[PDF][PDF] The versatility of squaramides: From supramolecular chemistry to chemical biology

LA Marchetti, LK Kumawat, N Mao, JC Stephens… - Chem, 2019 - cell.com
This review covers recent advances in the use of the squaramide moiety in chemical
research. We focus on the varied applications of squaramides under the broad headings of …

Bacterial transcription as a target for antibacterial drug development

C Ma, X Yang, PJ Lewis - Microbiology and Molecular Biology …, 2016 - Am Soc Microbiol
Transcription, the first step of gene expression, is carried out by the enzyme RNA
polymerase (RNAP) and is regulated through interaction with a series of protein transcription …

Structural biology of bacterial RNA polymerase

KS Murakami - Biomolecules, 2015 - mdpi.com
Since its discovery and characterization in the early 1960s (Hurwitz, J. The discovery of RNA
polymerase. J. Biol. Chem. 2005, 280, 42477–42485), an enormous amount of biochemical …

[PDF][PDF] Structural basis of transcription inhibition by fidaxomicin (lipiarmycin A3)

W Lin, K Das, D Degen, A Mazumder, D Duchi, D Wang… - Molecular cell, 2018 - cell.com
Fidaxomicin is an antibacterial drug in clinical use for treatment of Clostridium difficile
diarrhea. The active ingredient of fidaxomicin, lipiarmycin A3 (Lpm), functions by inhibiting …

Antibiotics from myxobacteria

TF Schäberle, F Lohr, A Schmitz, GM König - Natural product reports, 2014 - pubs.rsc.org
Covering: up to the end of 2013 Myxobacteria produce a vast range of structurally diverse
natural products with prominent biological activities. Here, we provide a detailed description …

Squaric acid analogues in medicinal chemistry

J Chasák, V Šlachtová, M Urban, L Brulíková - European Journal of …, 2021 - Elsevier
In this review, we summarize the published data on squaric acid analogues with a special
focus on their use in medicinal chemistry and as potential drugs. Squaric acid is an …

[HTML][HTML] Bacterial RNA polymerase-DNA interaction—the driving force of gene expression and the target for drug action

J Lee, S Borukhov - Frontiers in molecular biosciences, 2016 - frontiersin.org
DNA-dependent multisubunit RNA polymerase (RNAP) is the key enzyme of gene
expression and a target of regulation in all kingdoms of life. It is a complex multifunctional …

Synergy of streptogramin antibiotics occurs independently of their effects on translation

J Noeske, J Huang, NB Olivier… - Antimicrobial agents …, 2014 - Am Soc Microbiol
Streptogramin antibiotics are divided into types A and B, which in combination can act
synergistically. We compared the molecular interactions of the streptogramin combinations …

Mutant Alleles of lptD Increase the Permeability of Pseudomonas aeruginosa and Define Determinants of Intrinsic Resistance to Antibiotics

CJ Balibar, M Grabowicz - Antimicrobial agents and …, 2016 - Am Soc Microbiol
Gram-negative bacteria provide a particular challenge to antibacterial drug discovery due to
their cell envelope structure. Compound entry is impeded by the lipopolysaccharide (LPS) of …

X-ray Crystal Structures of Escherichia coli RNA Polymerase with Switch Region Binding Inhibitors Enable Rational Design of Squaramides with an Improved …

V Molodtsov, PR Fleming, CJ Eyermann… - Journal of medicinal …, 2015 - ACS Publications
Squaramides constitute a novel class of RNA polymerase inhibitors of which genetic
evidence and computational modeling previously have suggested an inhibitory mechanism …