Antibiotic adjuvants: diverse strategies for controlling drug‐resistant pathogens

EE Gill, OL Franco… - Chemical biology & drug …, 2015 - Wiley Online Library
The growing number of bacterial pathogens that are resistant to numerous antibiotics is a
cause for concern around the globe. There have been no new broad‐spectrum antibiotics …

Fragment-based drug discovery and molecular docking in drug design

T Wang, MB Wu, ZJ Chen, H Chen… - Current …, 2015 - ingentaconnect.com
Fragment-based drug discovery (FBDD) has caused a revolution in the process of drug
discovery and design, with many FBDD leads being developed into clinical trials or …

Ebselen as a potent covalent inhibitor of New Delhi metallo-β-lactamase (NDM-1)

E Wai-chiáChan - Chemical communications, 2015 - pubs.rsc.org
We report the discovery of a promising NDM-1 inhibitor, ebselen, through a cell-based
screening approach. Enzymatic kinetic study and ESI-MS analysis suggested that ebselen …

Multiple ligand detection and affinity measurement by ultrafiltration and mass spectrometry analysis applied to fragment mixture screening

S Qin, Y Ren, X Fu, J Shen, X Chen, Q Wang, X Bi… - Analytica Chimica …, 2015 - Elsevier
Binding affinity of a small molecule drug candidate to a therapeutically relevant biomolecular
target is regarded the first determinant of the candidate's efficacy. Although the ultrafiltration …

Identification of tyrosinase specific inhibitors from Xanthium strumarium fruit extract using ultrafiltration-high performance liquid chromatography

Z Wang, SH Hwang, B Huang, SS Lim - Journal of Chromatography B, 2015 - Elsevier
In this study, a strategy based on ultrafiltration-high performance liquid chromatography
coupled with diode array detection (UF-HPLC-DAD) was proposed for screening tyrosinase …

A ligand-observed mass spectrometry approach integrated into the fragment based lead discovery pipeline

X Chen, S Qin, S Chen, J Li, L Li, Z Wang, Q Wang… - Scientific reports, 2015 - nature.com
In fragment-based lead discovery (FBLD), a cascade combining multiple orthogonal
technologies is required for reliable detection and characterization of fragment binding to the …

Cysteine and its derivatives as New Delhi metallo-beta-lactamase-1 inhibitors

CG Bai, YT Xu, NN Li, JH Wang, C Yang… - Current Enzyme …, 2015 - ingentaconnect.com
Nearly all antibiotics are ineffective to the antibiotic-resistant bacteria New Delhi metallo-
beta-lactamase-1 (NDM-1), one of the most important reasons is that antibiotics can be …