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ESKM, a novel therapeutic agent for sensitive and resistant PH+ leukemias

Effects of PARP inhibitors in BRCA gene-mutated ovarian cancer

The mechanism of resistance to JAK2 inhibitor in myeloproliferative neoplasms patients

DASATINIB; An inhibitor of Receptor Tyrosine Kinase

GDC-0941, A NOVEL PI3K INHIBITOR

Blog of Signaling Pathways

Enhanced efficacy of 5-fluorouracil in combination with a dual histone deacetylase and phosphatidylinositide 3-kinase inhibitor (CUDC-907) in colorectal cancer cells

364 views | Dec 26 2018

Hamam R et al. revealed, for the first time, the enhanced inhibitory effect of CUDC-907 against CRC cells when combined with 5-FU, supporting the application of this combination as a potential therapeutic strategy in CRC treatment. [Read the Full Post]

CUDC-907 Promotes Bone Marrow Adipocytic Differentiation Through Inhibition of Histone Deacetylase and Regulation of Cell Cycle

409 views | Dec 26 2018

Ali D et al. revealed that HDAC, PI3K, and cell cycle genes are important regulators of BMA formation and demonstrate that adipocyte differentiation of hBMSCs is associated with complex changes in a number of epigenetic and genetic pathways, which can be targeted to regulate BMA formation. [Read the Full Post]

Dabigatran reduces thrombin-induced platelet aggregation and activation in a dose-dependent manner

0 views | Dec 25 2018

Vinholt PJ et al. indicated that dabigatran exclusively inhibits thrombin-induced platelet activation and aggregation with a dose-dependent response. Platelet stimulation with other agonists was not affected by dabigatran. [Read the Full Post]

Structure-activity relationships of nucleoside analogues for inhibition of tick-borne encephalitis virus

149 views | Dec 25 2018

Eyer L et al. indicated that high antiviral activity and low cytotoxicity of C2' methylated or C4' azido substituted pharmacophores suggest that such compounds might represent promising candidates for further development of potential therapeutic agents in treating TBEV infection. [Read the Full Post]

RNA Polymerase I Inhibition with CX-5461 as a Novel Therapeutic Strategy to Target MYC in Multiple Myeloma

166 views | Dec 24 2018

Lee HC et al. provided a rationale for the clinical translation of CX-5461 as a novel therapeutic approach to target MYC in myeloma. [Read the Full Post]

The antibiotic polymyxin B exhibits novel antifungal activity against Fusarium species

0 views | Dec 23 2018

Hsu LH et al. found that PMB was fungicidal against all 12 Fusarium strains, with minimum fungicidal concentrations of 32 µg/mL or 64 µg/mL for most strains tested, as evidenced by broth dilution, methylene blue staining and XTT reduction assays. PMB can reduce the germination rates of conidia, but not chlamydospores, and can cause defects in cell membrane integrity in Fusarium strains. [Read the Full Post]

WIP1 modulates responsiveness to Sonic Hedgehog signaling in neuronal precursor cells and medulloblastoma

0 views | Dec 23 2018

Wen J et al. found that Wip1 knockdown or treatment with a WIP1 inhibitor suppressed the effects of Shh stimulation and potentiated the growth inhibitory effects of SHH pathway-inhibiting drugs in Shh-activated MB cells in vitro. [Read the Full Post]

WNT5A: a motility-promoting factor in Hodgkin lymphoma

244 views | Dec 22 2018

Linke F et al. proposed a model where WNT signaling has an important role in regulating tumor-promoting processes. [Read the Full Post]

Regulation of XIAP Turnover Reveals a Role for USP11 in Promotion of Tumorigenesis

0 views | Dec 22 2018

Zhou Z et al. proposed that aberrant USP11, via stabilization of XIAP, promotes tumor initiation and progression. [Read the Full Post]

Cell-based assay system for high-throughput screening of anti-photo-aging agents in fibroblast transfectants

