Angiogenesis
Angiogenesis is the formation and remodelling of new blood vessels and capillaries from growth of pre-existing blood vessels. It normally occurs during wound healing and embryonic development, but is also required for tumour growth and metastasis in cancer.
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FGFR 抑制剂
BGJ398 (NVP-BGJ398)是一种有效的选择性抑制剂，具有成纤维细胞生长因子受体（FGFR）酪氨酸激酶1、2、3和4的潜在抗血管生成和抗肿瘤活性（对于FGFR1，FGFR2，FGFR3，IC50值为0.9、1.4、1.0和60 nM， 和FGFR4）。
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- Takehito Yamamoto, .et al. Chemosensitivity of Patient-Derived Cancer Stem Cells Identifies Colorectal Cancer Patients with Potential Benefit from FGFR Inhibitor Therapy, Cancers (Basel), 2020, Jul 22;12(8):E2010 PMID: 32708005
- Daniel Limonta, .et al. Fibroblast growth factor 2 enhances Zika virus infection in human fetal brain, J Infect Dis, 2019, 2019 PMID: 30799482
- Li Li, .et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1, Leukemia Res, 2019, 78:12-20 PMID: 30660961
- Anil Kumar, .et al. Human Sertoli cells support high levels of Zika virus replication and persistence, Sci Rep, 2018, 8: 5477 PMID: 29615760
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VEGFR 抑制剂
Pazopanib (GW-786034)是VEGFR-1，VEGFR-2，VEGFR-3，PDGFR-a/β和c-kit的有效且选择性的多靶点酪氨酸激酶抑制剂，可阻止肿瘤生长并抑制血管生成。
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- Koide H, .et al. Substrate-dependent effects of molecular-targeted anticancer agents on activity of organic anion transporting polypeptide 1B1, Xenobiotica, 2018, Oct;48(10):1059-1071 PMID: 29034773
- Ellawatty WEA, .et al. Organic cation transporter 1 is responsible for hepatocellular uptake of the tyrosine kinase inhibitor pazopanib, Drug Metab Dispos, 2018, Jan;46(1):33-40 PMID: 29089306
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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FGFR 抑制剂
AZD4547是一种有效，选择性和口服活性的pan-FGFR抑制剂，对于FGFR1、2、3和4的IC50分别为0.2、2.5、1.8和165 nM。
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- Ryuma Tokunaga, .et al. Fibroblast growth factor receptor 2 expression, but not its genetic amplification, is associated with tumor growth and worse survival in esophagogastric junction adenocarcinoma, Oncotarget, 2016, Apr 12; 7(15): 19748-19761 PMID: 26933914
- Mitsuko Kawano, .et al. FGF18 signaling in the hair cycle resting phase determines radioresistance of hair follicles by arresting hair cycling, Adv Radiat Oncol, 2016, Jul-Sep; 1(3): 170-181 PMID: 28740887
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RTK 抑制剂
Nintedanib esylate是多种受体酪氨酸激酶（RTK）和非受体酪氨酸激酶（nRTK）的有效抑制剂。
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- Thibaut Fourniols, .et al. Inhibition of Colorectal Cancer-Associated Fibroblasts by Lipid Nanocapsules Loaded With Acriflavine or Paclitaxel, Int J Pharm, 2020, Jun 30;584:119337 PMID: 32371002
- Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298
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RTK 抑制剂
