Dual targeting of RET and SRC synergizes in RET fusion‐positive cancer cells
Despite the strong activity of selective RET tyrosine kinase inhibitors (TKIs), resistance of RET fusion‐positive (RET+) lung cancer and thyroid cancer frequently occurs and is mainly driven by RET‐independent bypass mechanisms. Son et al. show that SRC TKIs significantly inhibit PAK and AKT survival signaling and enhance the efficacy of RET TKIs in ...
Juhyeon Son +13 more
wiley +1 more source
Rieske Oxygenase Catalyzed C-H Bond Functionalization Reactions in Chlorophyll b Biosynthesis. [PDF]
Liu J +4 more
europepmc +1 more source
Potential therapeutic targeting of BKCa channels in glioblastoma treatment
This review summarizes current insights into the role of BKCa and mitoBKCa channels in glioblastoma biology, their potential classification as oncochannels, and the emerging pharmacological strategies targeting these channels, emphasizing the translational challenges in developing BKCa‐directed therapies for glioblastoma treatment.
Kamila Maliszewska‐Olejniczak +4 more
wiley +1 more source
TREX1, a predator for treating MSI‐H tumors?
Immunotherapy benefits many patients; yet, some with MSI‐H tumors remain unresponsive despite their high immunogenicity. Xu et al. reveal that TREX1 enables immune evasion by degrading cytosolic DNA and suppressing cGAS–STING–IFN‐I signaling. TREX1 loss restores DNA sensing, increases CD8+ T and NK cell infiltration, and boosts antitumor immunity ...
Elena Benidovskaya +2 more
wiley +1 more source
Ruthenium-catalysed decarboxylative unsymmetric dual ortho-/meta-C-H bond functionalization of arenecarboxylic acids. [PDF]
Li X, Wang X, Zhang J.
europepmc +1 more source
ATF4‐mediated stress response as a therapeutic vulnerability in chordoma
We screened 5 chordoma cell lines against 100+ inhibitors of epigenetic and metabolic pathways and kinases and identified halofuginone, a tRNA synthetase inhibitor. Mechanistically halofuginone induces an integrated stress response, with eIF2alpha phosphorylation, activation of ATF4 and its target genes CHOP, ASNS, INHBE leading to cell death ...
Lucia Cottone +11 more
wiley +1 more source
Biocatalytic, Intermolecular C-H Bond Functionalization for the Synthesis of Enantioenriched Amides. [PDF]
Athavale SV +5 more
europepmc +1 more source
Cell surface interactome analysis identifies TSPAN4 as a negative regulator of PD‐L1 in melanoma
Using cell surface proximity biotinylation, we identified tetraspanin TSPAN4 within the PD‐L1 interactome of melanoma cells. TSPAN4 negatively regulates PD‐L1 expression and lateral mobility by limiting its interaction with CMTM6 and promoting PD‐L1 degradation.
Guus A. Franken +7 more
wiley +1 more source
Room‐Temperature Direct Homolysis of Csp3─H Bond via Catalyst‐Free Photoexcitation
The C─H bond is the most abundant chemical bond in organic compounds. Therefore, the development of the more direct methods for C─H bond cleavage and the elucidation of their mechanisms will provide an important theoretical basis for achieving more ...
Qi Miao +7 more
doaj +1 more source
Recent advances in metal catalyst- and oxidant-free electrochemical C-H bond functionalization of nitrogen-containing heterocycles. [PDF]
Li YN, Wang B, Huang YK, Hu JS, Sun JN.
europepmc +1 more source

