Inhibition of Nonessential Bacterial Targets : Discovery of a Novel Serine O-Acetyltransferase Inhibitor

Show simple item record Pinto de Magalhães, Joana Franko, Nina Raboni, Samanta Annunziato, Giannamaria Tammela, Päivi Bruno, Agostino Bettati, Stefano Mozzarelli, Andrea Pieroni, Marco Cambanini, Barbara Costantino, Gabriele 2021-02-12T22:51:37Z 2021-12-18T03:45:28Z 2020-05-14
dc.identifier.citation Pinto de Magalhães , J , Franko , N , Raboni , S , Annunziato , G , Tammela , P , Bruno , A , Bettati , S , Mozzarelli , A , Pieroni , M , Cambanini , B & Costantino , G 2020 , ' Inhibition of Nonessential Bacterial Targets : Discovery of a Novel Serine O -Acetyltransferase Inhibitor ' , ACS Medicinal Chemistry Letters , vol. 11 , no. 5 , pp. 790-797 .
dc.identifier.other PURE: 132798092
dc.identifier.other PURE UUID: 67b929e8-0a8c-416e-8602-aae6e02d9770
dc.identifier.other WOS: 000535281200028
dc.identifier.other ORCID: /0000-0003-4697-8066/work/78162425
dc.description.abstract In Upsilon-proteobacteria and Actinomycetales, cysteine biosynthetic enzymes are indispensable during persistence and become dispensable during growth or acute infection. The biosynthetic machinery required to convert inorganic sulfur into cysteine is absent in mammals; therefore, it is a suitable drug target. We searched for inhibitors of Salmonella serine acetyltransferase (SAT), the enzyme that catalyzes the rate-limiting step of L-cysteine biosynthesis. The virtual screening of three ChemDiv focused libraries containing 91 243 compounds was performed to identify potential SAT inhibitors. Scaffold similarity and the analysis of the overall physicochemical properties allowed the selection of 73 compounds that were purchased and evaluated on the recombinant enzyme. Six compounds displaying an IC50 en
dc.format.extent 8
dc.language.iso eng
dc.relation.ispartof ACS Medicinal Chemistry Letters
dc.rights unspecified
dc.rights.uri info:eu-repo/semantics/openAccess
dc.subject Adjuvant therapies
dc.subject Antimicrobial resistance
dc.subject COMPLEX
dc.subject Cysteine biosynthesis
dc.subject L-CYSTEINE
dc.subject Nonessential targets
dc.subject Serine acetyltransferase
dc.subject 317 Pharmacy
dc.subject 116 Chemical sciences
dc.subject 11832 Microbiology and virology
dc.title Inhibition of Nonessential Bacterial Targets : Discovery of a Novel Serine O-Acetyltransferase Inhibitor en
dc.type Article
dc.contributor.organization Division of Pharmaceutical Biosciences
dc.contributor.organization Drug Research Program
dc.contributor.organization Bioactivity Screening Group
dc.contributor.organization University Management
dc.description.reviewstatus Peer reviewed
dc.relation.issn 1948-5875
dc.rights.accesslevel openAccess
dc.type.version acceptedVersion

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