190publications
186kinase studies
4phosphatase studies
2001–2026years covered
Showing 190 publications
A Constellation of Fluorescent Biosensors to Illuminate the Galaxy of Protein Kinases
Multiple
Mechanism & structural biologyAssay & sensor technologyReview
Technology & reviews
An S752D activation loop mutation dynamically primes Muscle-Specific Kinase for activation
MuSK
Mechanism & structural biology
PhosphoSens
Enozertinib Is a Selective, Brain-Penetrant EGFR Inhibitor for Treating Non-Small Cell Lung Cancers with EGFR Exon 20 and Atypical Mutations
EGFR
Covalent inhibitor kineticsInhibitor discovery & SARSelectivity & kinome profiling
PhosphoSens
Erk inhibitors intercept Erk-mediated negative feedback while imposing cell-cycle arrest and activating p38
ERK1/2
Signaling biology
PhosphoSens
Global protein-ligand binding affinity profiling via photocatalytic labeling
Multiple
Selectivity & kinome profilingCell & tissue lysate assays
PhosphoSens
Identification of a New Phosphorylated Host Interactor of the Epstein-Barr Virus (EBV) Kinase BGLF4 Suggests Key Points for EBV-Specific Antiviral Drug Targeting
BGLF4 (EBV kinase)
Inhibitor discovery & SARAssay & sensor technology
PhosphoSens
Let the peptides shine: SOX (Sulfonamido-OXine)-labelled peptides for direct kinase and phosphatase monitoring
Multiple
Inhibitor discovery & SARMechanism & structural biologyCell & tissue lysate assaysAssay & sensor technologyPhosphatase biologyReview
Technology & reviews
Molecular modulators of cyclin-dependent kinase 4/6 inhibitor response in experimental glioma identified through genome-wide CRISPR-Cas9 screening
CDK2/Cyclin E1
Inhibitor discovery & SAR
PhosphoSens
Riding toward Selectivity: Optimization of Covalent 7-Azaindole-Based BMX Kinase Inhibitors
BMX
Covalent inhibitor kineticsInhibitor discovery & SARSelectivity & kinome profiling
PhosphoSens
Selective Inhibitor of Protein Kinase PKN3 Generated by Conjugation of a Structurally Optimized Bumped-(2-Aminoethyl)-8-anilinoisoquinoline-5-sulfonamide (H-9) with d-Arginine-Rich Chain
PKN3, PKN1
Covalent inhibitor kineticsInhibitor discovery & SARSelectivity & kinome profiling
PhosphoSens
Structural Studies of Fourth-Generation EGFR Inhibitors Reveal Insights into Selective T790M and C797S Targeting
EGFR and EGFR mutants
Inhibitor discovery & SARMechanism & structural biology
PhosphoSens
Structural basis of the cyclin Y/14-3-3 protein-mediated activation of CDK16
CDK16
Mechanism & structural biology
PhosphoSens
TAS3351 is a brain penetrable EGFR-TKI that overcomes T790M and C797S resistant mutations
EGFR and EGFR mutants
Signaling biology
PhosphoSens
18F-FLT PET, a Noninvasive Pharmacodynamic Biomarker of Tumor Cell Proliferation, Detected Differential Response to Various Cyclin-Dependent Kinase (CDK) Inhibitors
CDK2, CDK4/6, CDK7, CDK9
Inhibitor discovery & SAR
PhosphoSens
A "Ligand First" Approach toward Selective, Covalent JNK2/3 Inhibitors
JNK2/3
Covalent inhibitor kineticsInhibitor discovery & SARSelectivity & kinome profiling
PhosphoSens
A twist in the tale: shifting from covalent targeting of a tyrosine in JAK3 to a lysine in MK2
JAK3, MK2
Covalent inhibitor kineticsInhibitor discovery & SARMechanism & structural biology
PhosphoSens
Application and Cross-Validation of a High-Throughput SPR Method for Characterizing Covalent Binding Ligands
MK2
Covalent inhibitor kineticsAssay & sensor technology
PhosphoSens
Beyond FOXO1: AS1842856 inhibits GSK3 to enhance cytotoxic effects in B-ALL
Kinome Profiling (GSK3)
Inhibitor discovery & SARSelectivity & kinome profiling
KinSight services
COOKIE-Pro: covalent inhibitor binding kinetics profiling on the proteome scale
Not specified
Covalent inhibitor kineticsInhibitor discovery & SARSelectivity & kinome profiling
PhosphoSens
Cancer hotspot mutations rewire ERK2 specificity by selective exclusion of docking interactions
ERK2 and mutants
Mechanism & structural biology
PhosphoSens
Covalent Alkynylpyridopyrimidinones Targeting Cysteine 775 of the Epidermal Growth Factor Receptor Overcome Resistance to Current Therapies
