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

The mechanism of resistance to JAK2 inhibitor in myeloproliferative neoplasms patients

Effects of PARP inhibitors in BRCA gene-mutated ovarian cancer

DASATINIB; An inhibitor of Receptor Tyrosine Kinase

GP130/JAK/STAT3 signaling pathway induces multiple myeloma

Blog of Signaling Pathways

Inhibition of BRD4 enhanced the tumor suppression effect of dasatinib in gastric cancer

24 views | May 29 2023

The study suggests that targeting BRD4 in gastric cancer may improve patient prognosis and increase the sensitivity of chemotherapy drugs such as dasatinib. [Read the Full Post]

Inhibition of GSK-3β Enhances Osteoblast Differentiation of Human Mesenchymal Stem Cells through Wnt Signalling Overexpressing Runx2

72 views | May 29 2023

The study demonstrates that 1-Azakenpaullone, a highly selective inhibitor of GSK-3β, effectively induces osteoblastic differentiation and mineralization of human MSCs mediated by the activation of Wnt signaling and upregulation of Runx2, making it a promising osteo-promotor factor for bone tissue engineering. [Read the Full Post]

Aerobic exercise alleviates ventilator-induced lung injury by inhibiting NLRP3 inflammasome activation

93 views | May 29 2023

The study found that exercise can reduce ventilator-induced lung injury by inhibiting PKCɑ and NLRP3 activation. [Read the Full Post]

Temperature sensing by the calcium-sensing receptor

105 views | May 29 2023

The study suggests that CaSRs, a type of GPCR, may contribute to temperature sensing through a mechanism dependent on repetitive phosphorylation and dephosphorylation. [Read the Full Post]

Protective effects of gallic acid and SGK1 inhibitor on oxidative stress and cardiac damage in an isolated heart model of ischemia/reperfusion injury in rats

73 views | May 29 2023

The study suggests that concomitant administration of gallic acid and the SGK1 gene inhibitor GSK650394 may have a more beneficial effect on cardiac ischemia/reperfusion injury than each drug alone. [Read the Full Post]

Technique-Dependent Relationship between Local Ski Bending Curvature, Roll Angle and Radial Force in Alpine Skiing

73 views | May 28 2023

This study analyzed the interplay between ski and snow in skiing technique and performance using a PyzoFlex® ski prototype to measure local ski curvature and found that segmental w″ differed temporally and segmentally depending on the employed technique and turn phase. [Read the Full Post]

Host-Erythrocytic Sphingosine-1-Phosphate Regulates Plasmodium Histone Deacetylase Activity and Exhibits Epigenetic Control over Cell Death and Differentiation

71 views | May 28 2023

The study suggests that altering host S1P levels could dysregulate PfHDAC-1 activity and modulate the transcriptional patterns of genes associated with malaria parasite proliferation and virulence, offering a novel approach to combat malaria resistance to conventional antimalarial drugs. [Read the Full Post]

Repurposing drugs against Alzheimer's disease: can the anti-multiple sclerosis drug fingolimod (FTY720) effectively tackle inflammation processes in AD?

0 views | May 28 2023

Recent studies suggest that the FDA-approved drug fingolimod, which binds to sphingosine-1-phosphate receptors and was originally approved for multiple sclerosis, could potentially reverse synaptic deficits and memory dysfunction in Alzheimer's disease mouse models even when treatment is started after onset of symptoms. [Read the Full Post]

Monitoring recovery after CNS demyelination, a novel tool to de-risk pro-remyelinating strategies

44 views | May 28 2023

The study uses a Xenopus laevis transgenic model of conditional demyelination to test candidate molecules for promoting remyelination, correlating functional and clinical performance measures with histopathological parameters to identify potential therapies. [Read the Full Post]

Protein kinase D1 promotes the survival of random-pattern skin flaps in rats

124 views | May 28 2023

The study demonstrated that PKD1 improves skin flap survival by promoting angiogenesis, reducing oxidative stress, and inhibiting apoptosis and inflammation, suggesting it as a potential therapeutic target for flap failure treatment. [Read the Full Post]

