细胞肺癌和脑肿瘤模型中的功效。在刘易斯肺癌中，LY333531的使用增强了紫杉醇的活性和放射线分馏，并在较小程度上增强了卡铂和吉西他滨的活性。在人类T98G多形胶质母细胞瘤异种移植物中，在卡莫司汀（BCNU）的治疗中添加LY333531可使皮下生长的结节中的肿瘤反应增强，并使患有颅内肿瘤的动物的寿命从对照动物的37天增加到64天在BCNU处理过的动物中，以及LY333531加BCNU处理过的动物中有104天，其中五分之四是长期存活者。

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《Advances in enzyme regulation》 |1999年第0期|共15页
作者
Teicher BA; Alvarez E; Mendelsohn LG; Ara G; Menon K; Ways DK;
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正文语种 eng
中图分类生物化学;
关键词
Enzyme Inhibitors; Isoenzymes; Neoplasms; Experimental; Protein Kinase C; 酶抑制剂; 同工酶类; 肿瘤; 实验性; 蛋白激酶C;

机译：Enzyme Inhibitors;Isoenzymes;Neoplasms;Experimental;Protein Kinase C;酶抑制剂;同工酶类;肿瘤;实验性;蛋白激酶C;

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1. Enzymatic rationale and preclinical support for a potent protein kinase C beta inhibitor in cancer therapy. [J] . Teicher BA, Alvarez E, Mendelsohn LG, Advances in enzyme regulation . 1999,第0期

机译：在癌症治疗中有效的蛋白激酶Cβ抑制剂的酶学原理和临床前支持。
2. Preclinical rationale for use of the clinically available multitargeted tyrosine kinase inhibitor crizotinib in ROS1-translocated lung cancer [J] . YasudaH., DeFigueiredo-PontesL.L., KobayashiS., Journal of thoracic oncology: official publication of the International Association for the Study of Lung Cancer . 2012,第7期

机译：临床上可利用的多靶点酪氨酸激酶抑制剂克唑替尼用于ROS1易位肺癌的临床前理由
3. Preclinical testing of 5-amino-1-((1R,2S,3S,4R)-2,3-dihydroxy-4-methylcyclopentyl)-1H-imidazole-4-carboxamide: a potent protein kinase C-iota inhibitor as a potential prostate carcinoma therapeutic [J] . Apostolatos Andre H., Apostolatos Christopher A., Ratnayake Wishrawana S., Anti-cancer drugs . 2019,第1期

机译：5-氨基-1 - （（1R，2S，3S，4R）-2,3-二羟基-4-甲基环戊基）-1H-咪唑-4-甲酰胺：一种效率的蛋白激酶C-IOTA抑制剂作为潜力的临床前试验前列腺癌治疗
4. Screening of Indonesian Phytochemicals as Adenylate Kinase 2 Inhibitor for Cancer Therapy. [C] . Dhea Qiasita, Dono Indarto, Yuliana Heri Suselo International Conference on Biomedical Engineering . 2018

机译：印度尼西亚植物化学物质作为腺苷酸激酶2抑制剂的癌症治疗筛选。
5. Preclinical evaluation of inhibitors of the phosphatidylinositide 3-kinase/protein kinase B cell survival pathway in the treatment of pancreatic cancer. [D] . Ng, Sylvia Sze Wai. 2002

机译：磷脂酰肌醇3激酶/蛋白激酶B细胞存活途径抑制剂在胰腺癌治疗中的临床前评价。
6. Discovery of Potent Orally Active Compounds of Tyrosine Kinase and Serine/Threonine-Protein Kinase Inhibitor With Anti-Tumor Activity in Preclinical Assays [O] . Yun-Qing Qiu, Jue Zhou, Xin-Shan Kang, 2012

机译：在临床前测定中发现具有酪氨酸活性的酪氨酸激酶和丝氨酸/苏氨酸蛋白激酶抑制剂的有效口服活性化合物
7. Cyclin-dependent kinase inhibitor dinaciclib potently synergizes with cisplatin in preclinical models of ovarian cancer [O] . Xiu-Xiu Chen, Feng-Feng Xie, Xiu-Jie Zhu, 2015

机译：Cyclin依赖性激酶抑制剂Dinaciclib在卵巢癌的临床前模型中与顺铂有效地协同
8. Preclinical Testing the Therapeutic Potential of a Potent and Novel Small-molecule Inhibitor of Bc1-2 as a Novel Therapy for Hormone-refractory Prostate Cancer; Final rept. 30 Nov 2004-29 Nov 2007 [R] . Wang, S. 2007

机译：临床前测试有效和新型Bc1-2小分子抑制剂的治疗潜力，作为激素难治性前列腺癌的新疗法;最终的评论。 2004年11月30日至2007年11月29日

Enzymatic rationale and preclinical support for a potent protein kinase C beta inhibitor in cancer therapy.

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