EGFR L858R/T790M
Covalent inhibitor kineticsInhibitor discovery & SARSelectivity & kinome profiling
KinSight services
Discovery of BMS-986408, a First-In-Class Dual DGKα and DGKζ Inhibitor that Unleashes PD-1 Checkpoint and CAR T-cell Immunotherapies
DGKα, DGKζ (lipid kinases)
Inhibitor discovery & SARMechanism & structural biology
PhosphoSens
Discovery of STX-721, a Covalent, Potent, and Highly Mutant-Selective EGFR/HER2 Exon20 Insertion Inhibitor for the Treatment of Non-Small Cell Lung Cancer
EGFR/HER2 exon 20 mutants
Covalent inhibitor kineticsInhibitor discovery & SARSelectivity & kinome profiling
PhosphoSens
Factors affecting irreversible inhibition of EGFR and influence of chirality on covalent binding
EGFR
Covalent inhibitor kineticsInhibitor discovery & SARSelectivity & kinome profiling
KinSight services
Inhibition of Muscle-Specific Protein Kinase (MuSK) Releases Organophosphate-Aged Acetylcholinesterase (AChE) from C2C12 Cells
MuSK
Inhibitor discovery & SAR
PhosphoSens
Novel Flavonoid Derivatives Show Potent Efficacy in Human Lymphoma Models
Kinome Profiling
Inhibitor discovery & SARSelectivity & kinome profilingMechanism & structural biology
PhosphoSens
Profiling and Optimizing Targeted Covalent Inhibitors through EGFR-Guided Studies
EGFR
Covalent inhibitor kineticsInhibitor discovery & SARSelectivity & kinome profilingMechanism & structural biology
PhosphoSens
Proteome-wide ligandability maps of drugs with diverse cysteine-reactive chemotypes
JAK1
Covalent inhibitor kineticsInhibitor discovery & SAR
PhosphoSens
STX-721, a Covalent EGFR/HER2 Exon 20 Inhibitor, Utilizes Exon 20-Mutant Dynamic Protein States and Achieves Unique Mutant Selectivity Across Human Cancer Models
EGFR/HER2 exon 20 mutants
Covalent inhibitor kineticsInhibitor discovery & SARSelectivity & kinome profilingMechanism & structural biology
PhosphoSens
The role of kinase domain dimerization in EGFR activation
EGFR
Mechanism & structural biology
PhosphoSens
Time-evolved metrics for safety pharmacological assessments of small molecules and biologics
Not specified
Selectivity & kinome profilingReview
PhosphoSens
Type II kinase inhibitors that target Parkinson's disease-associated LRRK2
LRRK2
Inhibitor discovery & SARMechanism & structural biology
PhosphoSens
Un-LOK-ing a New Approach for Conformational Selective Targeting of STK10 (LOK)
STK10
Inhibitor discovery & SARSelectivity & kinome profilingMechanism & structural biology
PhosphoSens
Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations
ROS1
Inhibitor discovery & SARMechanism & structural biology
PhosphoSens
A destabilizing Y891D mutation in activated EGFR impairs sensitivity to kinase inhibition
EGFR and EGFR mutants
Inhibitor discovery & SARMechanism & structural biology
PhosphoSens
Conformation selection by ATP-competitive inhibitors and allosteric communication in ERK2
ERK2
Mechanism & structural biology
PhosphoSens
Demystifying Functional Parameters for Irreversible Enzyme Inhibitors
Covalent inhibitors (EGFR)
Covalent inhibitor kineticsSelectivity & kinome profiling
KinSight services
Development of Highly Potent and Selective Covalent FGFR4 Inhibitors Based on SAr Electrophiles
FGFR4
Covalent inhibitor kineticsInhibitor discovery & SARSelectivity & kinome profiling
PhosphoSens
Development of SYK NanoBRET cellular target engagement assays for gain-of-function variants
SYK and SYK mutants
Inhibitor discovery & SAR
PhosphoSens
Evaluation of STK17B as a cancer immunotherapy target utilizing highly potent and selective small molecule inhibitors
STK17B
Inhibitor discovery & SARSelectivity & kinome profiling
PhosphoSens
Exploring 2-Sulfonylpyrimidine Warheads as Acrylamide Surrogates for Targeted Covalent Inhibition: A BTK Story
BTK
Covalent inhibitor kineticsInhibitor discovery & SARSelectivity & kinome profiling
PhosphoSens
Genomic Discovery and Structure-Activity Exploration of a Novel Family of Enzyme-Activated Covalent Cyclin-Dependent Kinase Inhibitors
CDK1, CDK2, CDK7
Covalent inhibitor kineticsInhibitor discovery & SARSelectivity & kinome profiling