Dovitinib是一种小分子多靶点酪氨酸激酶抑制剂，可抑制通过ZNF198-FGFR1或BCR-FGFR1转化为IL3独立性的Ba / F3细胞，IC50值分别为150 nM和90 nM。
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- Yunping Hu, .et al. FGFR1/MAPK-directed brachyury activation drives PD-L1-mediated immune evasion to promote lung cancer progression, Cancer Lett, 2022, Oct 28;547:215867 PMID: 35985510
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Aurora 抑制剂
Danusertib (PHA-739358)是Aurora A/B/C的Aurora激酶抑制剂，在无细胞分析中的IC50为13 nM/79nM/61 nM，对Abl，TrkA，c-RET和FGFR1以及更低的浓度具有中等效力 对Lck，VEGFR2/3，c-Kit，CDK2等有效。
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VEGFR 抑制剂
Bibf1120 (Nintedanib)是一种新型的三联血管激酶抑制剂，可同时抑制三种生长因子受体：VEGFR，PDGF和FGFR。
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- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Chun-Jung Chang, .et al. Overcoming interferon (IFN)-γ resistance ameliorates transforming growth factor (TGF)-β-mediated lung fibroblast-to-myofibroblast transition and bleomycin-induced pulmonary fibrosis, Biochem Pharmacol, 2021, Jan;183:114356 PMID: 33285108
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FGFR1/VEGFR2 抑制剂
PD173074是有效的，细胞可渗透的和ATP竞争性的FGFR和VEGFR抑制剂。
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- Cheryl Q.E. Lee, .et al. What Is Trophoblast? A Combination of Criteria Define Human First-Trimester Trophoblast, Stem Cell Reports, 2016, Feb 9; 6(2): 257-272 PMID: 26862703
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PDFGRβ 抑制剂
TSU-68 (Orantinib,SU6668)在无细胞试验中具有8 nM的Ki对PDGFR自磷酸化的最大效力，但也强烈抑制Flk-1和FGFR1反磷酸化，对IGF-1R，Met，Src， Lck，Zap70，Abl和CDK2； 不抑制EGFR。
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- Aaron Y. Lai, .et al. Venular degeneration leads to vascular dysfunction in a transgenic model of Alzheimer's disease., Brain, 2015, Apr;138(Pt 4):1046-58 PMID: 25688079
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VEGFR-2 抑制剂
Brivanib (BMS-540215)是一种VEGFR-2抑制剂，IC50为25 nM，Ki为26 nM。
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- Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
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VEGFR/PDGFR/FGFR 抑制剂
Pazopanib HCl (GW786034)是VEGFR-1，VEGFR-2，VEGFR-3，PDGFR-a/β和c-kit的有效且选择性的多靶点酪氨酸激酶抑制剂，可阻止肿瘤生长并抑制血管生成。
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- Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Hideharu Yamada, .et al. lncRNA HAR1B has potential to be a predictive marker for pazopanib therapy in patients with sarcoma, Oncol Lett, 2021, Jun;21(6):455 PMID: 33907565
- Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298
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Irreversible FGFR 抑制剂
FIIN-3是一种有效的，选择性的，不可逆的下一代共价FGFR抑制剂。
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VEGFR 抑制剂
Brivanib alaninate (BMS-582664)是VEGFR和FGFR信号转导的双重酪氨酸激酶抑制剂。
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FLT3/FGFR/Bcr-Abl/Aurora 抑制剂
KW-2449是FLT3、ABl、ABl-T315I和Aurora激酶的多激酶抑制剂。
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RTK 抑制剂
Dovitinib是一种小分子多靶点酪氨酸激酶抑制剂，可抑制通过ZNF198-FGFR1或BCR-FGFR1转化为IL3独立性的Ba / F3细胞，IC50值分别为150 nM和90 nM。
