Role and mechanistic actions of protein kinase inhibitors as an effective drug target for cancer and COVID. [PDF]
Narayanan J +6 more
europepmc +1 more source
Mutant p53R273H disrupts PDPK1 homodimerization and contributes to PDPK1 activation
How mutant p53R273H drives AKT signaling is unclear. We show that p53R273H, but not wild‐type, directly binds PDPK1 via a mutation‐dependent conformational change. This interaction disrupts inhibitory PDPK1 homodimerization and enhances AKT phosphorylation.
Mei Chee Lim +11 more
wiley +1 more source
Design characteristics of mass balance studies conducted for protein kinase inhibitors. [PDF]
Riechelman B +5 more
europepmc +1 more source
Data sets of human and mouse protein kinase inhibitors with curated activity data including covalent inhibitors. [PDF]
Xerxa E, Bajorath J.
europepmc +1 more source
Targeting the EpCAM‐AXL axis to overcome drug resistance in lung cancer
Lung cancer cells often evade therapy by hijacking signaling pathways. We reveal that cleaved EpCAM (sEpCAM) stabilizes the oncogenic protein AXL, driving NF‐κB and STAT3‐mediated chemoresistance. This EpCAM‐AXL axis identifies a high‐risk patient subset with poor prognosis.
Alexa Guerrero‐Alba +5 more
wiley +1 more source
Editorial: The molecular mechanisms and therapeutic implications of protein kinase inhibitors in cancer therapy. [PDF]
Sun YH +4 more
europepmc +1 more source
Engineering IL‐4 resistant proinflammatory human myeloid cells for cancer immunotherapy
We developed a scalable workflow to generate proinflammatory human myeloid cells. CRISPR/Cas9‐edited CD34+ hematopoietic stem and progenitor cells were expanded and differentiated with M‐CSF. Deletion of STAT6 or STAT6/NFKB1 enhanced macrophage proinflammatory gene expression and cytokine secretion in the presence of IL‐4 while maintaining antibody ...
Theresa Barberi, Alan D. Friedman
wiley +1 more source
Cardiotoxicity Induced by Protein Kinase Inhibitors in Patients with Cancer. [PDF]
Grela-Wojewoda A +4 more
europepmc +1 more source
UiO‐66(Zr) metal–organic frameworks are chemically stable, biocompatible, and highly tunable nanomaterials. Their modular structure enables controlled drug delivery, multimodal bioimaging, and light‐activated photodynamic therapy, supporting integrated diagnostic and therapeutic (theranostic) applications in cancer and biomedical research.
Veronika Huntošová +2 more
wiley +1 more source
Research progress of small molecule protein kinase inhibitors (SMKIs) in the treatment of colorectal cancer: mechanism, application, and future prospects. [PDF]
Liu L +7 more
europepmc +1 more source