0 views | Dec 21 2018

Lee S et al. revealed that CCN1-GFs treated with sclareol showed decreased levels of UVB-induced CCN1 expression. [Read the Full Post]

Inhibition of Chk1 with the small molecule inhibitor V158411 induces DNA damage and cell death in an unperturbed S-phase

198 views | Dec 21 2018

Wayne J et al. identified two distinct classes of Chk1 inhibitors: those that induced a strong increase in γH2AX, pChk1 (S317) and pRPA32 (S4/S8) (including V158411, LY2603618 and ARRY-1A) and those that did not (including MK-8776 and GNE-900). [Read the Full Post]

Differential effects of histone deacetylase inhibitors on cellular drug transporters and their implications for using epigenetic modifiers in combination chemotherapy

289 views | Dec 20 2018

Valdez BC et al. further implied the possibility of antagonistic effects when HDAC inhibitors are combined with anthracyclines and other MDR1 drug ligands in chemotherapy. [Read the Full Post]

Dual inhibition of PI3K and mTOR by VS-5584 suppresses thrombus formation

139 views | Dec 19 2018

Später T et al. demonstrated that VS-5584 is a potent inhibitor of primary hemostasis targeting multiple platelet functions. [Read the Full Post]

FBW7 mutations mediate resistance of colorectal cancer to targeted therapies by blocking Mcl-1 degradation

0 views | Dec 19 2018

Tong J et al. demonstrated FBW7 mutational status as a key genetic determinant of CRC response to targeted therapies, and Mcl-1 as an attractive therapeutic target. [Read the Full Post]

Protease-activated receptor-2 promotes kidney tubular epithelial inflammation by inhibiting autophagy via the PI3K/Akt/mTOR signalling pathway

250 views | Dec 18 2018

Du C et al. suggested that PAR2 inhibition may play a role in the treatment of diseases with increased inflammatory responses in renal systems. [Read the Full Post]

PI3K Catalytic Isoform Alteration Promotes the LIMK1-related Metastasis Through the PAK1 or ROCK1/2 Activation in Cigarette Smoke-exposed Ovarian Cancer Cells

0 views | Dec 18 2018

Park GB et al. showed that characterization of the p110 isotypes of PI3K is critical for regulating cancer metastasis; LIMK1 could be a common therapeutic target of ovarian cancer metastasis. [Read the Full Post]

MicroRNA-24-1 suppresses mouse hepatoma cell invasion and metastasis via directly targeting O-GlcNAc transferase

121 views | Dec 17 2018

Liu Y et al. suggested that as a tumor suppressor, miR-24-1 may regulate mouse hepatocarcinoma cells migration and invasion, at least partially through targeting OGT, which could regulate the O-GlcNAcylation and the stability of this oncoprotein c-Myc. This may give insight into a novel mechanism and therapy of tumor lymphatic metastasis. [Read the Full Post]

SIRT1 prevents hyperuricemia via the PGC-1α/PPARγ-ABCG2 pathway

374 views | Dec 17 2018

Wang J et al. demonstrated that SIRT1 and its activator, RSV, have clear anti-hyperuricemia functions in this mouse model. One possible mechanism is the activation of ABCG2 in the ileum through the PGC-1α/PPARγ pathway. [Read the Full Post]

Microengineered cultures containing human hepatic stellate cells and hepatocytes for drug development

170 views | Dec 16 2018

Davidson MD et al. found that NADPH oxidase (NOX) inhibition and farnesoid X receptor (FXR) activation using clinically relevant drugs alleviated hepatic dysfunctions in MPTCs. In conclusion, MPTCs recapitulate symptoms of NASH- and early fibrosis-like dysfunctions in PHHs and have utility for drug discovery in this space. [Read the Full Post]

Spinal Glutamate Transporters Are Involved in the Development of Electroacupuncture Tolerance

231 views | Dec 16 2018

Cui L et al. indicated the participation of the spinal GTs in EAT. [Read the Full Post]

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