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c-Met 抑制剂
MK-2461是一种新型的多靶点激酶抑制剂，优先抑制活化的c-Met受体。
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FGFR/VEGFR2 抑制剂
LY2874455是一种新型有效的FGFR / VEGFR抑制剂。
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IGF-1R, Aurora, FGFR, ABL, SRC 抑制剂
XL228是靶向IGF1R，AURORA激酶，FGFR1-3，ABL和SRC家族激酶的蛋白激酶抑制剂。XL228是一种Aurora A抑制剂（IC50，f3 nmol/L），对ABL1（Ki，5 nmol/L）以及BCR-ABL1 T315I（Ki，1.4 nmol/L）激酶显示出有效的生化活性。
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Chk2, KDR, FGFR, Aurora A & Cdk2 抑制剂
R1530是吡唑并苯并二氮杂小分子，具有潜在的抗血管生成和抗肿瘤活性。R1530也是一种有丝分裂-血管生成抑制剂(MAI),可抑制多种参与血管生成的受体酪氨酸激酶，如血管内皮生长因子受体(VEGFR)-1，-2，-3，血小板衍生生长因子受体(PDGFR)βFMS样酪氨酸激酶(Flt)-3和成纤维细胞生长因子受体(FGFR) -1，-2。
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FGFR1 抑制剂
SSR128129E是一种口服活性变构FGFR1抑制剂，IC50为1.9 uM。
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FGFR1/2/3 抑制剂
Debio-1347 (CH5183284)是成纤维细胞生长因子受体亚型1（FGFR-1），2（FGFR-2）和3（FGFR-3）的生物利用抑制剂，具有潜在的抗肿瘤活性。
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FGFR1 抑制剂
ACTB-1003是一种口服激酶抑制剂，靶向癌症突变（FGFR抑制），血管生成（抑制VEGFR2和Tie-2）并诱导凋亡（靶向PI3激酶下游的RSK和p70S6K。
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VEGFR/FGFR 抑制剂
E-3810是一种有效且选择性的VEGF和FGF受体双重抑制剂，对VEGFR-1，VEGFR-2，VEGFR-3，FGFR-1和VEGF的IC50值分别为7nM，25nM，10nM，17.5nM和82.5nM。FGFR-2。
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FGFR 抑制剂
NVP-BGJ398 phosphate是一种新型的选择性泛特异性FGFR抑制剂，对FGFR1，FGFR2和FGFR3的IC50分别为0.9、1.4和1 nM。与FGFR4和VEGFR2相比，对FGFR具有40倍以上的选择性，并且对Abl，Fyn，Kit，Lck，Lyn和Yes的活性很小。
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FGFR 抑制剂
BLU9931是第一种选择性的FGFR4小分子抑制剂，IC50为3 nM。对FGFR1/2/3的效力较低（IC50> 150 nM）。
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FGFR 抑制剂
FIIN-2是FGFR1-4的不可逆抑制剂，IC50值分别为3.1、4.3、27和45 nM。
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FGFR2 抑制剂
Alofanib (RPT835)是FGFR2的强效选择性变构抑制剂，具有潜在的抗癌活性。
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FGFR 抑制剂
Erdafitinib (JNJ-42756493)是一种有效且选择性的口服生物利用型泛成纤维细胞生长因子受体（FGFR）抑制剂，具有潜在的抗肿瘤活性。
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FGFR4 抑制剂
FGFR4-IN-1是有效的FGFR4抑制剂，IC50为0.7 nM。
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FGFR4 抑制剂
H3B-6527是一种高度选择性的FGFR4抑制剂，在FGF19扩增的细胞系和小鼠中具有强大的抗肿瘤活性。
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FGFR 抑制剂
Derazantinib (ARQ-087)是成纤维细胞生长因子受体（FGFR）的口服生物利用抑制剂，对于FGFR2的IC50值为1.8 nM，对于FGFR1和3的IC50值为4.5 nM，对FGFR4的效力较低（IC50 = 34 nM）。它还抑制RET，DDR2，PDGFRβ，VEGFR和KIT。
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FGFR 抑制剂
Rogaratinib，也称为BAY-1163877，是一种异常的成纤维细胞生长因子受体（FGFR）抑制剂。
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FGFR 抑制剂
PD166866是FGFR1抑制剂，IC50值为55 nM，对c-Src，PDGFR-b，EGFR或胰岛素受体酪氨酸激酶或MEK，PKC和CDK4无影响。
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FGFR1/DDR2 inhibitor
FGFR1/DDR2 inhibitor 1 is an inhibitor of fibroblast growth factor receptor 1 (FGFR1) and discoindin domain receptor 2 (DDR2), with IC50 values of 31.1 nM, 108.4 nM and 3.2 nM for FGFR1, KG-1, and DDR2, respectively.
