This review highlights the role of #DYRK #kinases in #DNADamageResponse, linking their activity to #cancer progression, while evaluating current DYRK inhibitors and positioning DYRK inhibition as a promising #PrecisionOncology strategy.

#OpenAccess: doi.org/10.1016/j.ge...

Neutrophils and the NLRP3 inflammasome: a tale of proteases, kinases, and inflammation Cell type–specific mechanisms modulate Nod-like receptor family pyrin domain containing 3 inflammasome activation in macrophages and neutrophils, shaping i

"#Neutrophils and the #NLRP3 #Inflammasome: a tale of #Proteases, #Kinases, and #Inflammation" - read the new Review by Vinicius Leal @uspoficial.bsky.social & Alexander Weber @unituebingen.bsky.social

Genome-wide identification and expression analysis of wall-associated kinases (WAK/WAKLs) in Salvia miltiorrhiza with novel insights into tanshinone regulation in response to fungal elicitors Wall-associated kinases (WAKs) are transmembrane proteins involved in growth, cell wall expansion, and defence responses, particularly through antimicrobial metabolite accumulation.

Genome-wide identification and #expression analysis of wall-associated #kinases (WAK/WAKLs) in #Salvia miltiorrhiza with novel insights into #tanshinone regulation in response to #fungal elicitors.
To read this article in JHSB 101:1, visit:

Overall, I hope that 2026 will yield at least the same degree of scientific progress as 2025. (12/12)

#Chemistry #ChemBio #Science #Antibiotics #Synthesis #TPD #Degrader #Proteomics #Kinases #RNA #Screening #CovalentInhibitors #DirectToBiology

Interesting J. Med. Chem. paper by the group of Michael Waring. They developed alkynylpyridopyrimidinones that covalently target Cys775 of EGFR to allow development of #CovalentInhibitors even against the C797S resistance mutant.
pubs.acs.org/doi/10....
#ChemSky #ChemBio #DrugDiscovery #Kinases

Allosteric binding cooperativity in kinases signaling, signalopathies, and drug development Protein kinases catalyze the transfer of phosphate groups from ATP to specific substrates, initiating, modulating, or terminating signaling cascades. …

A nice review on #cooperativity in #kinases - I think exploiting these properties may be the way we can forgo some of the tox that is dose limiting in the clinic associated with kinase inhibitors #medchem

www.sciencedirect.com/science/arti...

Insightful talk by Anthe Janssen at #NWOCHAINS. He talked about his research with Dompé in the framework of #ChemistryNL on using #docking and #MachineLearning-assisted re-scoring to better predict compound binding affinity to #kinases.
pubs.acs.org/doi/10.1021/...
#ChemSky #ChemBio #DrugDiscovery

Looking to start up my blue account again. I am a postdoc based in the Parsons lab at the University of Birmingham (#uob). I have keen interests in how #kinases modulate #cellcycle and #DNAdamage response pathways. I welcome the opperunity to connect with fellow #cellsignalling researchers 🙂

A tour-de-force study by the group of Bernhard Küster (@kusterlab.bsky.social). They profiled 133 kinase inhibitors in 5 cell lines at 11 doses using #phosphoproteomics to identify 5,318 confident kinase::substrate relationships for 96 human #kinases www.biorxiv.org/content/10.1...
#ChemSky #ChemBio

Andrea Lacigová Click on the article title to read more.

proud #supervisor 👍👏:
📣Interview with a very talented #undergraduate 👩‍🎓student (@uebscimuni.bsky.social)
from our lab (@cajaneklab.bsky.social)
Andrea Lacigova, accompanying her recent review on #ciliary #kinases in #Cytoskeleton.

link for the interview👉
onlinelibrary.wiley.com/doi/10.1002/...

