Skip to Content
MDPIMDPI
Biomolecules
Submit to Biomolecules

Biomolecules, Volume 10, Issue 5

2020 May - 148 articles

Cover Story: β-Lactamase inhibitors (BLIs) are used in combination with existing β-lactam antibiotics to overcome β-lactamase-mediated antibiotic resistance. Boronic acid transition state analog inhibitors (BATSIs) are promising BLIs that form a reversible dative bond with the active site serine and mimic the tetrahedral transition state. Here, we report microbiological, biochemical, and structural studies of four BATSIs with a class C cephamycinase, FOX-4. X-ray crystal structures reveal that the compound, SM23, adopts different binding modes across class C β-lactamases. Comparison of the FOX-4/SM23 and FOX-4/cefoxitin complexes provides a rationale for the rapid turnover of cephamycins by FOX-4. Our analyses suggest new opportunities for the design of novel transition-state analogs of class C enzymes to be used as BLIs. View this paper.
  • Issues are regarded as officially published after their release is announced to the table of contents alert mailing list .
  • You may sign up for email alerts to receive table of contents of newly released issues.
  • PDF is the official format for papers published in both, html and pdf forms. To view the papers in pdf format, click on the "PDF Full-text" link, and use the free Adobe Reader to open them.

Articles

There are no articles in this issue yet.

Get Alerted

Add your email address to receive forthcoming issues of this journal.

XFacebookLinkedIn
Biomolecules - ISSN 2218-273X
Imprint
Download Flyer