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FGFR4 inhibitor
Roblitinib (FGF-401; Compound Example 83) is a highly selective and potent FGFR4 inhibitor with an IC50 of 1.9 nM. Roblitinib has antitumor activity.
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FGFR/VEGFR 抑制剂
ODM-203 is a potent FGFR and VEGFR families inhibitor with IC50s of 11, 16, 6, 35 nM towards recombinant FGFR1, FGFR2, FGFR3 and FGFR4 as well as 26, 9, 5 nM towards VEGFR1, VEGFR2 and VEGFR3, respectively.
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MET, AXL/MER, and FGFR1/2/3 inhibitor
S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3 with IC50 values below 20 nM.
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FGFR3 inhibitor
Dovitinib(CHIR-258; TKI258) lactate is a potent inhibitor of fibroblast growth factor receptor 3 (FGFR3) with an IC50 of 5 nM.
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Raf 抑制剂
Sorafenib Tosylate (Nexavar)是几种酪氨酸蛋白激酶(VEGFR和PDGFR)和RAF/MEK/ERK级联抑制剂的新型小分子抑制剂，Raf-1，wt BRAF和V599E突变型BRAF的IC50为6、22、38 nM。
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- Paula Sagmeister, .et al. Comparative Response of HCC Cells to TKIs: Modified in vitro Testing and Descriptive Expression Analysis, J Hepatocell Carcinoma, 2022, Jul 9;9:595-607 PMID: 35845819
- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Jindal A, .et al. Milciclib and sorafenib synergistically downregulate c-Myc to suppress tumor growth in an orthotopic murine model of human hepatocellular carcinoma, J Transl Sci, 2020, 7: 1-10
- Mariko Fujisawa, .et al. Involvement of the Interferon Signaling Pathways in Pancreatic Cancer Cells, Anticancer Res, 2020, 40: 4445-4455 PMID: 32727774
- Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298
- Fangyuan Lai, .et al. Platelet-rich plasma enhances the proliferation of human adipose stem cells through multiple signaling pathways, Stem Cell Res Ther, 2018, 9: 107 PMID: 29661222
- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
- Arum Park, .et al. Identification of Transcription Factor YY1 as a Regulator of a Prostate Cancer-Specific Pathway Using Proteomic Analysis, J Cancer, 2017, 8(12): 2303-2311 PMID: 28819434
- Cong Li, .et al. AMG 925 is a dual FLT3/CDK4 inhibitor with the potential to overcome FLT3 inhibitor resistance in acute myeloid leukemia., Mol Cancer Ther., 2015, Feb;14(2):375-83. PMID: 25487917
- Zhihong Li, .et al. Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3, J Med Chem, 2014, Apr 24;57(8):3430-49 PMID: 24641103
- Hideki Yamaguchi, .et al. Saracatinib impairs the peritoneal dissemination of diffuse-type gastric carcinoma cells resistant to Met and fibroblast growth factor receptor inhibitors, Cancer Sci, 2014, 105(5): 528-536 PMID: 24612061
- Yaping Zhang, .et al. FLT3 and CDK4/6 inhibitors: Signaling mechanisms and tumor burden in subcutaneous and orthotopic mouse models of acute myeloid leukemia, J Pharmacokinet Pharmacodyn., 2014, 41(6): 675-691 PMID: 25326874
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VEGFR 抑制剂
Tivozanib (AV-951)是一种口服VEGF受体酪氨酸激酶抑制剂，旨在抑制所有三种VEGF受体。
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- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298
- Majid Momeny, .et al. Anti-tumour activity of tivozanib, a pan-inhibitor of VEGF receptors, in therapy-resistant ovarian carcinoma cells, Sci Rep, 2017, 7: 45954 PMID: 28383032
