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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

Adenosine Receptor

Adenosine A1 Receptors Participate in Excitability Changes after Cortical Epileptic Afterdischarges in Immature Rats

45 views | Feb 08 2024

Adenosine A1 receptor modulation demonstrated age-dependent effects on postictal potentiation and refractoriness in rats, with A1 agonists suppressing both types of potentiation in younger rats while antagonists augmented delayed potentiation and moderately affected immediate refractoriness, indicating crucial regulatory roles of these receptors in post-seizure responses across different developmental stages. [Read the Full Post]

Current evidence for second-line treatment in metastatic renal cell carcinoma after progression to immune-based combinations

55 views | Jan 05 2024

The evolving landscape of metastatic renal cell carcinoma treatments, driven by immune checkpoint inhibitor-based combinations in the first line and uncertainties in subsequent therapies, highlights the need for predictive models and ongoing research to guide personalized, effective treatment strategies. [Read the Full Post]

Exercise attenuates neuronal degeneration in Parkinson's disease rat model by regulating the level of adenosine 2A receptor

275 views | Dec 23 2023

Exercise appears to mitigate Parkinson's disease symptoms in rats by reducing neurodegeneration through a-synuclein aggregation reduction and adenosine 2A receptor modulation, although the co-administration of an adenosine A2A receptor agonist reverses these beneficial effects. [Read the Full Post]

Antineoplastic effects of pharmacological inhibitors of aurora kinases in CSF3RT618I-driven cells

126 views | Dec 14 2023

The study demonstrates that aurora kinase inhibitors, particularly reversine, exert significant antineoplastic effects in Ba/F3 cells expressing the CSF3RT618I mutation, reducing cell viability, clonogenicity, and proliferative capacity, while modulating key molecular pathways associated with cell cycle and apoptosis in the context of chronic neutrophilic leukemia (CNL). [Read the Full Post]

Pharmacological Characterization of P626, a Novel Dual Adenosine A2A/A2B Receptor Antagonist, on Synaptic Plasticity and during an Ischemic-like Insult in CA1 Rat Hippocampus

55 views | Nov 02 2023

The newly synthesized dual A2AAR/A2BAR antagonist, P626, demonstrated the ability to prevent A2AAR- and A2BAR-mediated effects and delay anoxic depolarization in a concentration-dependent manner, potentially making it a promising neuroprotective compound for stroke treatment. [Read the Full Post]

Adenosine A2A Receptors Shut Down Adenosine A1 Receptor-Mediated Presynaptic Inhibition to Promote Implementation of Hippocampal Long-Term Potentiation

113 views | Jul 18 2023

Activation of A2A receptors dampens the inhibitory effects of A1 receptors, enabling the implementation of hippocampal long-term potentiation (LTP) during high-frequency induction. [Read the Full Post]

GW-2974 and SCH-442416 modulators of tyrosine kinase and adenosine receptors can also stabilize human telomeric G-quadruplex DNA

127 views | Apr 13 2023

GW-2974 and SCH-442416 could stabilize human telomeric G-quadruplex DNA in addition to their known tyrosine kinase and adenosine receptor modulation properties, suggesting that stabilizing G-quadruplex DNA could be a potential mechanism underlying their anti-cancer activity. [Read the Full Post]

In vitro pharmacological profile of KW-6356, a novel adenosine A2A receptor antagonist/inverse agonist

79 views | Apr 06 2023

The study found that KW-6356 is a potent and selective adenosine A2A receptor antagonist/inverse agonist with insurmountable antagonism, while istradefylline exhibits surmountable antagonism, and crystallography explains the differences in their pharmacological properties. [Read the Full Post]

Antiangiogenic Effects of Doxazosin on Experimental Choroidal Neovascularization in Mice

565 views | Feb 28 2019

Guo J et al. found that Doxazosin exerts antiangiogenic actions in an experimental mouse model of CNV and may be a potential adjunctive therapy for neovascular age-related macular degeneration in humans. [Read the Full Post]

Prenatal caffeine exposure induced a lower level of fetal blood leptin mainly via placental mechanism

1009 views | Apr 27 2018

Wu YM et al. found that PCE decreased fetal blood leptin mainly via reducing the expression and transportation of leptin in the placenta. [Read the Full Post]