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搜索结果包含 Cancer Res:新研究发现帮助清除癌症干细胞的新靶标 的内容

Aug 21,2023
TAK-931是一种高效的CDC7抑制剂,通过抑制CDC7来抑制DNA复制,具有抗肿瘤功效,体内药效研究通过美迪西进行
Replication stress (RS) is a cancer hallmark; chemotherapeutic drugs targeting RS are widely used as treatments for various cancers. To develop next-generation RS-inducing anticancer drugs, cell divis
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TAK-931是一种高效的CDC7抑制剂,通过抑制CDC7来抑制DNA复制,具有抗肿瘤功效,体内药效研究通过美迪西进行
Jul 06,2023
TRIM24和BRPF1是癌症的潜在治疗靶点。Y08624是一种新型TRIM24/BRPF1双重抑制剂,具有良好的Caco-2渗透性。Caco-2 渗透性测定通过美迪西进行
TRIM24 (tripartite motif-containing protein 24) and BRPF1 (bromodomain and PHD finger containing protein 1) are epigenetics “readers”and potential therapeutic targets for cancer and other diseases. Y0
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TRIM24和BRPF1是癌症的潜在治疗靶点。Y08624是一种新型TRIM24/BRPF1双重抑制剂,具有良好的Caco-2渗透性。Caco-2 渗透性测定通过美迪西进行
Jul 06,2023
IAP蛋白是有吸引力的癌症治疗靶点。SM-406 是一种口服有效的IAP拮抗剂。SM-406 在雄性SD大鼠、比格犬和NHP中的PK研究通过美迪西进行
Apoptosis is a cellular process critical to the normal development and homeostasis of multicellular organisms. The inhibitor of apoptosis proteins (IAPs) are a class of key apoptosis regulators.
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IAP蛋白是有吸引力的癌症治疗靶点。SM-406 是一种口服有效的IAP拮抗剂。SM-406 在雄性SD大鼠、比格犬和NHP中的PK研究通过美迪西进行
Jul 06,2023
设计合成一系列用于治疗胃癌的多靶点受体酪氨酸激酶抑制剂,并进行生物学评价。其中药代动力学分析通过美迪西进行
Gastric cancer is the second most lethal cancer across the world. Compounds 8f, inhibits FGFR1 signaling pathways as well as induces cell apoptosis, is a potential agent for the treatment of gastric c
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设计合成一系列用于治疗胃癌的多靶点受体酪氨酸激酶抑制剂,并进行生物学评价。其中药代动力学分析通过美迪西进行
Jul 06,2023
FBPase是与肿瘤和2型糖尿病相关的一个有前景的靶点。化合物W8对FBPase表现出高选择性。W8的药代动力学研究通过美迪西进行
Fructose-1,6-bisphosphatase (FBPase) is a promising target associated with cancer and type 2 diabetes. Compounds W8 and W8k exhibit high selectivity against FBPase and W8 effectively reduces blood glu
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FBPase是与肿瘤和2型糖尿病相关的一个有前景的靶点。化合物W8对FBPase表现出高选择性。W8的药代动力学研究通过美迪西进行
Jul 06,2023
PTX-HSN是一种高效纳米系统,具有较高耐受剂量,可将PTX递送至卵巢癌并增强主动肿瘤靶向性。此研究中所有体内实验均通过美迪西进行
Paclitaxel-loaded hyaluronan solid nanoemulsions (PTX-HSNs) were successfully fabricated for the delivery of PTX to improve ovarian cancer treatment via active tumor targeting. The in vivo #toxicity,
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PTX-HSN是一种高效纳米系统,具有较高耐受剂量,可将PTX递送至卵巢癌并增强主动肿瘤靶向性。此研究中所有体内实验均通过美迪西进行
Jul 06,2023
AD80是一种多激酶抑制剂,在多种肝细胞癌临床前动物模型中具有抗肿瘤活性,AD80在血浆中的含量通过美迪西进行LC-MS/MS测定
Liver cancer is the fourth greatest cause of cancer related mortality. AD80 is a multi-kinase inhibitor with anti-tumoral activity across a variety of hepatocellular carcinoma (HCC) preclinical models
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AD80是一种多激酶抑制剂,在多种肝细胞癌临床前动物模型中具有抗肿瘤活性,AD80在血浆中的含量通过美迪西进行LC-MS/MS测定
Jul 06,2023
免疫检查点阻断疗法改变了癌症治疗的范式,此研究中通过美迪西在23 个同源肿瘤模型中进行了抗PD-1抗体的体内研究
Immune checkpoint blockade therapies have changed the paradigm of cancer therapies. Reseachers performed in vivo screening for anti-PD-1 therapy across 23 syngeneic tumor models and found th
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免疫检查点阻断疗法改变了癌症治疗的范式,此研究中通过美迪西在23 个同源肿瘤模型中进行了抗PD-1抗体的体内研究
Jul 05,2023
研究人员设计合成STAT3和HDAC双通路抑制剂用于治疗实体肿瘤,PK实验通过美迪西进行
The inhibition of HDACs will lead to compensated activation of a notorious cancer-related drug target, STAT3, in breast cancer through a cascade, which probably limits the anti-proliferation effect of
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研究人员设计合成STAT3和HDAC双通路抑制剂用于治疗实体肿瘤,PK实验通过美迪西进行
Jul 05,2023
研究人员设计并合成了一种光笼PI3K抑制剂1,它可以通过紫外线照射激活,释放出高效PI3K抑制剂2。化合物1和2的ADME研究通过美迪西进行
Aberrant activation of the PI3K pathway has been intensively targeted for cancer therapeutics for decades.  In this work, researchers designed and synthesized a novel photocaged PI3K inhibitor 1,
