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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 
ProteomicsLabel-free quantitative phosphoproteomics of ΔB-Raf:ER cells treated with U0126 or 4-HT
ΔB-Raf:ER cells were treated with 10 µM U0126 or 1 µM 4-HT for 30 min. The cells were lysed in 6 M guanidine-HCl containing 100 mM HEPES-NaOH (pH7.5), 10 mM TCEP, and 40 mM CAA. The lysates were dissolved by heating and sonication and then centrifuged. The supernatants were recovered, and proteins (...
ORGANISM(S): Mus Musculus (mouse) 
2022-03-03 | PXD028723 | JPOST Repository
ProteomicsMembrane-Based Affinity Purification to Identify Target Proteins of a Small-Molecule Drug
We employ MaxLFQ to relatively quantify fold changes of proteins in two groups.
ORGANISM(S): Homo Sapiens (ncbitaxon:9606) 
2020-05-27 | MSV000085483 | MassIVE
UnknownLabel-free target identification using in-gel fluorescence difference via thermal stability shift.
Not available
S-EPMC5369521 | biostudies-literature
ProteomicsIdentification of ABL Kinase Substrates by Kinase Assay Linked Phosphoproteomics and Multiple Drug Treatments
The kinase assay linked phosphoproteomics (KALIP) strategy was used to identify direct substrates of the Abelson tyrosine kinase (ABL). First, kinase assays using peptides and proteins from chronic myelogenous leukemia cells and recombinant ABL were done to identify kinase substrates in vitro. The A...
ORGANISM(S): Homo Sapiens (human) 
2019-03-20 | PXD005431 | JPOST Repository
UnknownLabel-free target identification reveals oxidative DNA damage as the mechanism of a selective cytotoxic agent.
Not available
S-EPMC6438152 | biostudies-literature
ProteomicsEvaluation of phospho-tyrosine antibodies for label-free phosphoproteomics
In the past decade multiple tyrosine kinase inhibitors (TKIs) have been implemented in standard treatment regimens for patients with cancer. Unfortunately the majority of patients develops resistance to these drugs. Reliable tools for analysis of pharmacodynamic effects and drug resistance mechanism...
ORGANISM(S): Homo sapiens (Human) 
2015-12-09 | PXD001565 | Pride
Human Glioblastoma Single-shot Label-free U87 Phosphoproteomics Phosphotyrosine Ptyr ip 
ProteomicsBACE1 KO mouse CSF LC-MSMS - Label-free Quantitative Proteomics of Mouse Cerebrospinal Fluid Detects β-Site APP Cleaving Enzyme (BACE1) Protease Substrates In Vivo
Analysis of murine cerebrospinal fluid (CSF) by quantitative mass spectrometry is challenging due to low CSF volume, low total protein concentration and the presence of highly abundant proteins such as albumin. We demonstrate that the CSF proteome of individual mice can be analyzed in a quantitative...
ORGANISM(S): Mus musculus (Mouse) 
2015-10-12 | PXD001514 | Pride
Mouse csf Csf Label-free quantification 
ProteomicsChemical proteomics with novel fully functionalized fragments and stringent target prioritization identifies the glutathione-dependent isomerase GSTZ1 as a lung cancer target
Photoreactive fragment-like probes have been applied to discover target proteins that constitute novel cellular vulnerabilities and to identify viable chemical hits for drug discovery. Through forming covalent bonds, functionalized probes can achieve stronger target engagement and require less effor...
ORGANISM(S): Homo sapiens (Human) 
2024-04-05 | PXD035201 | Pride
Photoreactive probes Lung cancer Gstz1 Chemical proteomics 
ProteomicsStreamlined analysis of drug targets by proteome integral solubility alteration indicates organ-specific engagement
Proteins are the primary targets of almost all small molecule drugs. However, even the most selectively designed drugs can potentially target several unknown proteins. Identification of potential drug targets can facilitate design of new drugs and repurposing of existing ones. Current state-of-the-a...
ORGANISM(S): Homo sapiens (Human) Rattus norvegicus (Rat) 
2024-10-16 | PXD050784 | Pride
Drug target Small molecule Target identification Chemical proteomics Tpp Pisa 
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