7l0a
From Proteopedia
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=7l0a FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7l0a OCA], [https://pdbe.org/7l0a PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7l0a RCSB], [https://www.ebi.ac.uk/pdbsum/7l0a PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7l0a ProSAT]</span></td></tr> | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=7l0a FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7l0a OCA], [https://pdbe.org/7l0a PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7l0a RCSB], [https://www.ebi.ac.uk/pdbsum/7l0a PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7l0a ProSAT]</span></td></tr> | ||
</table> | </table> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Carboxy ester prodrugs are widely employed to increase oral absorption and potency of phosphonate antibiotics. Prodrugging can mask problematic chemical features that prevent cellular uptake and may enable tissue-specific compound delivery. However, many carboxy ester promoieties are rapidly hydrolyzed by serum esterases, limiting their therapeutic potential. While carboxy ester-based prodrug targeting is feasible, it has seen limited use in microbes as microbial esterase-specific promoieties have not been described. Here we identify the bacterial esterases, GloB and FrmB, that activate carboxy ester prodrugs in Staphylococcus aureus. Additionally, we determine the substrate specificities for FrmB and GloB and demonstrate the structural basis of these preferences. Finally, we establish the carboxy ester substrate specificities of human and mouse sera, ultimately identifying several promoieties likely to be serum esterase-resistant and microbially labile. These studies will enable structure-guided design of antistaphylococcal promoieties and expand the range of molecules to target staphylococcal pathogens. | ||
| + | |||
| + | Structure-guided microbial targeting of antistaphylococcal prodrugs.,Miller JJ, Shah IT, Hatten J, Barekatain Y, Mueller EA, Moustafa AM, Edwards RL, Dowd CS, Planet PJ, Muller FL, Jez JM, Odom John AR Elife. 2021 Jul 19;10. pii: 66657. doi: 10.7554/eLife.66657. PMID:34279224<ref>PMID:34279224</ref> | ||
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| + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| + | </div> | ||
| + | <div class="pdbe-citations 7l0a" style="background-color:#fffaf0;"></div> | ||
| + | == References == | ||
| + | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
Revision as of 06:31, 25 August 2021
Crystal structure of s-formylglutathione hydrolase (FrmB) from Staphylococcus aureus, apoenzyme
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