"RB-reactivator screening" as a novel cell-based assay for discoveries of molecular targeting agents including the first-in-class MEK inhibitor trametinib (trade name: Mekinist)

83 views | May 27 2023

The RB-reactivator screening led to the discovery of novel molecular-targeting agents, including trametinib, which was approved as the first-in-class MEK inhibitor and selected as the Drug Discovery of the Year in 2013 by the British Pharmacological Society. [Read the Full Post]

MAPK Inhibition Requires Active RAC1 Signaling to Effectively Improve Iodide Uptake by Thyroid Follicular Cells

77 views | May 27 2023

The present study suggests that potentiating RAC1 activity could enhance the recovery of NIS expression induced through MAPK pathway inhibition, providing new opportunities for therapeutic intervention in refractory differentiated thyroid carcinomas. [Read the Full Post]

Impact of setanaxib on quality of life outcomes in primary biliary cholangitis in a phase 2 randomized controlled trial

147 views | May 27 2023

The study suggests that setanaxib may improve quality of life in patients with PBC, particularly for those with clinically significant fatigue. [Read the Full Post]

Venetoclax resistance induced by activated T cells can be counteracted by sphingosine kinase inhibitors in chronic lymphocytic leukemia

44 views | May 27 2023

The study demonstrates the potential of SPHK inhibitors in combination with venetoclax as a promising treatment option for CLL patients by reducing the activation of CLL cells and the generation of venetoclax resistance induced by autologous activated T cells from CLL patients. [Read the Full Post]

Inhibition of Sphingosine Kinase 2 Results in PARK2-Mediated Mitophagy and Induces Apoptosis in Multiple Myeloma

47 views | May 27 2023

The study found that SK2 downregulation or inhibition induces mitophagy and apoptosis in multiple myeloma cell lines through the SET/PP2AC/PARK2 pathway, suggesting potential therapeutic strategies for the disease. [Read the Full Post]

Maternal embryonic leucine zipper kinase in tumor cells and tumor microenvironment: An emerging player and promising therapeutic opportunity

39 views | May 26 2023

MELK is a potential molecular target for cancer therapy due to its role in regulating tumor cell survival, growth, invasion, migration, and the tumor microenvironment, and small molecule inhibitors targeting it have shown promising results in clinical trials. [Read the Full Post]

CD137 signaling aggravates myocardial ischemia-reperfusion injury by inhibiting mitophagy mediated NLRP3 inflammasome activation

105 views | May 26 2023

CD137 signaling exacerbates myocardial ischemia-reperfusion injury by suppressing mitophagy and promoting NLRP3 inflammasome activation via increased mitochondrial ROS generation. [Read the Full Post]

The off-target effects of dynamin inhibitor Dyngo-4a during the internalization of dextran by bone marrow mesenchymal stem cells in rat

80 views | May 26 2023

The study concludes that the off-target effects of dynamin inhibitor Dyngo-4a are observed in the internalization of dextran by BMSCs. [Read the Full Post]

Dual inhibition of EZH2 and G9A/GLP histone methyltransferases by HKMTI-1-005 promotes differentiation of acute myeloid leukemia cells

151 views | May 26 2023

The study investigates the potential of using an EZH2 inhibitor, HKMTI-1-005, to improve the response of non-APL AML cells to ATRA-based therapy by inducing differentiation and upregulating the expression of differentiation pathway genes. [Read the Full Post]

Alteration of the tumor microenvironment by pharmacological inhibition of EZH2 in hepatocellular carcinoma

89 views | May 26 2023

The study found that EZH2 inhibition with UNC1999 impaired HCC tumor growth but also altered the TME by decreasing interferon-γ+ CD8+ T cells and regulatory T cells and increasing myeloid-derived suppressor cells, and combination therapy with agents that reduce MDSCs may represent a potential novel therapeutic strategy for HCC. [Read the Full Post]