Mutational fitness landscape and drug resistance

J Flynn, N Samant, G Schneider-Nachum… - Current opinion in …, 2023 - Elsevier
Robust technology has been developed to systematically quantify fitness landscapes that
provide valuable opportunities to improve our understanding of drug resistance and define …

CRISPR/Cas9 recombineering‐mediated deep mutational scanning of essential genes in Escherichia coli

A Choudhury, JA Fenster, RG Fankhauser… - Molecular Systems …, 2020 - embopress.org
Deep mutational scanning can provide significant insights into the function of essential
genes in bacteria. Here, we developed a high‐throughput method for mutating essential …

Small molecule regulated sgRNAs enable control of genome editing in E. coli by Cas9

RS Iwasaki, BA Ozdilek, AD Garst, A Choudhury… - Nature …, 2020 - nature.com
CRISPR-Cas9 has led to great advances in gene editing for a broad spectrum of
applications. To further the utility of Cas9 there have been efforts to achieve temporal control …

Predicting drug resistance using deep mutational scanning

G Pines, RG Fankhauser, CA Eckert - Molecules, 2020 - mdpi.com
Drug resistance is a major healthcare challenge, resulting in a continuous need to develop
new inhibitors. The development of these inhibitors requires an understanding of the …

Potential repurposing of four FDA approved compounds with antiplasmodial activity identified through proteome scale computational drug discovery and in vitro assay

BN Diallo, T Swart, HC Hoppe, Ö Tastan Bishop… - Scientific Reports, 2021 - nature.com
Malaria elimination can benefit from time and cost-efficient approaches for antimalarials
such as drug repurposing. In this work, 796 DrugBank compounds were screened against …

Inhibition of DXR in the MEP pathway with lipophilic N-alkoxyaryl FR900098 analogs

D Bague, R Wang, D Hodge, MO Mikati… - RSC Medicinal …, 2024 - pubs.rsc.org
In Mycobacterium tuberculosis (Mtb) and Plasmodium falciparum (Pf), the methylerythritol
phosphate (MEP) pathway is responsible for isoprene synthesis. This pathway and its …

Antimicrobial prodrug activation by the staphylococcal glyoxalase GloB

MO Mikati, JJ Miller, DM Osbourn… - ACS infectious …, 2020 - ACS Publications
With the rising prevalence of multidrug resistance, there is an urgent need to develop novel
antibiotics. Many putative antibiotics demonstrate promising in vitro potency but fail in vivo …

Antibacterial Activity of Peptide Derivatives of Phosphinothricin against Multidrug-Resistant Klebsiella pneumoniae

MV Demiankova, F Giovannercole, MA Khomutov… - Molecules, 2023 - mdpi.com
The fast spread of bacteria that are resistant to many classes of antibiotics (multidrug
resistant) is a global threat to human and animal health with a worrisome scenario ahead …

[HTML][HTML] Enzymatic Synthesis of Biologically Active H-Phosphinic Analogue of α-Ketoglutarate

VL Filonov, MA Khomutov, YV Tkachev, AV Udod… - Biomolecules, 2024 - mdpi.com
Amino acid analogues with a phosphorus-containing moiety replacing the carboxylic group
are promising sources of biologically active compounds. The H-phosphinic group, with …

Highly efficient libraries design for saturation mutagenesis

G Pines, A Pines, CA Eckert - Synthetic Biology, 2022 - academic.oup.com
Saturation mutagenesis is a semi-rational approach for protein engineering where sites are
saturated either entirely or partially to include amino acids of interest. We previously …