Serine/Arginine Protein Kinase Inhibitors Potentiate Melanoma Cell Death and Metastatic Inhibition Through Apoptotic Protein Triggering and Vimentin Dysregulation. [PDF]
Silsirivanit A +6 more
europepmc +1 more source
Approach for the Design of Covalent Protein Kinase Inhibitors via Focused Deep Generative Modeling. [PDF]
Yoshimori A, Miljković F, Bajorath J.
europepmc +1 more source
The neurokinin 1 receptor exists as full‐length (NK1L) and C‐terminally truncated (NK1S) splice variants. We show that NK1S heterodimerizes with NK1L, impairing Gαq coupling and Ca2+ mobilization while enhancing β‐arrestin1 recruitment. NK1S suppresses substance P‐driven gene expression and cell migration, revealing NK1S as an endogenous biased ...
Lan Phuong Nguyen +8 more
wiley +1 more source
Updated analysis of the prescription and evaluation of protein kinase inhibitors for oncology in Germany. [PDF]
Obst CS, Seifert R.
europepmc +1 more source
MARK4 enhances stress granule formation under oxidative stress and increases tau accumulation
MARK4 (red dots) localizes to stress granules (orange dots) and promotes their formation under oxidative stress by modulating TIA1 (blue dots). MARK4 and TIA1 synergistically increase tau (purple) accumulation, and the reduction of the TIA1 ortholog suppresses neurodegeneration in a fly model.
Sho Nakajima +8 more
wiley +1 more source
Novel 5-Oxopyrrolidine-3-carbohydrazides as Potent Protein Kinase Inhibitors: Synthesis, Anticancer Evaluation, and Molecular Modeling. [PDF]
Tumosienė I +5 more
europepmc +1 more source
IGF2 knockout reduces but does not abolish osteosarcoma growth in vitro and in vivo
To test whether endogenous IGF2 promotes osteosarcoma growth, IGF2 was knocked out in Saos2 cells via CRISPR‐Cas9. KO cells showed reduced proliferation in vitro, and knockout xenografts in mice reached only ~25% of wild‐type tumor volume. Insulin‐like growth factor 2 (IGF2) is implicated in osteosarcoma, but direct functional evidence of its role is ...
Shun Yao, Marco Archetti
wiley +1 more source
Clinical Activity of Mitogen-Activated Protein Kinase Inhibitors in Patients With MAP2K1 (MEK1)-Mutated Metastatic Cancers. [PDF]
Dankner M +18 more
europepmc +1 more source
Type I interferons modulate autophagy to shape gemcitabine response in pancreatic cancer cells
Type I interferons differentially modulate autophagy and the response of pancreatic cancer cells to gemcitabine. IFNα2b stimulates autophagic flux and protects cells from gemcitabine‐induced cell death, contributing to chemoresistance. In contrast, IFNβ1a inhibits autophagosome formation and enhances gemcitabine‐induced cell death, resulting in ...
Lucy E. Bonilla +10 more
wiley +1 more source
Searching for Old and New Small-Molecule Protein Kinase Inhibitors as Effective Treatments in Pulmonary Hypertension-A Systematic Review. [PDF]
Jasińska-Stroschein M, Glajzner P.
europepmc +1 more source