PhosphoSens
Linking ATP and allosteric sites to achieve superadditive binding with bivalent EGFR kinase inhibitors
EGFR and EGFR mutants
Inhibitor discovery & SARMechanism & structural biology
AQT co-authored
NVL-655 Is a Selective and Brain-Penetrant Inhibitor of Diverse ALK-Mutant Oncoproteins, Including Lorlatinib-Resistant Compound Mutations
Multiple (ALK & ALK mutants; TRKA, TRKB, TRKC)
Inhibitor discovery & SARSelectivity & kinome profiling
PhosphoSens
Organ-specific electrophile responsivity mapping in live C. elegans
Multiple
Selectivity & kinome profiling
KinSight services
Potent, Selective, and Orally Bioavailable Quinazoline-Based STK17A/B Dual Inhibitors
STK17A/B
Inhibitor discovery & SARSelectivity & kinome profiling
PhosphoSens
Steady State and Time-Dependent Fluorescent Peptide Assays for Protein Kinases
Multiple
Covalent inhibitor kineticsAssay & sensor technology
PhosphoSens
The mechanism of allosteric activation of SYK kinase derived from multiple phospho-ITAM-bound structures
SYK
Covalent inhibitor kineticsMechanism & structural biology
PhosphoSens
Tilting the Scales toward EGFR Mutant Selectivity: Expanding the Scope of Bivalent "Type V" Kinase Inhibitors
EGFR and EGFR mutants
Inhibitor discovery & SARSelectivity & kinome profilingMechanism & structural biology
PhosphoSens
Vinylpyridine as a Tunable Covalent Warhead Targeting C797 in EGFR
EGFR and EGFR mutants
Covalent inhibitor kineticsInhibitor discovery & SARSelectivity & kinome profiling
PhosphoSens
Bruton's tyrosine kinase inhibition reduces disease severity in a model of secondary progressive autoimmune demyelination
Kinome Profiling (BTK)
Inhibitor discovery & SARSelectivity & kinome profiling
KinSight services
Circulating tumor DNA reveals mechanisms of lorlatinib resistance in patients with relapsed/refractory ALK-driven neuroblastoma
ALK and ALK Mutants
Signaling biology
PhosphoSens
Controlling Ibrutinib's Conformations about Its Heterobiaryl Axis to Increase BTK Selectivity
BTK
Covalent inhibitor kineticsInhibitor discovery & SARSelectivity & kinome profilingMechanism & structural biology
PhosphoSens
Cytomegalovirus cyclin-dependent kinase ortholog vCDK/pUL97 undergoes regulatory interaction with human cyclin H and CDK7 to codetermine viral replication efficiency
pUL97 (CMV vCDK)
Assay & sensor technology
PhosphoSens
Development of a Covalent Inhibitor of c-Jun N-Terminal Protein Kinase (JNK) 2/3 with Selectivity over JNK1
JNK1-JNK3
Covalent inhibitor kineticsInhibitor discovery & SARSelectivity & kinome profiling
PhosphoSens
Linear motif specificity in signaling through p38α and ERK2 mitogen-activated protein kinases
MAPK
Signaling biology
PhosphoSens
Mutation in the Common Docking Domain Affects MAP Kinase ERK2 Catalysis and Stability
ERK2
Signaling biology
PhosphoSens
NVL-520 Is a Selective, TRK-Sparing, and Brain-Penetrant Inhibitor of ROS1 Fusions and Secondary Resistance Mutations
ROS1 and ROS1 mutants
Inhibitor discovery & SARSelectivity & kinome profiling
PhosphoSens
Novel LRR-ROC Motif That Links the N- and C-terminal Domains in LRRK2 Undergoes an Order-Disorder Transition Upon Activation
LRRK2 and LRRK2 mutants
Inhibitor discovery & SAR
PhosphoSens
Phosphorylation of tyrosine 90 in SH3 domain is a new regulatory switch controlling Src kinase
SRC
Mechanism & structural biology
PhosphoSens
Pitfalls and Considerations in Determining the Potency and Mutant Selectivity of Covalent Epidermal Growth Factor Receptor Inhibitors
EGFR
Covalent inhibitor kineticsInhibitor discovery & SARSelectivity & kinome profilingReview
AQT co-authored
Proteome-wide screening for mitogen-activated protein kinase docking motifs and interactors
MAPKs, JNK1, p38α
Signaling biology
PhosphoSens
Structural studies identify angiotensin II receptor blocker-like compounds as branched-chain ketoacid dehydrogenase kinase inhibitors
PDK1-4 (BCKDK)
Inhibitor discovery & SARSelectivity & kinome profilingMechanism & structural biology
KinSight services
Targeting the Brain with Single-Domain Antibodies: Greater Potential Than Stated So Far?
