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The key objectives of this study were to evaluate the selectivity profiles of three MELK inhibitors, 8a, HTH, and OTS, using a cell-based assay, in order to identify a highly selective inhibitor to subsequently investigate MELK function. To this end, we utilized a chemical proteomics approach called...
ORGANISM(S): Homo sapiens (Human) 
2020-01-09 | PXD016022 | Pride
In order to improve elution of proteins from the column, to reduce the cost as well as the hands on time of the analysis, we here present a modification of the Multiplexed Inhibitor Bead assay (MIB assay), where we elute the proteins from beads containing covalently bound inhibitors using trypsin di...
ORGANISM(S): Homo Sapiens (ncbitaxon:9606) 
2017-03-29 | MSV000080744 | MassIVE
Protein kinases (collectively termed the kinome) represent one of the most tractable drug targets in the pursuit of new and effective cancer treatments. However, less than 20% of the kinome is currently being explored as primary targets for cancer therapy, leaving the majority of the kinome untarget...
ORGANISM(S): Homo sapiens (Human) 
2020-09-30 | PXD020357 | Pride
Here we describe a bead-based method capable of profiling tyrosine kinase phosphorylations in a multiplexed, high-throughput and low-cost manner. This approach allows for the discovery of tyrosine kinase-activating events, even when the DNA sequence is wild-type. In an effort to pilot the establishm...
ORGANISM(S): Homo sapiens 
Purpose: Management of gastrointestinal stromal tumor (GIST) has been revolutionized by the identification of activating mutations in KIT and PDGFRA and the clinical application of receptor tyrosine kinase (RTK) inhibitors in the advanced disease setting. Stratification of GIST into molecularly defi...
ORGANISM(S): Homo sapiens (Human) 
2021-09-09 | PXD020720 | Pride
In order to improve elution of proteins from the column, to reduce the cost as well as the hands on time of the analysis, we here present a modification of the Multiplexed Inhibitor Bead assay (MIB assay), where we elute the proteins from beads containing covalently bound inhibitors using trypsin di...
ORGANISM(S): Hordeum vulgare (Barley) 
2017-02-13 | PXD005286 | Pride
In order to improve elution of proteins from the column, to reduce the cost as well as the hands on time of the analysis, we here present a modification of the Multiplexed Inhibitor Bead assay (MIB assay), where we elute the proteins from beads containing covalently bound inhibitors using trypsin di...
ORGANISM(S): Homo sapiens (Human) 
2017-02-13 | PXD005402 | Pride
Inhibition of the HER2/ERBB2 receptor is a keystone to treating HER2-positive malignancies, particularly breast cancer, but a significant fraction of HER2-positive (HER2+) breast cancers recur or fail to respond. Anti-HER2 monoclonal antibodies, like trastuzumab or pertuzumab, and ATP active site in...
ORGANISM(S): Homo sapiens (Human) 
2021-04-09 | PXD021865 | Pride
Neurofibromatosis type 1 (NF1) is the most common autosomal dominant disorder, affecting 1 in 3,500 individuals worldwide and predisposing to cancer. Germline mutations in the NF1 gene, encoding the p21Ras GTPase-activating protein (GAP) neurofibromin, are the underlying cause for NF1. Somatic inact...
ORGANISM(S): Mus musculus (Mouse) 
2020-11-19 | PXD019138 | Pride
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