- Majid Momeny, .et al. Blockade of vascular endothelial growth factor receptors by tivozanib has potential anti-tumour effects on human glioblastoma cells, Sci Rep, 2017, 7: 44075 PMID: 28287096
- Nicholas A. Manieri, .et al. Mucosally transplanted mesenchymal stem cells stimulate intestinal healing by promoting angiogenesis, J Clin Invest, 2015, Sep 1; 125(9): 3606-3618 PMID: 26280574
- Usui T, .et al. Brain-derived neurotrophic factor promotes angiogenic tube formation through generation of oxidative stress in human vascular endothelial cells., Acta Physiol (Oxf), 2014, 211, 385-394 PMID: 24612679
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VEGFR 抑制剂
Regorafenib (BAY 73-4506)是一种多激酶抑制剂，IC50为17、40和69 nM c-KIT，VEGFR2，B-Raf。Regorafenib（BAY 73-4506）是一种针对肿瘤及其脉管系统的口服生物利用型多激酶抑制剂。
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- Paula Sagmeister, .et al. Comparative Response of HCC Cells to TKIs: Modified in vitro Testing and Descriptive Expression Analysis, J Hepatocell Carcinoma, 2022, Jul 9;9:595-607 PMID: 35845819
- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Jindal A, .et al. Milciclib and sorafenib synergistically downregulate c-Myc to suppress tumor growth in an orthotopic murine model of human hepatocellular carcinoma, J Transl Sci, 2020, 7: 1-10
- Makoto Koyama, .et al. Low-dose trametinib and Bcl-xL antagonist have a specific antitumor effect in KRAS-mutated colorectal cancer cells, Int J Oncol, 2020, Sep 2 PMID: 32901840
- Mariko Fujisawa, .et al. Involvement of the Interferon Signaling Pathways in Pancreatic Cancer Cells, Anticancer Res, 2020, 40: 4445-4455 PMID: 32727774
- Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298
- Sunil Kumar Yadava, .et al. Low Temperature, Easy Scaling Up Method for Development of Smart Nanostructure Hybrid Lipid Capsules for Drug Delivery Application, Colloids Surf B Biointerfaces, 2020, Mar 2;190:110927 PMID: 32169777
- Takeshi Uenaka, .et al. In silico drug screening by using genome-wide association study data repurposed dabrafenib, an anti-melanoma drug, for Parkinson's disease, Hum Mol Genet, 2018, Nov 15; 27(22): 3974-3985 PMID: 30137437
- Yi Xu, .et al. Knockdown of delta-5-desaturase promotes the anti-cancer activity of dihomo-γ-linolenic acid and enhances the efficacy of chemotherapy in colon cancer cells expressing COX-2, Free Radic Biol Med, 2016, Jul; 96: 67-77 PMID: 27101738
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PDGFR 抑制剂
Imatinib (Gleevec)是一种多靶点酪氨酸激酶抑制剂，抑制v-Abl、c-Kit和PDGFR的IC50分别为0.6，0.1和0.1 μM。
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- Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Takafumi Shima, .et al. Glucose transporter-1 inhibition overcomes imatinib resistance in gastrointestinal stromal tumor cells, Oncol Rep, 2022, 47: 7 PMID: 34738628
- Reiko Watanabe, .et al. Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration, J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- BM Duggan, .et al. RIPK2 Dictates Insulin Responses to Tyrosine Kinase Inhibitors in Obese Male Mice, Endocrinology, 2020, May 30;bqaa086 PMID: 32473019
- Li Li, .et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1, Leukemia Res, 2019, 78:12-20 PMID: 30660961
- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
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RTK inhibitor
Sunitinib Malate是一种多靶点RTK抑制剂，作用于VEGFR2 (Flk-1)和 PDGFRβ，也会抑制c-Kit的活性。用于治疗肾细胞癌（RCC）和伊马替尼耐药的胃肠道间质瘤（GIST）。