LRRK2
Review
Technology & reviews
The complex impact of cancer-related missense mutations on the stability and on the biophysical and biochemical properties of MAPK1 and MAPK3 somatic variants
MAPK1/MAPK3 variants
Signaling biology
PhosphoSens
Triple targeting of mutant EGFR, COX-2, and 15-LOX: design and synthesis of novel quinazolinone tethered phenyl urea derivatives for anti-inflammatory and anticancer evaluation
EGFR and EGFR L858R/T790M
Inhibitor discovery & SARSelectivity & kinome profiling
PhosphoSens
Biochemical and structural basis for differential inhibitor sensitivity of EGFR with distinct exon 19 mutations
EGFR and EGFR variants
Mechanism & structural biology
PhosphoSens
Casein kinase 1 and disordered clock proteins form functionally equivalent, phospho-based circadian modules in fungi and mammals
CK1
Signaling biology
PhosphoSens
Deactivatable Bisubstrate Inhibitors of Protein Kinases
PKAc
Signaling biology
PhosphoSens
High-throughput mechanistic screening of non-equilibrium inhibitors by a fully automated data analysis pipeline in early drug-discovery
Multiple, names not disclosed
Inhibitor discovery & SARAssay & sensor technology
PhosphoSens
Highly Conserved Interaction Profiles between Clinically Relevant Mutants of the Cytomegalovirus CDK-like Kinase pUL97 and Human Cyclins: Functional Significance of Cyclin H
pUL97 that represents a viral CDK ortholog (vCDK)
Signaling biology
PhosphoSens
Nanobodies as allosteric modulators of Parkinson's disease-associated LRRK2
LRRK2
Inhibitor discovery & SARMechanism & structural biology
PhosphoSens
Neurospora casein kinase 1a recruits the circadian clock protein FRQ via the C-terminal lobe of its kinase domain
CK1a, CK1a- p1, and CK1a- p2
Signaling biology
PhosphoSens
Shining Light on Protein Kinase Biomarkers with Fluorescent Peptide Biosensors
Multiple
Assay & sensor technologyReview
Technology & reviews
Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448)
EGFR and HER2
Inhibitor discovery & SARMechanism & structural biology
AQT co-authored
The CaMKIIα hub ligand Ph-HTBA promotes neuroprotection after focal ischemic stroke by a distinct molecular interaction
CaMKIIα
Signaling biology
PhosphoSens
A Novel High-Throughput FLIPR Tetra-Based Method for Capturing Highly Confluent Kinetic Data for Structure-Kinetic Relationship Guided Early Drug Discovery
Multiple kinases, names not disclosed
Covalent inhibitor kineticsInhibitor discovery & SARAssay & sensor technologyReview
Technology & reviews
A novel GSK-3 inhibitor binds to GSK-3β via a reversible, time and Cys-199-dependent mechanism
GSK-3 (Ser/Thr)
Inhibitor discovery & SAR
PhosphoSens
Cellular model system to dissect the isoform-selectivity of Akt inhibitors
Akt (Ser/Thr)
Covalent inhibitor kineticsInhibitor discovery & SARSelectivity & kinome profilingMechanism & structural biology
PhosphoSens
Design, Synthesis, and Biochemical Evaluation of New Triazole Derivatives as Aurora-A Kinase Inhibitors
Aurora A
Inhibitor discovery & SAR
PhosphoSens
Inhibitors of the Hippo Pathway Kinases STK3/MST2 and STK4/MST1 Have Utility for the Treatment of Acute Myeloid Leukemia
STK3/4 (Ser/Thr)
Inhibitor discovery & SAR
PhosphoSens
Separase cleaves the kinetochore protein Meikin at the meiosis I/II transition
Plk1 (Ser/Thr)
Covalent inhibitor kinetics
PhosphoSens
Synthesis and Pharmacological Characterization of Visabron, a Backbone Cyclic Peptide Dual Antagonist of α4β1 (VLA-4)/α9β1 Integrin for Therapy of Multiple Sclerosis
NTRK1 (TRKA)/ NTRK2 (TRKB) (Tyr)
Inhibitor discovery & SARSelectivity & kinome profilingMechanism & structural biology
AQT co-authored
A fluorescent probe for monitoring PTP-PEST enzymatic activity
Phosphatase non-receptor type 12 (PTPN12 or PTP-PEST)
Assay & sensor technologyPhosphatase biology
Technology origin
Biochemical characterization of tirabrutinib and other irreversible inhibitors of Bruton's tyrosine kinase reveals differences in on - and off - target inhibition
BTK (Tyr)
Covalent inhibitor kineticsSelectivity & kinome profiling
PhosphoSens
Enhancing intracellular accumulation and target engagement of PROTACs with reversible covalent chemistry
BTK
Covalent inhibitor kineticsInhibitor discovery & SAR
PhosphoSens
Insight into the Therapeutic Selectivity of the Irreversible EGFR Tyrosine Kinase Inhibitor Osimertinib through Enzyme Kinetic Studies
EGFR (Tyr) wild-type & oncogenic mutants, Covalent ...
