EGF regulates tyrosine phosphorylation and membrane-translocation of the scaffold protein Tks5 [PDF]
Background: Tks5/FISH is a scaffold protein comprising of five SH3 domains and one PX domain. Tks5 is a substrate of the tyrosine kinase Src and is required for the organization of podosomes/invadopodia implicated in invasion of tumor cells.
Buday, László +5 more
core +1 more source
GSK3-mediated raptor phosphorylation supports amino acid-dependent Q2 mTORC1-directed signalling [PDF]
The mammalian or mechanistic target of rapamycin (mTOR) complex 1 (mTORC1) is a ubiquitously expressed multimeric protein kinase complex that integrates nutrient and growth factor signals for the co-ordinated regulation of cellular metabolism and cell ...
Alan Prescott +60 more
core +3 more sources
1,2,6-thiadiazinones as novel narrow spectrum calcium/calmodulin-dependent protein kinase kinase 2 (CaMKK2) inhibitors [PDF]
We demonstrate for the first time that 4H-1,2,6-thiadiazin-4-one (TDZ) can function as a chemotype for the design of ATP-competitive kinase inhibitors. Using insights from a co-crystal structure of a 3,5-bis(arylamino)-4H-1,2,6-thiadiazin-4-one bound to ...
Asquith, Christopher R.M. +11 more
core +3 more sources
Pockets as structural descriptors of EGFR kinase conformations [PDF]
Epidermal Growth Factor Receptor (EGFR), a tyrosine kinase receptor, is one of the main tumor markers in different types of cancers. The kinase native state is mainly composed of two populations of conformers: active and inactive.
Barletta Roldan, Patricio German +4 more
core +1 more source
Organoids in pediatric cancer research
Organoid technology has revolutionized cancer research, yet its application in pediatric oncology remains limited. Recent advances have enabled the development of pediatric tumor organoids, offering new insights into disease biology, treatment response, and interactions with the tumor microenvironment.
Carla Ríos Arceo, Jarno Drost
wiley +1 more source
Extracellular Signal-Regulated Kinase (ERK) Inhibitors in Oncology Clinical Trials [PDF]
The mitogen-activated protein kinase (MAPK) pathway consists of the series of protein kinases RAS-RAF-MEK- Extracellular signal-regulated kinase (ERK), and its function is important to cell proliferation, differentiation, motility, and survival.
Haelee M Chin +2 more
doaj +1 more source
Rapid evolution of protein kinase PKR alters sensitivity to viral inhibitors. [PDF]
Protein kinase PKR (also known as EIF2AK2) is activated during viral infection and phosphorylates the alpha subunit of eukaryotic translation initiation factor 2 (eIF2), leading to inhibition of translation and viral replication. We report fast evolution
Dever, Thomas E +4 more
core
Activation of tyrosine kinases by mutation of the gatekeeper threonine. [PDF]
Protein kinases targeted by small-molecule inhibitors develop resistance through mutation of the gatekeeper threonine residue of the active site. Here we show that the gatekeeper mutation in the cellular forms of c-ABL, c-SRC, platelet-derived growth ...
Azam, Mohammad +4 more
core +1 more source
The Serine/Threonine Protein Kinase (Akt)/ Protein Kinase B (PkB) Signaling Pathway in Breast Cancer [PDF]
According to statistical data published in 2019, breast cancer is among the leading causes of death in women worldwide. The serine/threonine kinase (AKT) or protein kinase B (PkB) signaling pathway is activated by phosphorylation processes, which further
Bratu, Ovidiu Gabriel +8 more
core +3 more sources
Reciprocal control of viral infection and phosphoinositide dynamics
Phosphoinositides, although scarce, regulate key cellular processes, including membrane dynamics and signaling. Viruses exploit these lipids to support their entry, replication, assembly, and egress. The central role of phosphoinositides in infection highlights phosphoinositide metabolism as a promising antiviral target.
Marie Déborah Bancilhon, Bruno Mesmin
wiley +1 more source

