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搜索结果包含 Cancer Cell 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
氯磺丙脲对蠕虫和人肺成纤维细胞MRC-5细胞具有抗衰老作用,氯磺丙脲在小鼠中的生物利用度测定通过美迪西进行
Sulfonylureas exert their anti-diabetic effects by inhibiting K-ATP channels in the plasma membrane of islet β-cells. Chlorpropamide acts on complex II directly or indirectly via mitoK-ATP to produce
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氯磺丙脲对蠕虫和人肺成纤维细胞MRC-5细胞具有抗衰老作用,氯磺丙脲在小鼠中的生物利用度测定通过美迪西进行
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 06,2023
SKLB-YTH-60可改善博来霉素诱导的肺纤维化小鼠模型中的炎症和纤维化,YTH-60的体内药代动力学研究通过美迪西进行
Idiopathic pulmonary fibrosis is a chronic and lethal lung disease associated with fibroblast activation, myoblast proliferation and extracellular matrix deposition. SKLB-YTH-60 was developed through
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SKLB-YTH-60可改善博来霉素诱导的肺纤维化小鼠模型中的炎症和纤维化,YTH-60的体内药代动力学研究通过美迪西进行
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
阿帕替尼通过VEGFR2通路抑制紫杉醇对胃癌细胞的耐药性
Overexpression of VEGFR2 can offset the rescue effect of Apatinib on Paclitaxel-induced drug resistance of MGC803 cells. Apatinib inhibits Paclitaxel resistance of MGC803 cells via the VEGFR2 #signali
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阿帕替尼通过VEGFR2通路抑制紫杉醇对胃癌细胞的耐药性
Jul 05,2023
研究人员报告了一种具有细胞渗透性的选择性METTL3纳摩尔抑制剂UZH1a,作者感谢美迪西合成了UZH1a和UZH1b
The methylase METTL3 is the writer enzyme of the N6‐methyladenosine (m6A) modification of RNA.Here researchers report a nanomolar inhibitor of METTL3 (UZH1a) which is selective and cell‐permeable, whi
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研究人员报告了一种具有细胞渗透性的选择性METTL3纳摩尔抑制剂UZH1a,作者感谢美迪西合成了UZH1a和UZH1b
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
RIPK2激酶参与多种慢性炎症,UH15-15抑制RIPK2激酶并具有良好的体外ADME和PK特性,PK研究通过美迪西进行
Receptor interacting protein kinase-2 (#RIPK2) is an enzyme involved in the transduction of pro-inflammatory nucleotide-binding oligomerization domain cell signaling, a pathway implicated in numerous
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RIPK2激酶参与多种慢性炎症,UH15-15抑制RIPK2激酶并具有良好的体外ADME和PK特性,PK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
zapERtrap:光调节的内质网释放系统揭示了意想不到的神经元运输途径,Zapalog的合成通过美迪西进行
zapERtrap opens the door to previously unapproachable questions concerning how proteins are processed, trafficked, and secreted in space and time in complex cellular environments. zapERtrap relies on
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zapERtrap:光调节的内质网释放系统揭示了意想不到的神经元运输途径,Zapalog的合成通过美迪西进行
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
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