Covalent inhibitor kineticsInhibitor discovery & SARSelectivity & kinome profilingMechanism & structural biology
PhosphoSens
Modular bioengineered kinase sensorsscaffold protein-mediated split-luciferase complementation
PKA
Cell & tissue lysate assaysAssay & sensor technology
PhosphoSens
Neurotropic activity and safety of methylene-cycloalkylacetate (MCA) derivative 3-(3-allyl-2-methylenecyclohexyl) propanoic acid
Multiple kinases (Ser/Thr & Tyr)
Signaling biology
AQT co-authored
Structural Insights into Pseudokinase Domains of Receptor Tyrosine Kinases
RTK pseudokinases
Mechanism & structural biology
PhosphoSens
An ultrasensitive fiveplex activity assay for cellular kinases
AKT, IKKβ, JNK1-3, MK2
Selectivity & kinome profiling
PhosphoSens
Design and synthesis of fluorescent activity probes for protein phosphatases
Not specified
Inhibitor discovery & SARCell & tissue lysate assaysAssay & sensor technologyPhosphatase biology
Technology origin
Enrichment of Aurora B kinase at the inner kinetochore controls outer kinetochore assembly
Aurora B (Ser/Thr)
Signaling biology
PhosphoSens
Safety profiling of genetically engineered Pim-1 kinase overexpression for oncogenicity risk in human c-kit+ cardiac interstitial cells
AKT1-3, CDK1/3-6, CK1, ERK1/2, JNK1-3, p38a/b/g/d, PIM1, ...
Selectivity & kinome profilingAssay & sensor technology
AQT co-authored
Interrogating Protein Phosphatases with Chemical Activity Probes
Phosphatases
Covalent inhibitor kineticsAssay & sensor technologyPhosphatase biologyReview
Technology origin
Phosphorylated immunoreceptor tyrosine-based activation motifs and integrin cytoplasmic domains activate spleen tyrosine kinase via distinct mechanisms
Syk (Tyr)
Mechanism & structural biologyAssay & sensor technology
PhosphoSens
Discovery of N-((3R,4R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR Mutants with Selectivity over Wild-Type EGFR
EGFR (Tyr) wild-type & oncogenic mutants: exon 19 deletion ...
Covalent inhibitor kineticsInhibitor discovery & SARSelectivity & kinome profiling
PhosphoSens
Discovery of a Potent BTK Inhibitor with a Novel Binding Mode by Using Parallel Selections with a DNA-Encoded Chemical Library
BTK (Tyr)
Inhibitor discovery & SARMechanism & structural biology
PhosphoSens
Measuring Kinase Activity-A Global Challenge
Multiple
Selectivity & kinome profilingReview
Technology & reviews
Quantification of Cell Signaling Networks Using Kinase Activity Chemosensors
Multiple
Cell & tissue lysate assaysAssay & sensor technologyReview
Technology origin
An algebraic model to determine substrate kinetic parameters by global nonlinear fit of progress curves
EGFR (Tyr)
Assay & sensor technology
AQT co-authored
Bistability of a coupled Aurora B kinase-phosphatase system in cell division
Aurora A & B (Ser/Thr)
Assay & sensor technologyPhosphatase biology
PhosphoSens
Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants
EGFR & Mutants (Tyr), Covalent Inhibitors
Covalent inhibitor kineticsInhibitor discovery & SARSelectivity & kinome profiling
PhosphoSens
Disulfide-activated protein kinase G Iα regulates cardiac diastolic relaxation and fine-tunes the Frank-Starling response
PKG (Ser/Thr)
Signaling biology
PhosphoSens
Nitidine chloride suppresses epithelial-to-mesenchymal transition in osteosarcoma cell migration and invasion through Akt/GSK-3β/Snail signaling pathway
GSK-3beta (Ser/Thr)
Signaling biology
PhosphoSens
Phosphodiesterase 5 Inhibition Limits Doxorubicin-induced Heart Failure by Attenuating Protein Kinase G Iα Oxidation
PKG (Ser/Thr)
Signaling biology
PhosphoSens
Phosphorylation of the dimeric cytoplasmic domain of the phytosulfokine receptor, PSKR1
PSKR1 (Ser/Thr)
Signaling biology
PhosphoSens
Temporal Analysis of PP2A Phosphatase Activity During Insulin Stimulation Using a Direct Activity Probe
PP2A (Ser/Thr Phosphatase)
Cell & tissue lysate assaysAssay & sensor technologyPhosphatase biology
Technology origin
A real-time, fluorescence-based assay for Rho-associated protein kinase activity
ROCK (Ser/Thr)
Inhibitor discovery & SARAssay & sensor technology
Technology origin
Cyclin-dependent kinase 5 regulates degranulation in human eosinophils
CDK5 (Ser/Thr)
Inhibitor discovery & SAR
PhosphoSens
Design and evaluation of a real-time activity probe for focal adhesion kinase
FAK (Tyr)
Inhibitor discovery & SARSelectivity & kinome profilingAssay & sensor technology
Technology origin
First Selective Small Molecule Inhibitor of FGFR4 for the Treatment of Hepatocellular Carcinomas with an Activated FGFR4 Signaling Pathway
FGFR4 (Tyr), Covalent Inhibitors
