WebNov 9, 2024 · Compound binding to cysteine 252 on MSH3 was confirmed using chemoproteomic reactive cysteine profiling. Overall, these results suggested that chemoproteomic DNA bead pull-downs enable the specific readout of transcription factor activity and can identify functional “hotspots” on DNA binders toward expanding the …
Reactive-cysteine profiling for drug discovery - PubMed
WebMar 18, 2024 · A reactive-cysteine profiling method, known as isoTOP-ABPP, has the potential to aid in two key aspects of covalent irreversible inhibitor discovery: (1) to identify novel ligandable cysteines for covalent modulation of protein function; and, (2) to evaluate both on and off-target cysteine engagement so as to minimize risks associated with off ... WebCysteine is unique among all protein-coding amino acids, owing to its intrinsically high nucleophilicity. The cysteinyl thiol group can be covalently modified by a broad range of redox mechanisms or by various electrophiles derived from … coteo
Cysteine-reactive probes and their use in chemical …
WebMar 4, 2024 · To comprehensively assess reactive-cysteine-containing proteins, the development of chemical proteomic probes to label cysteine residues in human cells is an important objective. ... C-Sul particularly has no inhibitory effects on cell viability, enabling its application in proteomic profiling of reactive cysteine residues under biorelevant ... WebOur method, Streamlined Cysteine Activity-Based Protein Profiling (SLC-ABPP), achieved a 42-fold improvement in sample throughput, corresponding to profiling library members at a depth of >8,000 reactive cysteine sites in 18 min per compound. We applied it to identify proteome-wide targets of covalent inhibitors to mutant KRASG12C and BTK. WebApr 14, 2024 · SNO refers to the formation of nitroso moieties in cysteine residues, and SNO ... thus affecting the citric acid cycle and leading to changes in the concentration of reactive ... Liu T, Camp DG 2nd, Smith RD, et al. Resin-assisted enrichment of thiols as a general strategy for proteomic profiling of cysteine-based reversible modifications. ... mafalda ricca parma