Integrated Technology Platform Protein Kinases for Drug Development in Oncology
Protein kinases are among the most promising targets for drug discovery and development, mostly in oncology but also in other fields such as inflammation, Alzheimer's, and infectious diseases.
Christoph Sachsenmaier+1 more
doaj +1 more source
Kinases on Double Duty: A Review of UniProtKB Annotated Bifunctionality within the Kinome
Phosphorylation facilitates the regulation of all fundamental biological processes, which has triggered extensive research of protein kinases and their roles in human health and disease.
Aziz M. Rangwala+3 more
doaj +1 more source
Polyubiquitin binding to ABIN1 is required to prevent autoimmunity [PDF]
The protein ABIN1 possesses a polyubiquitin-binding domain homologous to that present in nuclear factor kappa B (NF-kappa B) essential modulator (NEMO), a component of the inhibitor of NF-kappa B (I kappa B) kinase (IKK) complex.
Alban Ordureau+57 more
core +5 more sources
Billion-years old proteins show the importance of N-lobe orientation in Imatinib-kinase selectivity [PDF]
The molecular origins of proteins' functions are a combinatorial search problem in the proteins' sequence space, which requires enormous resources to solve. However, evolution has already solved this optimization problem for us, leaving behind suboptimal solutions along the way. Comparing suboptimal proteins along the evolutionary pathway, or ancestors,
arxiv
Insights into PI3K/AKT signaling in B cell development and chronic lymphocytic leukemia
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
Targeting Protein Kinases Degradation by PROTACs
Kinase dysregulation is greatly associated with cell proliferation, migration and survival, indicating the importance of kinases as therapeutic targets for anticancer drug development.
Fei Yu+3 more
doaj +1 more source
A three-state kinetic mechanism for scaffold mediated signal transduction [PDF]
Signaling events in eukaryotic cells are often guided by a scaffolding protein. Scaffold proteins assemble multiple proteins in a spatially localized signaling complex and exert numerous physical effects on signaling pathways. To study these effects, we consider a minimal, three-state kinetic model of scaffold mediated kinase activation.
arxiv +1 more source
Taurine promotes glucagon‐like peptide‐1 secretion in enteroendocrine L cells
Taurine, a sulfur‐containing amino acid, is likely taken up by enteroendocrine L cells via the taurine transporter. This process increases the levels of cytosolic ATP. The increase in intracellular Ca2+ concentrations and glucagon‐like peptide‐1 secretion through membrane depolarization is caused by the closure of ATP‐sensitive potassium channels ...
Yuri Osuga+6 more
wiley +1 more source
Kinases and pseudokinases: Lessons from RAF [PDF]
Protein kinases are thought to mediate their biological effects through their catalytic activity. The large number of pseudokinases in the kinome and an increasing appreciation that they have critical roles in signaling pathways, however, suggest that ...
Ahuja, Lalima G+4 more
core +2 more sources
Making tau amyloid models in vitro: a crucial and underestimated challenge
This review highlights the challenges of producing in vitro amyloid assemblies of the tau protein. We review how accurately the existing protocols mimic tau deposits found in the brain of patients affected with tauopathies. We discuss the important properties that should be considered when forming amyloids and the benchmarks that should be used to ...
Julien Broc, Clara Piersson, Yann Fichou
wiley +1 more source