Inhibition of the EGF receptor by binding of MIG6 to an activating kinase domain interface. [PDF]
, 2007 Members of the epidermal growth factor receptor family (EGFR/ERBB1, ERBB2/HER2, ERBB3/HER3 and ERBB4/HER4) are key targets for inhibition in cancer therapy.
Bose, Ron +5 more
core +1 more source
Accuracy of position determination in Ca$^{2+}$ signaling [PDF]
, 2019 A living cell senses its environment and responds to external signals. In this work, we study theoretically, the precision at which cells can determine the position of a spatially localized transient extracellular signal. To this end, we focus on the case, where the stimulus is converted into the release of a small molecule that acts as a second ...
arxiv +1 more source
Advance in Reversible Covalent Kinase Inhibitors [PDF]
arXiv, 2021 Reversible covalent kinase inhibitors (RCKIs) are a class of novel kinase inhibitors attracting increasing attention because they simultaneously show the selectivity of covalent kinase inhibitors, yet avoid permanent protein-modification-induced adverse effects.
arxiv
KA1-targeted regulatory domain mutations activate Chk1 in the absence of DNA damage [PDF]
, 2015 The Chk1 protein kinase is activated in response to DNA damage through ATR-mediated phosphorylation at multiple serine-glutamine (SQ) residues within the C-terminal regulatory domain, however the molecular mechanism is not understood. Modelling indicates
Freire, Raimundo +6 more
core +1 more source
Intramolecular C2 Domain-Mediated Autoinhibition of Protein Kinase C βII
Cell Reports, 2015 The signaling output of protein kinase C (PKC) is exquisitely controlled, with its disruption resulting in pathophysiologies. Identifying the structural basis for autoinhibition is central to developing effective therapies for cancer, where PKC activity ...
Corina E. Antal +4 more
doaj +1 more source
Proline-rich tyrosine kinase 2 mediates gonadotropin-releasing hormone signaling to a specific extracellularly regulated kinase-sensitive transcriptional locus in the luteinizing hormone beta-subunit gene [PDF]
, 2007 G protein-coupled receptor regulation of gene transcription primarily occurs through the phosphorylation of transcription factors by MAPKs. This requires transduction of an activating signal via scaffold proteins that can ultimately determine the outcome
Adam J. Pawson +73 more
core +1 more source
Insights into PI3K/AKT signaling in B cell development and chronic lymphocytic leukemia
FEBS Letters, EarlyView.This Review explores how the phosphoinositide 3‐kinase and protein kinase B pathway shapes B cell development and drives chronic lymphocytic leukemia, a common blood cancer. It examines how signaling levels affect disease progression, addresses treatment challenges, and introduces novel experimental strategies to improve therapies and patient outcomes.
Maike Buchner
wiley +1 more source
Inferring the Sign of Kinase-Substrate Interactions by Combining Quantitative Phosphoproteomics with a Literature-Based Mammalian Kinome Network [PDF]
, 2010 Protein phosphorylation is a reversible post-translational modification commonly used by cell signaling networks to transmit information about the extracellular environment into intracellular organelles for the regulation of the activity and sorting of proteins within the cell.
arxiv +1 more source
The Biology of Protein Kinase C
, 2012 This review gives a basic introduction to the biology of protein kinase C, one of the first calcium-dependent kinases to be discovered. We review the structure and function of protein kinase C, along with some of the substrates of individual isoforms.
Philip M. Newton +2 more
openaire +5 more sources
Plasmodium falciparum infection induces dynamic changes in the erythrocyte phospho-proteome [PDF]
, 2016 The phosphorylation status of red blood cell proteins is strongly altered during the infection by the malaria parasite Plasmodium falciparum. We identify the key phosphorylation events that occur in the erythrocyte membrane and cytoskeleton during ...
Bouyer, Guillaume +7 more
core +4 more sources