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- Rachel K Toth, .et al. Stabilization of PIM Kinases in Hypoxia Is Mediated by the Deubiquitinase USP28, Cells, 2022, Mar 16;11(6):1006 PMID: 35326457
- Reiko Watanabe, .et al. Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration, J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Thibaut Fourniols, .et al. Inhibition of Colorectal Cancer-Associated Fibroblasts by Lipid Nanocapsules Loaded With Acriflavine or Paclitaxel, Int J Pharm, 2020, Jun 30;584:119337 PMID: 32371002
- Li Li, .et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1, Leukemia Res, 2019, 78:12-20 PMID: 30660961
- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
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VEGFR 抑制剂
Axitinib是一种小分子酪氨酸激酶抑制剂，可抑制多种靶标，包括VEGFR-1，VEGFR-2，VEGFR-3，血小板衍生生长因子受体（PDGFR）和cKIT（CD117）。
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- Youcef M. Rustum, .et al. Non-Coding Micro RNAs and Hypoxia-Inducible Factors Are Selenium Targets for Development of a Mechanism-Based Combination Strategy in Clear-Cell Renal Cell Carcinoma-Bench-to-Bedside Therapy, Int J Mol Sci, 2018, Nov; 19(11): 3378 PMID: 30380599
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PDGFRα/β 抑制剂
CP 673451是一种有效的PDGFR-β抑制剂，IC50为1 nM。
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- Kaori Aoto, .et al. Complex formation between platelet-derived growth factor receptor β and transforming growth factor β receptor regulates the differentiation of mesenchymal stem cells into cancer-associated fibroblasts, Oncotarget, 2018, Sep 25; 9(75): 34090-34102 PMID: 30344924
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KIT/PDGFR 抑制剂
Masitinib mesylate是Kit和PDGFRα/β的新型抑制剂，IC50为200 nM和540 nM/800 nM，对ABL和c-Fms的抑制作用较弱。
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- Julia M Harrison, .et al. Muscle fiber-type specific terminal Schwann cell pathology leads to sprouting deficits following partial denervation in SOD1 G93A mice, Neurobiol Dis, 2020, Aug 20;145:105052 PMID: 32827689
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c-Kit 抑制剂
Masitinib (AB1010)是一种蛋白质酪氨酸激酶抑制剂。
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PDGFR/FLT3 抑制剂
Crenolanib (CP-868596)是口服生物可用的PDGFR酪氨酸激酶的选择性小分子抑制剂，在皮摩尔浓度下抑制PDGFRA和PDGFRB。
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- N Naganna, .et al. Amino alkynylisoquinoline and alkynylnaphthyridine compounds potently inhibit acute myeloid leukemia proliferation in mice, EBioMedicine, 2019, Jan 24. pii: S2352-3964(19)30012-X PMID: 30686755
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VEGFR/PDGFR 抑制剂
Linifanib (ABT-869)是一种结构新颖的有效RTK，VEGF和PDGF抑制剂，对人内皮细胞，PDGFR-β，KDR和CSF-1R的IC50分别为0.2、2、4和7 nM。
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- Li Li, .et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1, Leukemia Res, 2019, 78:12-20 PMID: 30660961
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Bcr-Abl 抑制剂
Imatinib mesylate是一种选择性酪氨酸激酶抑制剂，通过抑制KIT信号转导途径，在治疗胃肠间质瘤中诱导了持续的客观反应。
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- Inge Govaerts, .et al. PSEN1-selective gamma-secretase inhibition in combination with kinase or XPO-1 inhibitors effectively targets T cell acute lymphoblastic leukemia, J Hematol Oncol, 2021, 14: 97 PMID: 34167562
- Genevra Kuziel, .et al. Stromal CCL2 Signaling Promotes Mammary Tumor Fibrosis through Recruitment of Myeloid-Lineage Cells, Cancers (Basel), 2020, Jul 28;12(8):E2083 PMID: 32731354
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