Cysteine-based #redox sensors in the #cardiovascular system: from identification to physiology and drug discovery

Joseph R. Burgoyne and Philip Eaton
doi.org/10.1152/phys...
#CysteineThiols #Kinases

Modulating the Binding Kinetics of Bruton’s Tyrosine Kinase Inhibitors through Transition-State Effects Optimization exercises strive toward increasing the efficacy and selectivity of small molecules toward the target of interest while simultaneously phasing out design elements that lead to off-target interactions. Given the nonequilibrium nature of biological systems, greater reliance should be placed on engineering kinetic selectivity in addition to equilibrium thermodynamic selectivity; however, the rational design of kinetic selectivity is a challenging endeavor. This study presents a systematic knowledge-based approach to the design of inhibitors that vary in their binding kinetics for Bruton’s tyrosine kinase (BTK), a target for treating B-cell malignancies and autoimmune diseases. A detailed kinetic assessment was performed on existing BTK inhibitors, which, together with structural studies, provided critical insights into BTK-inhibitor interactions that control the kinetics of enzyme inhibition. Subsequently, a series of pyrazolopyrimidines was designed with the objective of modifying interactions between the inhibitor and the regulatory (R) spine in the kinase back pocket, which were hypothesized to modulate the stability of the transition state on the binding reaction coordinate. This resulted in the development of BTK inhibitors with extended residence time in which the variation in kon and koff was uncoupled from equilibrium thermodynamic affinity.

Interesting paper by the group of Peter Tonge in @jacs.acspublications.org. They studied the #kinetics of non-covalent #BTK inhibitors. Clinical compounds showed increased residence times, while association rates were nearly constant. pubs.acs.org/doi/10....
#Kinases #DrugDiscovery #ChemSky #ChemBio

🧪TOMORROW 15:00 BST 22/04/2025🧪: gather round for the latest in #cilia & #centrosome research including curious #kinases, co-translational assembly, cilia in #meiosis & spermatogenesis, AND complexes controlling ciliary content from the field's rising talent! Free & open to all... just register!

Genome-wide identification and #expression analysis of wall-associated #kinases (WAK/WAKLs) in #Salvia miltiorrhiza with novel insights into #tanshinone regulation in response to #fungal elicitors.
To read this new article in JHSB, visit: doi.org/10.1080/1462...

Spectral shift competition assay data for three kinases and a panel of kinase inhibitors

Domainex has successfully developed a #competition based spectral shift assay for ATP-competitive inhibitors for several #kinases.
Read the full case study here: www.domainex.co.uk/drug-discove...
#SpectralShift #CompetitionAssay #AssayDevelopment

Phosphorylation at the Helm: Kinase‐Mediated Regulation of Primary Cilia Assembly and Disassembly The primary cilium serves as an antenna of most vertebrate cells and is important for conveying cues from several signaling pathways into appropriate cellular responses during development and homeost...

Proud of Andrea Lacigová, a very talented #student 👩‍🎓from our lab, whose insightful review on the role of #kinases in #cilia assembly and disassembly is now published in #Cytoskeleton.
doi.org/10.1002/cm.2...

New research shows salt-inducible #kinases (SIKs) transduce mechanical forces in pancreatic endocrine lineage specifications. www.cell.com/stem-cell-re...

@isscr.org

@cellpress.bsky.social

@gairdnerawards.bsky.social

@sickkidsvs.bsky.social

How plants fend off pathogens: The role of calcium and kinases Plant pests such as bacteria and fungi lead to significant yield losses in agriculture. In order to develop new strategies against such pathogens, understanding the plant's immune response is of centr...

How #plants fend off #pathogens: The role of #calcium and #kinases

#immune_response #agriculture #bacteria #fungi #signalling #bi-kinase_module

phys.org/news/2025-01...

❄️ We hope you're having an ice week so far!

Today's #festiveFEBSJ #Editorschoice is brought to you by:

🕵️ Wilkins & team, who identified two new #kinases that regulate the #histone methyltransferase DOT1L

Find out more here: https://buff.ly/41uY2hl

Registration is open for a #Canadian classic. Signalling in Normal & Cancer Cells. #Science4All #ScienceSaves #ScienceIsFun #SignalTransduction #scRNAseq #ModelSystems #kinases #oncogenes #cytoskeleton #CellCycle #Chromatin #epigenetics
@cdnwomenstem.bsky.social

event.fourwaves.com/banffsncc202...