Photoswitchable Inhibitors to Optically Control Specific Kinase Activity

T Aguirre, E Teichmann, FQ Römpp… - ACS chemical …, 2023 - ACS Publications
… -workers established a chemical genetic method for targeting protein kinases, often referred
… of the protein kinase and a small-molecule inhibitor is accomplished by mutating an

Discovering new biology with drug-resistance alleles

AM Freedy, BB Liau - Nature chemical biology, 2021 - nature.com
alleles’ could be important tools for interrogating proteinprotein interactions with precise
chemical … Furthermore, we believe that characterizing resistance mutations for proteinprotein

Allele-specific activation, enzyme kinetics, and inhibitor sensitivities of EGFR exon 19 deletion mutations in lung cancer

BP Brown, YK Zhang, S Kim… - Proceedings of the …, 2022 - National Acad Sciences
protein structure and function. Herein, we identified allele-specific functional differences
among ex19del variants attributable to recurring sequence and structure motifs. We built all-…

Downfalls of chemical probes acting at the kinase ATP-site: CK2 as a case study

EL Atkinson, J Iegre, PD Brear, EA Zhabina… - Molecules, 2021 - mdpi.com
an array of protein kinases to aid in the discovery of chemical probes to further understand
each kinase’… contains 518 genes that encode for serine/threonine/tyrosine kinases, each with …

Phosphoproteomics meets chemical genetics: Approaches for global mapping and deciphering the phosphoproteome

J Jurcik, B Sivakova, I Cipakova, T Selicky… - International Journal of …, 2020 - mdpi.com
chemical genetics in analog-sensitive protein kinase mutants and highlight selected strategies
for identifying protein kinase … powerful allele-specific chemical genetics strategies [58,59]. …

An unconventional gatekeeper mutation sensitizes inositol hexakisphosphate kinases to an allosteric inhibitor

T Aguirre, GL Dornan, S Hostachy, M Neuenschwander… - Elife, 2023 - elifesciences.org
… to over 80 protein kinases, the implementation for kinases phosphorylating small molecules,
… cerevisiae VPS34, a PI3 kinase, yielded an active mutant allele, however, mutation of the …

[HTML][HTML] An analog sensitive allele permits rapid and reversible chemical inhibition of PKC-3 activity in C. elegans

KB Ng, T Bland, N Hirani, NW Goehring - Micropublication Biology, 2022 - ncbi.nlm.nih.gov
… elegans zygotes, in which RNAi allows highly efficient depletion of the relevant players,
including the key polarity kinase atypical protein kinase C (PKC-3 in C. elegans ). Indeed, work …

Biochemical characterization of EGFR exon 20 insertion variants and their inhibitor sensitivities

H Zhao - 2023 - search.proquest.com
protein kinases, the kinase domain of EGFR is comprised of a smaller Nterminal lobe (N-lobe)
with a five-stranded β-sheet and an … than that of the inhibitor-sensitive L858R mutant, …

KinaseMD: kinase mutations and drug response database

R Hu, H Xu, P Jia, Z Zhao - Nucleic acids research, 2021 - academic.oup.com
… Somatic mutations in kinase genes can affect drug treatment, both sensitivity and resistance…
publications, we applied it to all the protein kinases and collected drug response data. …

ZNL0325, a Pyrazolopyrimidine-Based Covalent Probe, Demonstrates an Alternative Binding Mode for Kinases

Z Li, W Lu, TS Beyett, SB Ficarro, J Jiang… - … Medicinal Chemistry, 2024 - ACS Publications
… to other kinases with an αD-1 cysteine such as for BTK, BLK, and JAK3 in vitro and in cellulo,
which paves the road for new design strategies for drugging kinase and nonkinase targets …