Covalent inhibitor kineticsInhibitor discovery & SARSelectivity & kinome profiling
PhosphoSens
Fluorescent Reporters and Biosensors for Probing the Dynamic Behavior of Protein Kinases
Multiple
Assay & sensor technologyReview
Technology & reviews
Interrogating Endogenous Protein Phosphatase Activity with Rationally Designed Chemosensors
PTP1B (Tyr Phosphatase)
Cell & tissue lysate assaysAssay & sensor technologyPhosphatase biology
Technology origin
Peptide-based biosensors
Multiple
Selectivity & kinome profilingAssay & sensor technologyReview
Technology & reviews
Protein kinase profiling assays: a technology review
Multiple
Selectivity & kinome profilingReview
Technology & reviews
A continuous and direct assay to monitor leucine-rich repeat kinase 2 activity
LRRK2 (Ser/Thr)
Inhibitor discovery & SARAssay & sensor technology
PhosphoSens
An algebraic model for the kinetics of covalent enzyme inhibition at low substrate concentrations
EGFR (Tyr), Covalent Inhibitors
Covalent inhibitor kinetics
PhosphoSens
Cyclometalated iridium(III)-β-carboline complexes as potent autophagy-inducing agents
CDK1 & 2 (Ser/Thr)
Signaling biology
PhosphoSens
Design, synthesis, and evaluation of a selective chemosensor for leucine-rich repeat kinase 2
LRRK2 (Ser/Thr)
Inhibitor discovery & SARAssay & sensor technology
Technology origin
Differential sensing of MAP kinases using SOX-peptides
MAPKs, ERK1/2, JNK1/2/3, and
Assay & sensor technology
Technology origin
Discovery of novel AKT inhibitors with enhanced anti-tumor effects in combination with the MEK inhibitor
AKT 1, 2 & 3 (Ser/Thr)
Inhibitor discovery & SARSelectivity & kinome profiling
PhosphoSens
In vitro and in vivo characterization of irreversible mutant-selective EGFR inhibitors that are wild-type sparing
EGFR (Tyr), Covalent Inhibitors
Covalent inhibitor kineticsInhibitor discovery & SAR
PhosphoSens
Microfluidic probe for single-cell analysis in adherent tissue culture
AKT (Ser/Thr), Microfluidics
Signaling biology
PhosphoSens
Olive phenolics as c-Met inhibitors: (-)-Oleocanthal attenuates cell proliferation, invasiveness, and tumor growth in breast cancer models
cMET/HGFR (Tyr)
Inhibitor discovery & SAR
PhosphoSens
Protein kinase C and extracellular signal-regulated kinase regulate movement, attachment, pairing and egg release in Schistosoma mansoni
PKC (Ser/Thr)
Signaling biology
PhosphoSens
Quantification of a Pharmacodynamic ERK End Point in Melanoma Cell Lysates: Toward Personalized Precision Medicine
MAPKs - ERK1& 2 (Ser/Thr)
Inhibitor discovery & SARCell & tissue lysate assaysAssay & sensor technology
Technology origin
SAICAR induces protein kinase activity of PKM2 that is necessary for sustained proliferative signaling of cancer cells
MAPKs - ERK1 & 2 (Ser/Thr)
Signaling biology
PhosphoSens
Selective mitogen activated protein kinase activity sensors through the application of directionally programmable D domain motifs
p38abdg (Ser/Thr)
Inhibitor discovery & SARSelectivity & kinome profilingAssay & sensor technology
Technology origin
Single cell kinase signaling assay using pinched flow coupled droplet microfluidics
EGFR (Tyr). Microfluidics
Inhibitor discovery & SARAssay & sensor technology
PhosphoSens
Structure-based optimization of tyrosine kinase inhibitor CLM3. Design, synthesis, functional evaluation, and molecular modeling studies
VEGFR2/KDR and RET (Tyr)
Inhibitor discovery & SAR
PhosphoSens
Synthesis and biological evaluation of pyrido[2,3-d]pyrimidine-2,4-dione derivatives as eEF-2K inhibitors
eEF-2K (Ser/Thr)
Inhibitor discovery & SAR
Technology origin
The spleen tyrosine kinase (Syk) regulates Alzheimer amyloid-β production and Tau hyperphosphorylation
SYK (Tyr)
Mechanism & structural biology
PhosphoSens
Covalent EGFR inhibitor analysis reveals importance of reversible interactions to potency and mechanisms of drug resistance
EGFR (Tyr), Covalent Inhibitors
Covalent inhibitor kineticsInhibitor discovery & SAR
PhosphoSens
Design, synthesis and biological evaluation of new classes of thieno[3,2-d]pyrimidinone and thieno[1,2,3]triazine as inhibitor of vascular endothelial growth factor receptor-2 (VEGFR-2)
VEGFR-2/KDR (Tyr)
Inhibitor discovery & SAR
PhosphoSens
Discovery and characterization of LY2784544, a small-molecule tyrosine kinase inhibitor of JAK2V617F
JAK2 (Tyr)
Inhibitor discovery & SARSelectivity & kinome profilingAssay & sensor technology
PhosphoSens
Discovery of novel insulin-like growth factor-1 receptor inhibitors with unique time-dependent binding kinetics
IGF1R (Tyr)
Inhibitor discovery & SAR
AQT co-authored
Fluorescent sensors of protein kinases: from basics to biomedical applications
