Results 71 to 80 of about 10,618 (207)
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
Rapamycin induces transactivation of the EGFR and increases cell survival. [PDF]
The mammalian target of rapamycin (mTOR) signaling network regulates cell growth, proliferation and cell survival. Deregulated activation of this pathway is a common event in diverse human diseases such as cancers, cardiac hypertrophy, vascular ...
Chaturvedi, D +4 more
core +2 more sources
Cathepsin B‐sensitive peptide–adjuvant conjugates are designed, synthesized, and evaluated to deliver an antigenic peptid and an adjuvant targeting Toll‐like receptors 7 and 8 (TLR7/8) to antigen presenting cells. The adjuvant is released by cathepsin B resulting in antigen presentation and TLR mediated T cell activation.
Marjolein M. E. Isendoorn +6 more
wiley +1 more source
A series of 3-ethyl(methyl)-2-thioxo-2,3-dihydrobenzo[g]quinazolines (1–17) were synthesized, characterized, and evaluated in vitro for their antiangiogenesis VEGFR-2-targeting, antiproliferative, and antiapoptotic activities against breast MCF-7 and ...
Hatem A. Abuelizz +6 more
doaj +1 more source
High Throughput Screening of a GlaxoSmithKline Protein Kinase Inhibitor Set Identifies an Inhibitor of Human Cytomegalovirus Replication that Prevents CREB and Histone H3 Post-Translational Modification. [PDF]
To identify new compounds with anti-human cytomegalovirus (HCMV) activity and new anti-HCMV targets, we developed a high throughput strategy to screen a GlaxoSmithKline (GSK) Published Kinase Inhibitor Set (PKIS).
Ho, CMK +5 more
core +3 more sources
This review summarizes recent advances in copper‐ and silver‐catalyzed reactions of active methylene isocyanides for the synthesis of highly substituted five‐ and six‐membered heterocycles. Emphasis is placed on [3+n] cycloadditions, annulations, and asymmetric strategies, highlighting current limitations and future opportunities in heterocycle ...
Jimil George, Kyungsoo Oh
wiley +1 more source
Prevention of Weight Regain After GLP1RA Cessation With Oral TIX100
Diabetes, Obesity and Metabolism, EarlyView.
SeongHo Jo +5 more
wiley +1 more source
In organic synthesis, deep eutectic solvents (DES) have demonstrated their ability to be used as reaction media for the development of reactions in line with green chemistry principles. This review presents an overview of microwave‐assisted organic synthesis in DES, highlighting the diversity of uses for these solvents, their role in mechanisms, the ...
Pierre‐Olivier Delaye +2 more
wiley +1 more source
The heterocyclic compounds have a great importance in medicinal chemistry. One of the most important heterocycles in medicinal chemistry are quinazolines possessing wide spectrum of biological properties like antibacterial, antifungal, anticonvulsant ...
Elham Jafari +4 more
doaj
EGFR tyrosine kinase targeted compounds [PDF]
In this study, we illustrate computer aided drug design of new benzothiazole and pyrimido[2,1-b]benzothiazole derivatives as epidermal growth factor receptor tyrosine kinase (EGFR-TK) inhibitors.
El-Bendary, Eman R. +3 more
core

