Sortase A: an ideal target for anti-virulence drug development

S Cascioferro, M Totsika, D Schillaci - Microbial pathogenesis, 2014 - Elsevier
Sortase A is a membrane enzyme responsible for the anchoring of surface-exposed proteins
to the cell wall envelope of Gram-positive bacteria. As a well-studied member of the sortase …

Sortase transpeptidases: insights into mechanism, substrate specificity, and inhibition

KW Clancy, JA Melvin, DG McCafferty - Peptide Science, 2010 - Wiley Online Library
Gram‐positive bacteria pose a serious healthcare threat. The growing antibiotic resistance
epidemic creates a dire need for new antibiotic targets. The sortase family of enzymes is a …

New substructure filters for removal of pan assay interference compounds (PAINS) from screening libraries and for their exclusion in bioassays

JB Baell, GA Holloway - Journal of medicinal chemistry, 2010 - ACS Publications
This report describes a number of substructural features which can help to identify
compounds that appear as frequent hitters (promiscuous compounds) in many biochemical …

Pd-catalyzed intermolecular C–H amination with alkylamines

EJ Yoo, S Ma, TS Mei, KSL Chan… - Journal of the American …, 2011 - ACS Publications
C–H amination of N-aryl benzamides with O-benzoyl hydroxylamines has been achieved
with either Pd (II) or Pd (0) catalysts. Furthermore, we demonstrate that secondary amines …

Sortase A inhibitors: recent advances and future perspectives

S Cascioferro, D Raffa, B Maggio… - Journal of medicinal …, 2015 - ACS Publications
Here, we describe the most promising small synthetic organic compounds that act as potent
Sortase A inhibitors and cater the potential to be developed as antivirulence drugs. Sortase …

Non-innocent additives in a palladium (II)-catalyzed C–H bond activation reaction: insights into multimetallic active catalysts

M Anand, RB Sunoj, HF Schaefer III - Journal of the American …, 2014 - ACS Publications
The role of a widely employed additive (AgOAc) in a palladium acetate-catalyzed ortho-C–H
bond activation reaction has been examined using the M06 density functional theory. A new …

Productive steps toward an antimicrobial targeting virulence

AK Barczak, DT Hung - Current opinion in microbiology, 2009 - Elsevier
Targeting virulence factors has gained increasing attention as a potential approach to new
antibiotics. Small molecule inhibitors of virulence have been shown to change the course of …

Development and prospects of dedicated tracers for the molecular imaging of bacterial infections

A Bunschoten, MM Welling, MF Termaat… - Bioconjugate …, 2013 - ACS Publications
Bacterial infections have always been, and still are, a major global healthcare problem. For
accurate treatment it is of upmost importance that the location (s), severity, type of bacteria …

Sorting out the superbugs: Potential of sortase A inhibitors among other antimicrobial strategies to tackle the problem of antibiotic resistance

N Zrelovs, V Kurbatska, Z Rudevica, A Leonchiks… - Antibiotics, 2021 - mdpi.com
Rapid spread of antibiotic resistance throughout the kingdom bacteria is inevitably bringing
humanity towards the “post-antibiotic” era. The emergence of so-called “superbugs” …

Chemical biology of sortase a inhibition: A gateway to anti-infective therapeutic agents

R Sapra, AK Rajora, P Kumar, GP Maurya… - Journal of Medicinal …, 2021 - ACS Publications
Staphylococcus aureus is the leading cause of hospital-acquired infections. The enzyme
sortase A, present on the cell surface of S. aureus, plays a key role in bacterial virulence …