Valerie Reader

TL;DR: Quantitative profiling of the drugs Imatinib, dasatinib and bosutinib in K562 cells confirms known targets including ABL and SRC family kinases and identifies the receptor tyrosine kinase DDR1 and the oxidoreductase NQO2 as novel targets of imatinib.

TL;DR: This work revealed the selectivity with which 16 HDAC inhibitors target multiple HDAC complexes scaffolded by ELM-SANT domain subunits, including a novel mitotic deacetylase complex (MiDAC) and identified several non-HDAC targets for hydroxamate inhibitors.

TL;DR: In this paper, the authors present methods for the characterization of enzymes or of enzyme-compound complexes, wherein the enzyme is obtained from a protein preparation with the help of at least one broad spectrum ligand immobilized on a solid support and wherein the enzymes are characterized by mass spectrometry.

TL;DR: A chemoproteomics approach based on a combination of unselective active-site ligands tethered to beads enabling affinity capturing of around 40 different dioxygenase enzymes from human cells indicates that intracellular competition by endogenous cofactors and high active site similarity present substantial challenges for drug discovery for this target class.

TL;DR: In this paper, the present invention relates to compounds of formula (I), wherein X1 to X5, Z1 to Z3, Y0, Y1, RY1,RY2 and RY3 have the meaning as cited in the description and the claims.