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ProteomicsChemical genetics strategy to profile kinase target engagement reveals role of FES in neutrophil phagocytosis via SYK activation
Identification of covalently bound protein targets of probe WEL028 in wild-type or mutant HL-60 cells.
ORGANISM(S): Homo sapiens (Human) 
2020-05-25 | PXD018270 | Pride
Target validation Chemical genetics Inhibitor Target engagement Chemical biology Kinase Probe 
ProteomicsABPP using chemical proteomics in Alzheimer's Disease and Resilience
pulldown on enzymes targeted by serine hydrolase probes tetrahydrolipstatin-biotin and fluorophosphonate biotin probe in lysates from the frontal cortex of 36 patients (12 conrol, 12 Alzheimer's, 12 Resilient). below is the abstract: Alzheimer’s Disease (AD) is the most common form of dementia. Wh...
ORGANISM(S): Homo sapiens (Human) 
2026-02-09 | PXD057993 | Pride
Abpp Alzheimer's disease Serine hydrolases 
ProteomicsDiscovery of a NAPE-PLD inhibitor that modulates emotional behavior in mice
N‑acylethanolamines (NAEs), which include the endocannabinoid anandamide, represent an important family of signaling lipids in the brain. The lack of chemical probes that modulate NAE biosynthesis in living systems hamper the understanding of the biological role of these lipids. Using a high-through...
ORGANISM(S): Homo sapiens (Human) 
2020-05-15 | PXD017586 | Pride
Lipids Drug discovery Endocannabinoids Chemical biology 
ProteomicsProfiling the anandamide reuptake inhibitor WOBE437
Anandamide, or N-arachidonoylethanolamine (AEA), is a signaling lipid that modulates neurotransmitter release via activation of the cannabinoid receptor type 1 (CB1R) in the brain. Termination of anandamide signaling is thought to be mediated via a facilitated cellular reuptake process utilizing an ...
ORGANISM(S): Mus musculus (Mouse) 
2022-05-04 | PXD031488 | Pride
Abpp Photoaffinity Proteomics Endocannabinoid 
ProteomicsCHEMICAL PROTEOMIC ANALYSIS OF ENDOCANNABINOID HYDROLASE ACTIVITY IN NIEMANN-PICK TYPE C MOUSE BRAIN
The endocannabinoid system is considered to be an endogenous protective system in various neurodegenerative diseases. Niemann-Pick Type C is a neurodegenerative disease in which the role of the endocannabinoid system has not been studied yet. Here, we report the endocannabinoid hydrolase activity in...
ORGANISM(S): Mus musculus (Mouse) 
2018-04-19 | PXD008979 | Pride
Mouse Brain Orbitrap Activity-based protein profiling Niemann-pick type c Synapt 
ProteomicsMapping in vivo target interaction profiles of covalent inhibitors using chemical proteomics with label-free quantification
Activity-based protein profiling (ABPP) has emerged as a valuable chemical proteomics method to guide the therapeutic development of covalent drugs by assessing their on-target engagement and off-target activity. Recently, we reported on the establishment, by ABPP, of the serine hydrolase interactio...
ORGANISM(S): Mus musculus (Mouse) 
2018-02-23 | PXD007965 | Pride
Activity-based protein profiling  covalent inhibitors  chemical proteomics  label-free quantification  target engagement 
ProteomicsEmploying Sterculic Acid–a naturally occurring 1, 2-cyclopropene fatty acid–for live-cell imaging of lipids by inverse electron-demand Diels-Alder reaction
To allow the study of unsaturated free fatty acids in live cells, we here report the use of sterculic acid, a 1,2-cyclopropene containing oleic acid analogue, as a bioorthogonal probe. We here show that this lipid can be readily taken up by dendritic cells without toxic side-effects, and that it can...
ORGANISM(S): Mus musculus (Mouse) 
2023-04-28 | PXD033831 | Pride
Lipidation Ptm Bioorthogonal Sterculic Cyclopropene 
ProteomicsActivity-based protein profiling in human M2 macrophages using DHA-based photoaffinity probes
17-Hydroxydocosahexaenoic acid (17-HDHA), an oxidative metabolite of the fish oil constituent docosahexaenoic acid (DHA, 22:6 n-3), is a signaling lipid with anti-inflammatory properties. The molecular mechanisms underlying the biological effect of 17-HDHA are poorly understood. Here, we report the ...
ORGANISM(S): Homo sapiens (Human) 
2023-04-28 | PXD027600 | Pride
Human Abpp Photoaffinity Macrophage 
ProteomicsEstablishing an activity-based protein profiling platform to screen in situ kinase inhibitor engagement
Activity-based protein profiling is a powerful tool to study target engagement in complex biological environments. XO44 is a chemical probe based on the scaffold of a promiscuous kinase binder, which covalently reacts with a conserved lysine in the ATP-binding pocket of kinases. Pretreatment of cell...
ORGANISM(S): Homo sapiens (Human) 
2025-04-09 | PXD055387 | Pride
Drug discovery Kinase Phosphoproteomics Abpp 
ProteomicsA selective photoaffinity probe enables assessment of cannabinoid CB2 receptor expression and ligand engagement in human cells
Chemical tools and methods that report on G protein-coupled receptor (GPCR) expression levels and receptor occupancy by small molecules are highly desirable. We report the development of LEI121 as a photoreactive probe to study the type 2 cannabinoid receptor (CB2R), a promising GPCR to treat tissue...
ORGANISM(S): Homo sapiens (Human) Cricetulus griseus (Chinese hamster) (Cricetulus barabensis griseus) 
2018-06-15 | PXD008460 | Pride
Target engagement Cb2 receptor Gpcrs Photo-affinity labeling Bio-orthogonal chemistry 
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