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研究人员设计并合成了一种光笼PI3K抑制剂1,它可以通过紫外线照射激活,释放出高效PI3K抑制剂2。化合物1和2的ADME研究通过美迪西进行
Jul 05,2023
合成具有体内抗肿瘤活性的强效PD-L1抑制剂,并进行生物学评价和机制研究。PK研究通过美迪西进行
PD-1 and PD-L1 have been very successful for the treatment of various tumors, including NSCLC, urothelial cancer, melanoma, head and neck squamous cell cancer, and lymphoma. Researchers identified com
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合成具有体内抗肿瘤活性的强效PD-L1抑制剂,并进行生物学评价和机制研究。PK研究通过美迪西进行
Jul 05,2023
苯并咪唑衍生物XY123是一种口服有效的选择性RORγ反向激动剂。在本研究中,所有肝微粒体测定均通过美迪西进行
Receptor-related orphan receptor γ (RORγ) has emerged as an attractive therapeutic target for the treatment of cancer and inflammatory diseases. XY123 potently inhibits the RORγ transcription activity
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苯并咪唑衍生物XY123是一种口服有效的选择性RORγ反向激动剂。在本研究中,所有肝微粒体测定均通过美迪西进行
Jul 05,2023
端锚聚合酶1/2影响WNT/β-连环蛋白和Hippo信号通路,这些信号通路涉及包括肿瘤在内的多种疾病
Tankyrase 1 and 2 (TNKS1/2) impact the WNT/β-catenin and Hippo signaling pathways that are involved in numerous human disease conditions including cancer. OM-153 shows picomolar IC50 inhibition in a c
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端锚聚合酶1/2影响WNT/β-连环蛋白和Hippo信号通路,这些信号通路涉及包括肿瘤在内的多种疾病
Jul 05,2023
设计合成和评估用于治疗前列腺癌的CBP溴结构域抑制剂。PK评估、肝微粒体稳定性测定和Caco-2渗透性测定通过美迪西进行
Prostate cancer (PCa) is one of the most commonly diagnosed cancers and the leading cause of cancer mortalities in men. CREB (cyclic-AMP responsive element binding protein) binding protein (CBP) is a
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设计合成和评估用于治疗前列腺癌的CBP溴结构域抑制剂。PK评估、肝微粒体稳定性测定和Caco-2渗透性测定通过美迪西进行
Jul 05,2023
研究人员开发了一种高特异性的CDC7抑制剂TAK-931作为临床肿瘤治疗剂,抗肿瘤药效研究通过美迪西进行
Cell division cycle 7 (CDC7) plays important roles in DNA replication. Researchers developed a highly specific CDC7 inhibitor, TAK-931, as a clinical cancer therapeutic agent. The antitumor efficacy s
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研究人员开发了一种高特异性的CDC7抑制剂TAK-931作为临床肿瘤治疗剂,抗肿瘤药效研究通过美迪西进行
Jul 05,2023
合成一类新型选择性TNIK抑制剂并评估其抗结直肠癌作用,PK研究通过美迪西进行
The Traf2- and Nck-interacting protein kinase (TNIK) is a downstream signal protein of the Wnt/β-catenin pathway and has been thought of as a potential target for the treatment of colorectal cancer.
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合成一类新型选择性TNIK抑制剂并评估其抗结直肠癌作用,PK研究通过美迪西进行
Jul 05,2023
选择性小分子c-Myc降解剂可有效消退c-Myc过表达的肿瘤,表面等离子共振 (SPR) 实验通过美迪西进行
Cancer is one of the leading causes of death worldwide. MYC oncogene is involved in the majority of human cancers and is often associated with poor outcomes. WBC100, a novel oral active molecule glue
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选择性小分子c-Myc降解剂可有效消退c-Myc过表达的肿瘤,表面等离子共振 (SPR) 实验通过美迪西进行
Jun 28,2023
设计合成一系列DHODH抑制剂作为潜在的类风湿性关节炎治疗药物,PK研究通过美迪西进行
Human dihydroorotate dehydrogenase (DHODH) is a viable target for the development of therapeutics to treat cancer and immunological diseases. Herein, researchers designed and synthesized a series of acrylamide-based novel DHODH inhibitors as potential rhe
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设计合成一系列DHODH抑制剂作为潜在的类风湿性关节炎治疗药物,PK研究通过美迪西进行
Jun 28,2023
放射疗法用作肺癌的主要治疗方法,在次研究中建立抗电离辐射肺癌细胞系的放射治疗通过美迪西进行
Radiation therapy is used as the primary treatment for lung cancer. In this study, radiation therapy for establish ionizing radiation-resistant lung cancer cell lines (A549-IR/H1299-IR) was supported by Medicilon.
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放射疗法用作肺癌的主要治疗方法,在次研究中建立抗电离辐射肺癌细胞系的放射治疗通过美迪西进行
Jun 28,2023
设计合成一种新型选择性的口服有效苏氨酸酪氨酸激酶 (TTK) 抑制剂,PK研究均通过美迪西进行
TTK inhibition is an attractive wide-spectrum strategy for cancer therapy. Researchers designed and synthesized a series of pyrido[2, 3-d]pyrimidin-7(8H)-ones as new selective orally bioavailable TTK inhibitors. All the pharmacokinetic studies were carrie
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设计合成一种新型选择性的口服有效苏氨酸酪氨酸激酶 (TTK) 抑制剂,PK研究均通过美迪西进行