UNIGE document Scientific Article
previous document  unige:85263  next document
add to browser collection
Title

Screening for covalent inhibitors using DNA-display of small molecule libraries functionalized with cysteine reactive moieties

Authors
Published in MedChemComm. 2016, vol. 7, no. 7, p. 1340-1351
Abstract DNA-encoded chemical libraries are increasingly used to identify leads for drug discovery or chemical biology. Despite the resurging interest in covalent inhibitors, libraries are typically designed with synthon filtered out for reactive functionalities that can engage a target through covalent interactions. Herein, we report the synthesis of two libraries containing Michael acceptors to identify cysteine reactive ligands. We developed a simple procedure to discriminate between covalent and high affinity non-covalent inhibitors using DNA display of the library in a microarray format. The methodology was validated with known covalent and high affinity non-covalent kinase inhibitors. Screening of the library revealed novel covalent inhibitors for MEK2 and ERBB2.
Identifiers
Full text
Article (Published version) (4.9 MB) - document accessible for UNIGE members only Limited access to UNIGE
Other version: http://xlink.rsc.org/?DOI=C6MD00242K
Structures
Research group Groupe Winssinger
Citation
(ISO format)
ZAMBALDO, Claudio et al. Screening for covalent inhibitors using DNA-display of small molecule libraries functionalized with cysteine reactive moieties. In: MedChemComm, 2016, vol. 7, n° 7, p. 1340-1351. https://archive-ouverte.unige.ch/unige:85263

153 hits

10 downloads

Update

Deposited on : 2016-07-13

Export document
Format :
Citation style :