Multiple
Mechanism & structural biologyAssay & sensor technologyReview
Technology & reviews
Glucose sensor O-GlcNAcylation coordinates with phosphorylation to regulate circadian clock
GSK3beta (Ser/Thr)
Assay & sensor technology
PhosphoSens
High-throughput screens for eEF-2 kinase
eEF-2K (Ser/Thr)
Inhibitor discovery & SARAssay & sensor technology
PhosphoSens
In-situ generation of differential sensors that fingerprint kinases and the cellular response to their expression
MAPKs - ERK- 1/2, JNK-3 & p38g (Ser/Thr)
Assay & sensor technology
Technology origin
Inhibition of Btk with CC-292 provides early pharmacodynamic assessment of activity in mice and humans
BTK (Tyr), Covalent Inhibitors
Covalent inhibitor kineticsInhibitor discovery & SAR
PhosphoSens
Rapid discovery of a novel series of Abl kinase inhibitors by application of an integrated microfluidic synthesis and screening platform
ABL (Tyr), Microfluidics
Inhibitor discovery & SAR
PhosphoSens
Structural characterization of the RLCK family member BSK8: a pseudokinase with an unprecedented architecture
BSK5 & 8 (Ser/Thr)
Mechanism & structural biology
PhosphoSens
Biophysical and mechanistic insights into novel allosteric inhibitor of spleen tyrosine kinase
SYK (Tyr)
Selectivity & kinome profilingMechanism & structural biology
PhosphoSens
Identification of a hidden strain switch provides clues to an ancient structural mechanism in protein kinases
Aurora (Ser/Thr)
Inhibitor discovery & SARMechanism & structural biology
PhosphoSens
Interrogating signaling nodes involved in cellular transformations using kinase activity probes
Not specified
Cell & tissue lysate assaysAssay & sensor technology
Technology origin
Spatially coordinated kinase signaling regulates local axon degeneration
GSK-3 (Ser/Thr)
Signaling biology
PhosphoSens
Targeting GSK3 from Ustilago maydis: type-II kinase inhibitors as potential antifungals
GSK-3 (Ser/Thr)
Inhibitor discovery & SARSelectivity & kinome profilingMechanism & structural biology
PhosphoSens
Adiponectin inhibits osteoclastogenesis and bone resorption via APPL1-mediated suppression of Akt1
AKT (Ser/Thr)
Phosphatase biology
PhosphoSens
CHEK2 contribution to hereditary breast cancer in non-BRCA families
CHEK2 (Ser/Thr)
Signaling biology
PhosphoSens
Discovery and characterization of a cell-permeable, small-molecule c-Abl kinase activator that binds to the myristoyl binding site
ABL (Tyr)
Inhibitor discovery & SARMechanism & structural biology
PhosphoSens
Protein kinase Cδ inactivation inhibits cellular proliferation and decreases survival in human neuroendocrine tumors
PKC-d (Ser/Thr)
Inhibitor discovery & SARSelectivity & kinome profiling
PhosphoSens
Redox modification of Akt mediated by the dopaminergic neurotoxin MPTP, in mouse midbrain, leads to down-regulation of pAkt
AKT (Ser/Thr)
Phosphatase biology
PhosphoSens
Study of the PDK1/AKT signaling pathway using selective PDK1 inhibitors, HCS, and enhanced biochemical assays
PDK1, AKT1 & 2. (Ser/Thr)
Signaling biology
PhosphoSens
The phytosulfokine (PSK) receptor is capable of guanylate cyclase activity and enabling cyclic GMP-dependent signaling in plants
PSKR1 (Ser/Thr)
Signaling biology
PhosphoSens
Trypanosoma brucei glycogen synthase kinase-3, a target for anti-trypanosomal drug development: a public-private partnership to identify novel leads
GSK-3 (HS & Tbru, Ser/Thr)
Inhibitor discovery & SARSelectivity & kinome profiling
PhosphoSens
A p38α-selective chemosensor for use in unfractionated cell lysates
Not specified
Inhibitor discovery & SARSelectivity & kinome profilingCell & tissue lysate assaysAssay & sensor technology
Technology origin
Characterization of PF-4708671, a novel and highly specific inhibitor of p70 ribosomal S6 kinase (S6K1)
S6K1 (Ser/Thr)
Inhibitor discovery & SAR
PhosphoSens
Characterization of irreversible kinase inhibitors by directly detecting covalent bond formation: a tool for dissecting kinase drug resistance
Src (Tyr), Covalent Inhibitors
Covalent inhibitor kinetics
PhosphoSens
Fluorescent peptide assays for protein kinases
Multiple
Assay & sensor technologyReview
Technology & reviews
Protein kinase A regulates GDNF/RET-dependent but not GDNF/Ret-independent ureteric bud outgrowth from the Wolffian duct
PKA (Ser/Thr)
Signaling biology
PhosphoSens
Role of DAB2IP in modulating epithelial-to-mesenchymal transition and prostate cancer metastasis
GSK-3b (Ser/Thr)
Mechanism & structural biology
PhosphoSens
Swiprosin-1/EFhd2 controls B cell receptor signaling through the assembly of the B cell receptor, Syk, and phospholipase C gamma2 in membrane rafts
