Discovery of novel TAOK2 inhibitor scaffolds from high-throughput screening

Piala Alexander T.; Akella Radha; Potts Malia B.; Dudics-Giagnocavo Stephanie A.; He Haixia; Wei Shuguang; White Michael A.; Posner Bruce A.; Goldsmith Elizabeth J.

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Discovery of novel TAOK2 inhibitor scaffolds from high-throughput screening

机译：通过高通量筛选发现新型TAOK2抑制剂支架

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The MAP3K (Mitogen Activated Protein Kinase Kinase Kinase) TAOK2 (Thousand-And-One Kinase 2) is an activator of p38 MAP kinase cascade that is up-regulated in response to environmental stresses. A synthetic lethal screen performed using a NSCLC (non-small cell lung cancer) cell line, and a second screen identifying potential modulators of autophagy have implicated TAOK2 as a potential cancer therapeutic target. Using a 200,000 compound high throughput screen, we identified three specific small molecule compounds that inhibit the kinase activity of TAOK2. These compounds also showed inhibition of autophagy. Based on SAR (structure-activity relationship) studies, we have predicted the modifications on the reactive groups for the three compounds. (C) 2016 Elsevier Ltd. All rights reserved.

机译：MAP3K（促分裂原活化蛋白激酶激酶激酶）TAOK2（一千个激酶2）是p38 MAP激酶级联反应的活化剂，可响应环境压力而被上调。使用NSCLC（非小细胞肺癌）细胞系进行的合成致死筛选和确定自噬潜在调节剂的第二次筛选已暗示TAOK2作为潜在的癌症治疗靶标。使用200,000种化合物的高通量筛选，我们鉴定了三种抑制TAOK2激酶活性的特定小分子化合物。这些化合物也显示出对自噬的抑制作用。基于SAR（结构-活性关系）研究，我们预测了这三种化合物的反应性基团的修饰。（C）2016 Elsevier Ltd.保留所有权利。

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《Bioorganic and Medicinal Chemistry Letters》 |2016年第16期|共5页
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Piala Alexander T.; Akella Radha; Potts Malia B.; Dudics-Giagnocavo Stephanie A.; He Haixia; Wei Shuguang; White Michael A.; Posner Bruce A.; Goldsmith Elizabeth J.;
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正文语种 eng
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Kinase; MAP3K; High-throughput screening; Autophagy; Drug discovery; Inhibitor;

机译：激酶;MAP3K;高通量筛选;自噬;药物发现;抑制剂;

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1. Discovery of novel TAOK2 inhibitor scaffolds from high-throughput screening [J] . Piala Alexander T., Akella Radha, Potts Malia B., Bioorganic and Medicinal Chemistry Letters . 2016,第16期

机译：通过高通量筛选发现新型TAOK2抑制剂支架
2. Discovery of structurally-diverse inhibitor scaffolds by high-throughput screening of a fragment library with dimethylarginine dimethylaminohydrolase [J] . LinskyT.W., FastW. Bioorganic and medicinal chemistry . 2012,第18期

机译：通过高通量筛选二甲基精氨酸二甲基氨基水解酶片段库，发现结构多样的抑制剂支架
3. High-throughput screening campaigns against a PI3Kα isoform bearing the H1047R mutation identified potential inhibitors with novel scaffolds [J] . Jia Wang, Jack Urquhart Flanagan, Peter Robin Shepherd, 中国药理学报：英文版 . 2018,第011期

机译：针对带有H1047R突变的PI3Kα亚型的高通量筛选活动确定了具有新型支架的潜在抑制剂
4. Discovery of Novel Inhibitors of Serine Palmitoyltransferase (SPT) by Mass Spectrometry-Based High-Throughput Screening (HTS) [C] . Pete Meyn, Paul Maresca, Maureen Brooks, American Society for Mass Spectrometry Conference on Mass Spectrometry and Allied Topics . 2009

机译：基于质谱的高通量筛选（HTS）发现丝氨酸棕榈酰转移酶（SPT）的新抑制剂
5. Computer-Assisted Drug Discovery Part I: Design, Development, Validation and Application of FRESH, a Novel In-Silico High-throughput Screening Program Part II: Monocarbonyl Curcumin Analogues: Heterocyclic Pleiotropic Kinase Inhibitors that Mediate Anticancer Properties Part III: Development of 2nd Generation NAMFIS Software Program [D] . Shi, Qi 2014

机译：计算机辅助药物发现，第一部分：FRESH的设计，开发，验证和应用，一种新型的硅中高通量筛选程序第二部分：单羰基姜黄素类似物：介导抗癌特性的杂环多效性激酶抑制剂第三部分：第二代药物的开发NAMFIS软件程序
6. Discovery of structurally-diverse inhibitor scaffolds by high-throughput screening of a fragment library with dimethylarginine dimethylaminohydrolase [O] . Thomas W. Linsky, Walter Fast -1

机译：用二甲基丙氨酸二甲基氨基水解酶的碎片文库的高通量筛选来发现结构多样化的抑制剂支架
7. Discovery of structurally-diverse inhibitor scaffolds by high-throughput screening of a fragment library with dimethylarginine dimethylaminohydrolase [O] . Thomas W. Linsky, Walter Fast 2012

机译：用二甲基丙氨酸二甲基氨基水解酶的碎片文库的高通量筛选来发现结构多样化的抑制剂支架

Discovery of novel TAOK2 inhibitor scaffolds from high-throughput screening

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