“Tutalthromycin second gen”的搜索结果
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Ferroptosis inhibitor
RSL3 is a ferroptosis activator in a VDAC-independent manner,exhibiting selectivity for tumor cells bearing oncogenic RAS.
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- Sampilvanjil A, .et al. Cigarette smoke extract induces ferroptosis in vascular smooth muscle cells, Am J Physiol Heart Circ Physiol, 2020, Mar 1;318(3):H508-H518 PMID: 31975626
- Fujiki K, .et al. Blockade of ALK4/5 signaling suppresses cadmium- and erastin-induced cell death in renal proximal tubular epithelial cells via distinct signaling mechanisms, Cell Death Differ, 2019, Feb 25 PMID: 30804470
- Samantha W. Alvarez, .et al. NFS1 undergoes positive selection in lung tumours and protects cells from ferroptosis, Nature, 2017, Nov 30; 551(7682): 639-643 PMID: 29168506
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Glucosylceramide synthase 抑制剂
Eliglustat是葡萄糖神经酰胺合成酶的一种特异而有效的抑制剂。
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GL1 synthase 抑制剂
Genz-123346 free base是GL1合酶的抑制剂，可阻止神经酰胺向GL1的转化。抑制GM1的IC50为14 nM。
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Glucocerebroside synthase 抑制剂
Eliglustat tartrate通常用作酒石酸盐，据信Eliglustat通过抑制葡萄糖基神经酰胺合酶起作用。
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- Zunke F, .et al. Reversible Conformational Conversion of α-Synuclein into Toxic Assemblies by Glucosylceramide, Neuron, 2018, Jan 3;97(1):92-107.e10 PMID: 29290548
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Smad 抑制剂
Kartogenin能有效诱导人骨髓间充质干细胞分化为软骨细胞。
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Lck 抑制剂
AMG-47a是口服有效的Lck和T细胞增殖抑制剂。它在抗CD3诱导的小鼠IL-2产生中表现出抗炎活性（ED50 11 mg/kg）。
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topoisomerase 1 抑制剂
GENZ-644282是拓扑异构酶I的非喜树碱抑制剂，具有潜在的抗肿瘤活性。
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Dihydroorotate Dehydrogenase 抑制剂
Brequinar是二氢乳清酸脱氢酶的抑制剂，二氢乳清酸脱氢酶是从头进行嘧啶生物合成的酶。
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Androgen Receptor 抑制剂
Apalutamide (ARN-509)是一种具有潜在抗肿瘤活性的雄激素受体拮抗剂，IC50 为 16 nM。ARN-509与靶组织中的AR结合，从而阻止了雄激素诱导的受体激活，并促进了无法转运至细胞核的无活性复合物的形成。这防止了AR应答基因的结合和转录。
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- Frédérique Mittler, .et al. High-Content Monitoring of Drug Effects in a 3D Spheroid Model, Front Oncol, 2017, 7: 293 PMID: 29322028
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Dehydrogenase 抑制剂
CPI-613是合成的α-硫辛酸硫辛酸类似物的对映异构体的外消旋混合物，具有潜在的化学预防和抗肿瘤活性。
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- Takuji Sakuratani, .et al. Downregulation of ARID1A in gastric cancer cells: a putative protective molecular mechanism against the Harakiri-mediated apoptosis pathway, Virchows Arch, 2020, Aug 13 PMID: 32789692
- Egawa Y, .et al. Therapeutic potential of CPI-613 for targeting tumorous mitochondrial energy metabolism and inhibiting autophagy in clear cell sarcoma, PLoS One, 2018, Jun 7;13(6):e0198940 PMID: 29879220
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Hydrogen peroxide 抑制剂
Acetanilide在过氧化氢中用作抑制剂，并用于稳定纤维素酯清漆。
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dehydrogenase inhibitor
Gossypol是一种多酚醛，渗透细胞并作为几种脱氢酶的抑制剂。
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- Amy L. Farthing, .et al. Response of northern bobwhites fed single doses of gossypol, Wildlife Society Bulletin, 2018, 42(3):460-466;
- Jin Qu, .et al. Gossypol potentiates carboplatin effects against ovarian cancer, Biomed Res, 2017, 28 (8): 3355-3361
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Protein kinase 抑制剂
Apigenin是中央苯并二氮杂central受体的配体，其Ki为4μM竞争性抑制氟硝西epa的结合，发挥抗焦虑和轻微的镇静作用。
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NLRP3 inflammasome 抑制剂
Isoliquiritigenin是从光果甘草根中分到的黄酮类化合物，具有抗肿瘤的活性。目前正处于试验阶段，用于癌症和可卡因成瘾的辅助治疗的研究。
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DNA Methyltransferase 抑制剂
Decitabine是一种次甲基化剂，它通过抑制DNA甲基转移酶来使DNA次甲基化。
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- Borbala Szabo, .et al. Aspirin mediates its antitumoral effect through inhibiting PTTG1 in pituitary adenoma, J Clin Endocrinol Metab, 2022, Sep 5;dgac496 PMID: 36059148
- Sangni Qian, .et al. Hypermethylation of tumor suppressor lncRNA MEF2C-AS1 frequently happened in patients at all stages of colorectal carcinogenesis, Clin Epigenetics, 2022, Sep 5;14(1):111 PMID: 36064442
- Borb??la Szab??, .et al. Demethylation status of somatic DNA extracted from pituitary neuroendocrine tumors indicates proliferative behavior, J Clin Endocrinol Metab, 2020, Jun 1;105(6):dgaa156 PMID: 32232382
- Bracha Shraibman, .et al. Human Leukocyte Antigen (HLA) Peptides Derived from Tumor Antigens Induced by Inhibition of DNA Methylation for Development of Drug-facilitated Immunotherapy, Mol Cell Proteomics, 2016, Sep; 15(9): 3058-3070 PMID: 27412690
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COX-1 抑制剂
Ibuprofen (Advil)是一种非甾体抗炎药(NSAID)，靶向COX-1，IC50为13 μM。
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- Azuma T, .et al. Distribution of six anticancer drugs and a variety of other pharmaceuticals, and their sorption onto sediments, in an urban Japanese river, Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. Detection of pharmaceuticals and phytochemicals together with their metabolites in hospital effluents in Japan, and their contribution to sewage treatment plant influents, Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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