[HTML][HTML] A synthetic antibiotic class overcoming bacterial multidrug resistance

MJ Mitcheltree, A Pisipati, EA Syroegin, KJ Silvestre… - Nature, 2021 - nature.com
The dearth of new medicines effective against antibiotic-resistant bacteria presents a
growing global public health concern. For more than five decades, the search for new …

An antibiotic preorganized for ribosomal binding overcomes antimicrobial resistance

KJY Wu, BIC Tresco, A Ramkissoon, EV Aleksandrova… - Science, 2024 - science.org
We report the design conception, chemical synthesis, and microbiological evaluation of the
bridged macrobicyclic antibiotic cresomycin (CRM), which overcomes evolutionarily diverse …

Structural basis of Cfr-mediated antimicrobial resistance and mechanisms to evade it

EV Aleksandrova, KJY Wu, BIC Tresco… - Nature Chemical …, 2024 - nature.com
The bacterial ribosome is an essential drug target as many clinically important antibiotics
bind and inhibit its functional centers. The catalytic peptidyl transferase center (PTC) is …

Expression of Bacillus subtilis ABCF antibiotic resistance factor VmlR is regulated by RNA polymerase pausing, transcription attenuation, translation attenuation and …

H Takada, ZF Mandell, H Yakhnin… - Nucleic Acids …, 2022 - academic.oup.com
Since antibiotic resistance is often associated with a fitness cost, bacteria employ multi-
layered regulatory mechanisms to ensure that expression of resistance factors is restricted to …

Lincosamide Antibiotics: Structure, Activity, and Biosynthesis

T Mori, I Abe - ChemBioChem, 2024 - Wiley Online Library
Lincosamides are naturally occurring antibiotics isolated from Streptomyces sp. Currently,
lincomycin A and its semisynthetic analogue clindamycin are used as clinical drugs. Due to …

Macrolide, lincosamide, glycopeptide, and other antibacterial antibiotics

Y Qian, S Mobashery, JF Fisher - Medicinal Chemistry of Chemotherapeutic …, 2023 - Elsevier
The golden age of antibiotic discovery was marked not only by the discovery of numerous
new antibiotic structures but also by the recurring correlation of these antibiotics to two …

Synthetic oxepanoprolinamide iboxamycin is active against Listeria monocytogenes despite the intrinsic resistance mediated by VgaL/Lmo0919 ABCF ATPase

T Brodiazhenko, KJ Turnbull, KJY Wu… - JAC-antimicrobial …, 2022 - academic.oup.com
Background Listeriosis is a food-borne disease caused by the Gram-positive Bacillota
(Firmicute) bacterium Listeria monocytogenes. Clinical L. monocytogenes isolates are often …

A method for tritiation of iboxamycin permits measurement of its ribosomal binding

KJY Wu, D Klepacki, AS Mankin, AG Myers - Bioorganic & Medicinal …, 2023 - Elsevier
Hydrogen-tritium exchange is widely employed for radioisotopic labeling of molecules of
biological interest but typically involves the metal-promoted exchange of sp 2-hybridized …

[HTML][HTML] Structural basis of Cfr-mediated antimicrobial resistance and mechanisms for its evasion

EV Aleksandrova, KJY Wu, BIC Tresco, EA Syroegin… - bioRxiv, 2023 - ncbi.nlm.nih.gov
The ribosome is an essential drug target as many classes of clinically important antibiotics
bind and inhibit its functional centers. The catalytic peptidyl transferase center (PTC) is …

Synthesis of lincosamide analogues via oxime resin aminolysis

T Tremblay, P Haguette, G Robert-Scott, JB Alcée… - Synlett, 2023 - thieme-connect.com
In this work, the synthetic development of an oxime resin aminolysis to lincosamide
analogues is described. This synthetic endeavor hinges on a protecting-group-free strategy …