The objective of this study was to investigate the effect of modified Dioscorea pills (MDP) on microcirculatory remodeling in the hippocampus of rats with chronic cerebral hypoperfusion (CCH) through the angiopoietin (Ang)/tyrosine kinase receptor ...
Kuang Guiying+4 more
doaj +1 more source
Exploring receptor tyrosine kinases-inhibitors in Cancer treatments
Background Receptor tyrosine kinases (RTKs) are signaling enzymes responsible for the transfer of Adenosine triphosphate (ATP) γ-phosphate to the tyrosine residues substrates.
D. Samuel Metibemu+5 more
doaj +1 more source
Insulin signaling inhibits the 5-HT2C receptor in choroid plexus via MAP kinase
Background G protein-coupled receptors (GPCRs) interact with heterotrimeric GTP-binding proteins (G proteins) to modulate acute changes in intracellular messenger levels and ion channel activity.
Guan Kunliang+7 more
doaj +1 more source
MicroRNA-208b inhibits human osteosarcoma progression by targeting ROR2
MicroRNAs are widely involved in cancer progression by inhibiting the expression levels of oncogenes or tumor suppressor genes, and dysregulation of microRNAs may contribute to tumorigenesis.
Zhe Jiang+3 more
doaj +1 more source
Reprogramming signal transduction through a designer receptor tyrosine kinase
Kongkrongtong et al. present motif-based engineering of tyrosine kinase receptor for reprogramming signal transduction. Here, by swapping internal tyrosine of receptor with those that bind intracellular STAT signaling proteins, they demonstrate that ...
Tatphon Kongkrongtong+3 more
doaj +1 more source
Src-Like adaptor protein (SLAP) binds to the receptor tyrosine kinase Flt3 and modulates receptor stability and downstream signaling. [PDF]
Fms-like tyrosine kinase 3 (Flt3) is an important growth factor receptor in hematopoiesis. Gain-of-function mutations of the receptor contribute to the transformation of acute myeloid leukemia (AML).
Julhash U Kazi, Lars Rönnstrand
doaj +1 more source
Dynamic anticipation by Cdk2/Cyclin A-bound p27 mediates signal integration in cell cycle regulation [PDF]
p27$^{Kip1}$ (p27) is an intrinsically disordered protein (IDP) that folds upon binding to cyclin-dependent kinase (Cdk)$/$cyclin complexes (e.g., Cdk2$/$cyclin A), inhibiting their catalytic activity and causing cell cycle arrest. However, cell division progresses when stably Cdk2$/$cyclin A-bound p27 is phosphorylated on one or two structurally ...
arxiv +1 more source
Background We have previously demonstrated that PDGF receptor activation indirectly inhibits N-methyl-D-aspartate (NMDA) currents by modifying the cytoskeleton. PDGF receptor ligand is also neuroprotective in hippocampal slices and cultured neurons. PDGF
Beazely Michael A+2 more
doaj +1 more source
Benchmarking the performance of DFT functionals for absorption and fluorescence spectra of EGFR inhibitor AG-1478 using TD-DFT [PDF]
Optical spectra (UV-vis and fluorescence) are sensitive to the chemical environment and conformation of fluorophores and therefore, are ideal probes for their conformation and solvent responses. Tyrosine kinase inhibitors (TKI) such as AG-1478 of epidermal growth factor receptor (EGFR) when containing a quinazolinamine scaffold are fluorophores ...
arxiv
A Novel Bis-Coumarin Targets Multiple Tyrosine Kinases of Key Signaling Pathways in Melanoma and Inhibits Melanoma Cell Survival, Proliferation, and Migration [PDF]
Melanoma is one of the most dangerous skin malignancies due to its high metastatic tendency and high mortality. Activation of key signaling pathways enforcing melanoma progression depends on phosphorylation of tyrosine kinases, and oxidative stress. We here investigated the effect of the new bis-coumarin derivative (3,5-DCPBC) on human melanoma cell ...
arxiv