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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

LRRK2

LRRK2 Kinase Inhibitor Rejuvenates Oxidative Stress-Induced Cellular Senescence in Neuronal Cells

77 views | Jan 12 2024

Rotatenone-induced LRRK2 upregulation triggers cellular senescence, promoting α-synuclein accumulation in Parkinson's disease, which can be mitigated by LRRK2 kinase inhibition, suggesting a potential therapeutic avenue for disease intervention. [Read the Full Post]

Capturing Differences in the Regulation of LRRK2 Dynamics and Conformational States by Small Molecule Kinase Inhibitors

130 views | Oct 14 2023

This study combines enhanced sampling simulations with HDX-MS to investigate the effects of type I and type II kinase inhibitors on the conformational dynamics and allosteric communications within the C-terminal domains of LRRK2, providing insights for the design of allosteric modulators that can regulate LRRK2 conformations and its interactions with other proteins. [Read the Full Post]

Activation of Most Toll-Like Receptors in Whole Human Blood Attenuates Platelet Deposition on Collagen under Flow

244 views | Apr 11 2023

The study found that TLR signaling plays a complex role in platelet function under flow conditions and that the effects of TLR activation on platelet deposition depend on the specific TLR and its ligand, and that IKK and NF-κB inhibitors may be effective in inhibiting platelet deposition under flow. [Read the Full Post]

KL-FGF23-VD Axis in Improving Late-Onset Alzheimer's Disease by Modulating IKK/NF- κ B Signal Pathway

158 views | Apr 10 2023

The study suggests that the KL-FGF23-VD axis has potential therapeutic value for Alzheimer's disease treatment by regulating the IKK/NF-κB pathway. [Read the Full Post]

URMC-099 prophylaxis prevents hippocampal vascular vulnerability and synaptic damage in an orthopedic model of delirium superimposed on dementia

284 views | Oct 19 2022

Patrick Miller-Rhodes et al. linked post-surgical endothelial activation, microglial MafB immunoreactivity, and synapse loss as key substrates for DSD, all of which could be prevented by URMC-099. [Read the Full Post]

MLK3 mediates impact of PKG1α on cardiac function and controls blood pressure through separate mechanisms

1023 views | Nov 25 2021

Timothy D Calamaras et al. suggested augmenting MLK3 kinase activity could preserve LV function in HF but avoid hypotension from PKG1α activation. [Read the Full Post]

Mixed lineage kinase 3 inhibition induces T cell activation and cytotoxicity

1168 views | Dec 07 2020

Sandeep Kumar et al. demonstrated that MLK3 played an important role in T cell biology, and targeting MLK3 could serve as a potential therapeutic intervention via increasing T cell cytotoxicity in cancer. [Read the Full Post]

URMC-099 Facilitates Amyloid-β Clearance in a Murine Model of Alzheimer's Disease

1175 views | Mar 01 2020

Tomomi Kiyota et al. indicated that URMC-099 facilitates Aβ clearance in the brain of APP/PS1 mice. The multifaceted immune modulatory and neuroprotective roles of URMC-099 make it an attractive candidate for ameliorating the course of AD. This is buttressed by removal of pathologic Aβ species and restoration of the brain's microenvironment during disease. [Read the Full Post]