{With the|Using the|With all the|Together with the} {idea|concept|thought|notion} of exploiting metal-templated reactions {to achieve|to attain} selective modification of cysteines in proteins for antibacterial applications, an organometallic cyclometalated Au(III) compound was explored {in a|inside a|within a} competitive chemoproteomic {approach|method|strategy} {based on|according to|depending on|determined by} the isoDTB-ABPP (isotopically labelled desthiobiotin azide-activity-based protein profiling) {technology|technologies} in S. aureus cell extracts. {In this|Within this} way, {more|much more|a lot more|far more|additional|extra} than {100|one hundred} ligandable cysteines {where|exactly where} identified, of which {10|ten} {were|had been|have been} close to functional {sites|websites|web sites|internet sites|web-sites|web pages} of proteins encoded by {essential|important|crucial|vital|necessary|critical} genes indicating {potential|possible|prospective} for antibiotic {development|improvement}. Interestingly, {more|much more|a lot more|far more|additional|extra} than 50% {of the|from the|in the|on the|with the|of your} identified ligandable {sites|websites|web sites|internet sites|web-sites|web pages} {were|had been|have been} not engaged by organic α-chloroacetamides {in a|inside a|within a} {previous|prior|earlier|preceding} study, indicating that organometallic compounds expand the ligandable space in bacteria. A {selected|chosen} interaction identified by isoDTB-ABPP was validated {using|utilizing|making use of|employing|working with|applying} an enzyme activity assay, and intact protein mass spectrometry showed that cysteine arylation of an unprecedented target {occurs|happens} {with the|using the|with all the|together with the} studied compound. The obtained {results|outcomes|final results|benefits} constitute the proof-of-concept that this {family|family members|loved ones|household} of organogold compounds has {potential|possible|prospective} for therapeutic protein targeting {via|by way of|through|by means of} selective, covalent modification of cysteine residues in bacteria. {Looking|Searching|Seeking|Hunting} {more|much more|a lot more|far more|additional|extra} broadly, our study demonstrates that the targets of cyclometalated gold compounds {can be|may be|could be|might be|is often|is usually} studied proteome-wide with competitive residue-specific chemoproteomics enabling the expansion {of the|from the|in the|on the|with the|of your} {known|recognized|identified} ligandable proteome to {sites|websites|web sites|internet sites|web-sites|web pages} {that can|that may|that will|that could|which will|which can} be addressed with this compound class. 210539-05-2 site 2′-Deoxyadenosine web PMID:32180353
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