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Showing results 1 to 4 of 4

Industry article

Bi-functional particles for real-time acidification and proteolysis multiplex assay in macrophages

Authors : Alejandre, Alba Méndez (2023)

Phagosome acidification and proteolysis are essential processes in the immune response to contain and eliminate pathogens. In recent years, there has been an increased desire for a rapid and accurate method of assessing these processes in real-time. Here, we outline the development of a multiplexed assay that allows simultaneous monitoring of phagosome acidification and proteolysis in the same sample using silica beads conjugated to pHrodo...

Ebooks (Sách điện tử)

Characterizing glucokinase variant mechanisms using a multiplexed abundance assay

Authors : Gersing, Sarah (2023)

Amino acid substitutions can perturb protein activity in multiple ways. Understanding 14 their mechanistic basis may pinpoint how residues contribute to protein function. Here, we 15 characterize the mechanisms of human glucokinase (GCK) variants, building on our previous 16 comprehensive study on GCK variant activity. We assayed the abundance of 95% of GCK 17 missense and nonsense variants, and found that 43% of hypoactive variants have&#x...

Journal article

Discovery of DTX3L inhibitors through a homogeneous FRET-based assay that monitors formation and removal of poly-ubiquitin chains

Authors : Rodríguez, Carlos Vela- (2023)

Ubiquitination is a complex and reversible protein post-translational modification in which the subsequent action of enzymes belonging to three different families, broadly referred to as E1, E2 and E3, results in the covalent linking of ubiquitin to a target protein. While this linkage is canonically an isopeptide bond between the C-terminus of ubiquitin and the lysine residue of the target protein, Ser, Thr, and Tyr can also be susceptible to&...

Journal article

System-wide profiling by proteome integral solubility alteration assay of drug residence times for target characterization

Authors : Sabatier, Pierre (2023)

Most drugs used in the clinic and drug candidates target multiple proteins, and thus detailed characterization of their efficacy targets is required. While current methods rely on quantitative measurements at thermodynamic equilibrium, kinetic parameters such as the residence time of a drug on its target provide a better proxy for efficacy in vivo. Here, we present Residence Time Proteome Integral Solubility Alteration (ResT-PISA) assay which provides monitor...