PUBLICATION

Antisense Oligonucleotide Activation via Enzymatic Antibiotic Resistance Mechanism

Authors
Darrah, K.E., Albright, S., Kumbhare, R., Tsang, M., Chen, J.K., Deiters, A.
ID
ZDB-PUB-230617-32
Date
2023
Source
ACS Chemical Biology   18(10): 2176-2182 (Journal)
Registered Authors
Chen, James K., Tsang, Michael
Keywords
none
MeSH Terms
  • Animals
  • Anti-Bacterial Agents/metabolism
  • Anti-Bacterial Agents/pharmacology
  • Bacteria/metabolism
  • Cephalosporins/metabolism
  • Drug Resistance, Microbial
  • Gene Expression
  • Mammals/genetics
  • Mammals/metabolism
  • Microbial Sensitivity Tests
  • Oligonucleotides, Antisense*/pharmacology
  • Zebrafish*/genetics
  • beta-Lactamase Inhibitors
  • beta-Lactamases/metabolism
PubMed
37326511 Full text @ ACS Chem. Biol.
Abstract
The structure and mechanism of the bacterial enzyme β-lactamase have been well-studied due to its clinical role in antibiotic resistance. β-Lactamase is known to hydrolyze the β-lactam ring of the cephalosporin scaffold, allowing a spontaneous self-immolation to occur. Previously, cephalosporin-based sensors have been developed to evaluate β-lactamase expression in both mammalian cells and zebrafish embryos. Here, we present a circular caged morpholino oligonucleotide (cMO) activated by β-lactamase-mediated cleavage of a cephalosporin motif capable of silencing the expression of T-box transcription factor Ta (tbxta), also referred to as no tail a (ntla), eliciting a distinct, observable phenotype. We explore the use of β-lactamase to elicit a biological response in aquatic embryos for the first time and expand the utility of cephalosporin as a cleavable linker beyond targeting antibiotic-resistant bacteria. The addition of β-lactamase to the current suite of enzymatic triggers presents unique opportunities for robust, orthogonal control over endogenous gene expression in a spatially resolved manner.
Genes / Markers
Figures
Show all Figures
Expression
Phenotype
Mutations / Transgenics
Human Disease / Model
Sequence Targeting Reagents
Fish
Antibodies
Orthology
Engineered Foreign Genes
Mapping