SYK (Ser/Thr)
Mechanism & structural biology
PhosphoSens
The presynaptic component of the serotonergic system is required for clozapine's efficacy
CHEK2 (Ser/Thr)
Signaling biology
PhosphoSens
Bacillus anthracis edema toxin suppresses human macrophage phagocytosis and cytoskeletal remodeling via the protein kinase A and exchange protein activated by cyclic AMP pathways
PKA (Ser/Thr)
Signaling biology
PhosphoSens
Biochemical characterization of GSK1070916, a potent and selective inhibitor of Aurora B and Aurora C kinases with an extremely long residence time1
Aurora B & C (Ser/Thr), Covalent Inhibitors
Inhibitor discovery & SAR
PhosphoSens
Design of a bioactive cell-penetrating peptide: when a transduction domain does more than transduce
MAPKAPK2/M K2 (Ser/Thr)
Inhibitor discovery & SAR
PhosphoSens
Enzymatic characterization of c-Met receptor tyrosine kinase oncogenic mutants and kinetic studies with aminopyridine and triazolopyrazine inhibitors
cMET (HGFR; Tyr)
Inhibitor discovery & SARSelectivity & kinome profiling
PhosphoSens
Epidermal growth factor receptor cooperates with Src family kinases in acquired resistance to cetuximab
Src-Family Kinases (Tyr), IP-kinase assays
Signaling biology
PhosphoSens
Inhibition of angiogenesis by extracellular protein kinase A
PKA (Ser/Thr)
Signaling biology
PhosphoSens
Microfluidic concentration-enhanced cellular kinase activity assay
MAPKAPK2/M K2 & PKA (Ser/Thr). Microfluidics
Cell & tissue lysate assays
PhosphoSens
Monitoring protein kinases in cellular media with highly selective chimeric reporters
Not specified
Cell & tissue lysate assays
Technology origin
Response and resistance to MEK inhibition in leukaemias initiated by hyperactive Ras
MAPKAPK2/M K2 (Ser/Thr)
Signaling biology
PhosphoSens
Syk tyrosine 317 negatively regulates osteoclast function via the ubiquitin-protein isopeptide ligase activity of Cbl
SYK (Tyr)
Signaling biology
PhosphoSens
Synthesis of red-shifted 8-hydroxyquinoline derivatives using click chemistry and their incorporation into phosphorylation chemosensors
Not specified
Assay & sensor technology
Technology origin
The endogenous inhibitor of Akt, CTMP, is critical to ischemia-induced neuronal death
AKT (Ser/Thr)
Signaling biology
PhosphoSens
A rapid method for generation of selective Sox-based chemosensors of Ser/Thr kinases using combinatorial peptide libraries
Not specified
Assay & sensor technology
Technology origin
Evidence for PI-3K-dependent migration of Th17-polarized cells in response to CCR2 and CCR6 agonists
(Ser/Thr)
Signaling biology
PhosphoSens
Homogenous fluorescent assays for characterizing small-molecule activators of AMP-activated protein kinase (AMPK)
AMPK (Ser/Thr)
Inhibitor discovery & SARMechanism & structural biologyAssay & sensor technology
PhosphoSens
Kinetic assay for characterization of spleen tyrosine kinase activity and inhibition with recombinant kinase and crude cell lysates
SYK (Tyr)
Mechanism & structural biologyCell & tissue lysate assaysAssay & sensor technology
AQT co-authored
Molecular mechanism of the Syk activation switch
SYK (Tyr)
Mechanism & structural biologyCell & tissue lysate assaysAssay & sensor technology
PhosphoSens
Recognition-domain focused chemosensors: versatile and efficient reporters of protein kinase activity
Not specified
Selectivity & kinome profilingMechanism & structural biologyCell & tissue lysate assaysAssay & sensor technology
Technology origin
Structure-based tailoring of compound libraries for high-throughput screening: discovery of novel EphB4 kinase inhibitors
EphB4 (Tyr)
Inhibitor discovery & SARAssay & sensor technology
PhosphoSens
Apolipoprotein E interrupts interleukin-1beta signaling in vascular smooth muscle cells
PKA (Ser/Thr)
Signaling biology
PhosphoSens
Steady state kinetics of spleen tyrosine kinase investigated by a real time fluorescence assay
SYK (Tyr)
Mechanism & structural biologyAssay & sensor technology
PhosphoSens
Optimal Sox-based fluorescent chemosensor design for serine/threonine protein kinases
Not specified
Assay & sensor technology
Technology origin
A multiplexed homogeneous fluorescence-based assay for protein kinase activity in cell lysates
Not specified
Cell & tissue lysate assaysAssay & sensor technology
Technology origin
Versatile fluorescence probes of protein kinase activity
Not specified
Assay & sensor technology
Technology origin
Derivatives of 8-hydroxy-2-methylquinoline are powerful prototypes for zinc sensors in biological systems
Not specified
Assay & sensor technology
Technology origin
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