Multi-kinase inhibitor
Antitumor activity of the novel multi-kinase inhibitor EC-70124 in triple negative breast cancer
... Disseminated triple negative breast cancer (TNBC) is an incurable disease with limited therapeutic options beyond chemotherapy. Therefore, identification of druggable vulnerabilities is an important aim. Protein kinases ...
15
Pre-clinical characterization of PKC412, a multi-kinase inhibitor, against colorectal cancer cells
... AKT hyper-activity in CRC promotes cancer cell progression [12]. Thus, AKT is an known oncotarget for CRC [12]. Since PKC412 theoretically blocks multiple AKT upstream receptor kinases [8], it is not surprised to see ...
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<p>Lenvatinib, a molecule with versatile application: from preclinical evidence to future development in anti-cancer treatment</p>
... emerging multi-kinase inhibitor with a preferential anti- angiogenic activity, which has shown ef fi cacy in the treatment of renal cell carcinoma, differentiated thyroid cancer and hepatocellular ...
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Characterization of vascular endothelial growth factor's effect on the activation of protein kinase C, its isoforms, and endothelial cell growth
... tyrosine-kinase inhibitor, blocked VEGF-induced PLCg and PKC activity and subsequent cell growth was not surprising since receptors for VEGF are known to be tyrosine ...
10
The novel combination of dual mTOR inhibitor AZD2014 and pan-PIM inhibitor AZD1208 inhibits growth in acute myeloid leukemia via HSF pathway suppression
... serine/threonine kinase signaling takes part in various pathways exerting tumorigenic ...PIM kinase inhibitor with an mTOR inhibitor might have complementary growth- inhibitory effects against ...
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Synergistic activity of vorinostat combined with gefitinib but not with sorafenib in mutant KRAS human non-small cell lung cancers and hepatocarcinoma
... (EGFR)-tyrosine kinase inhibitor (gefitinib) or a multi-targeted kinase inhibitor (sorafenib) in combination with a histone deacetylase inhibitor (vorinostat) on cell ...
13
Danusertib, a potent pan-Aurora kinase and ABL kinase inhibitor, induces cell cycle arrest and programmed cell death and inhibits epithelial to mesenchymal transition involving the PI3K/Akt/mTOR-mediated signaling pathway in human gastric cancer AGS and NCI-N78 cells
... tyrosine kinase inhibitor with potent anticancer effects, but its antitumor effect and underlying mechanisms in the treatment of human gastric cancer are ...cyclin-dependent kinase 1 and upregulation ...
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TARGETING ONCOGENIC KINASE SIGNALING WITH SMALL MOLECULE KINASE INHIBITOR IMATINIB
... CONCLUSION AND PERSPECTIVES: Imatinib mesylate revolutionized the treatment and outcome of chronic myeloid leukemia and certain other cancer types. It is very effective against some types of leukemia that express ...
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Comprehensive kinase profile of pacritinib, a nonmyelosuppressive Janus kinase 2 inhibitor
... In conclusion, pacritinib inhibits a variety of tyrosine kinases (JAK2, JAK2V617F, FLT3) and nontyrosine kinases (CSF1R, IRAK1, tyrosine kinase nonreceptor 1, and ROS1) at low nanomolar levels. Pacritinib ...
9
Transformation of SV40-immortalized human uroepithelial cells by 3-methylcholanthrene increases IFN- and Large T Antigen-induced transcripts
... cyclin-dependent kinase inhibitor; TRICK2A: death receptor 5 or DR5 (also Apo2; TRAIL-R2; TRICK2; or KILLER); IAP3: inhibitor of apoptosis protein 3; HSIAH2: inhibitor of apoptosis protein 2; ...
14
ERK2 phosphorylation of EBNA1 serine 383 residue is important for EBNA1-dependent transactivation
... indicated kinase are as follows: ERK2 (PxS/TP or xxS/TP, CaMK II (RxxS/T), CDK1 (S/TPxR/K), CK1* (SxxS/T), GSK3b* (SxxxS), bold S/T (phosphorylation site), underlined S (prior phosphorylation site needed for ...
9
Raf kinase inhibitor protein1 is a myogenic inhibitor with conserved function in avians and mammals
... Raf Kinase Inhibitor Protein1 (RKIP) is a tumour suppressor that is present in a number of adult ...an inhibitor of both Raf/Mek/Erk and NFĸB signalling when unphosphorylated, but following ...
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Anticancer drug targets: growth factors and growth factor signaling
... The EGF receptor is also the target for the develop- ment of inhibitors of the intracellular tyrosine kinase domain. ZD-1839 and CP-358,774, competitive in- hibitors of ATP binding to the receptor’s active site, ...
6
<p>The Analysis of the Anti-Tumor Mechanism of Ursolic Acid Using Connectively Map Approach in Breast Cancer Cells Line MCF-7</p>
... non-competitive inhibitor of separase, inhibits breast cancer cell growth through decreasing phosphorylation levels of RAF, PLK1, and ...PLK1 inhibitor and tankyr- ase-1 inhibitor could enhance the ...
8
Pim kinase inhibition sensitizes FLT3-ITD acute myeloid leukemia cells to topoisomerase 2 inhibitors through increased DNA damage and oxidative stress
... Pim kinase, Pim-1, Pim-2 and Pim-3, supports the utility of developing pan-Pim kinase inhibitors ...Pim kinase inhibitors have entered clinical trials to ...Pim kinase and FLT3, showed ...
16
Failure to ubiquitinate c Met leads to hyperactivation of mTOR signaling in a mouse model of autosomal dominant polycystic kidney disease
... Autosomal dominant polycystic kidney disease (ADPKD) is a common inherited disorder that is caused by mutations at two loci, polycystin 1 (PKD1) and polycystin 2 (PKD2). It is characterized by the formation of multiple ...
13
Intracellular signaling in the regulation of renal Na K ATPase I Role of cyclic AMP and phospholipase A2
... an inhibitor of adenylate cyclase, completely blocked Na-K-ATPase inhibition by DA or fenoldopam, and IP20, an inhibitor peptide of cAMP-dependent protein kinase A (PKA), abolished the Na:K pump ...
6
Nilotinib: optimal therapy for patients with chronic myeloid leukemia and resistance or intolerance to imatinib
... BCR-ABL inhibitor imatinib mesylate (IM) has improved survival in all phases of CML and is the standard of care for newly diagnosed patients in chronic ...Bcr-Abl kinase domain being amongst the most common ...
14
Next-generation sequencing for BCR-ABL1 kinase domain mutation testing in patients with chronic myeloid leukemia: a position paper
... algorithms for chronic myeloid leukemia (CML) patients who do not achieve an optimal response to tyrosine kinase inhibitors (TKIs). Conventional Sanger sequencing is the method currently recommended to test ...
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A Chemical Biology Platform to Develop Small Molecule Probes for Bromodomains
... XMD11-50 (19) to define the binding modes and to predict how these scaffolds further direct the medicinal chemistry effort around modifying the dual kinase-bromodomain inhibitory activity against either kinases or ...
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