The DNA-encoded library (DEL) is a powerful hit generation tool for chemical biology and drug discovery; however, the optimization of DEL hits remained a daunting challenge for the medicinal chemistry community. In this study, hit compounds targeting the WIN binding domain of WDR5 were discovered by the initial three-cycle linear DEL selection, and their potency was further enhanced by a cascade DEL selection from the focused DEL designed based on the original first run DEL hits. As expected, these new compounds from the second run of focused DEL were more potent WDR5 inhibitors in the protein binding assay confirmed by the off-DNA synthesis. Interestingly, selected inhibitors exhibited good antiproliferative activity in two human acute leu...
The discovery of small organic ligands or biologics capable of modulating biological processes remai...
Werner syndrome (WS), an autosomal recessive genetic disorder, displays accelerated clinical symptom...
The DNA methyltransferases (DNMTs) found in mammals include DNMT1, DNMT3A, and DNMT3B and are attrac...
The DNA-encoded library (DEL) is a powerful hit generation tool for chemical biology and drug discov...
WDR5 is a chromatin-regulatory scaffold protein overexpressed in various cancers and a potential epi...
WD repeat domain 5 (WDR5) is a member of the WD40-repeat protein family that plays a critical role i...
WDR5 is a chromatin-regulatory scaffold protein overexpressed in various cancers and a potential epi...
The WD40-repeat protein WDR5 scaffolds various epigenetic writers and is a critical component of the...
The chromatin-associated protein WDR5 is a promising target for pharmacological inhibition in cancer...
The frequent deregulation of MYC and its elevated expression via multiple mechanisms drives cells to...
The chromatin-associated protein WDR5 is a promising target for pharmacological inhibition in cancer...
SummaryDNA-encoded chemical libraries are promising tools for the discovery of ligands toward protei...
WD repeat domain 5 (WDR5) is a prominent target for pharmacological inhibition in cancer through its...
Protein kinases are essential in cell signaling pathways and are well-validated targets for cancer t...
The chromatin-associated protein WDR5 (WD repeat domain 5) is an essential cofactor for MYC and a co...
The discovery of small organic ligands or biologics capable of modulating biological processes remai...
Werner syndrome (WS), an autosomal recessive genetic disorder, displays accelerated clinical symptom...
The DNA methyltransferases (DNMTs) found in mammals include DNMT1, DNMT3A, and DNMT3B and are attrac...
The DNA-encoded library (DEL) is a powerful hit generation tool for chemical biology and drug discov...
WDR5 is a chromatin-regulatory scaffold protein overexpressed in various cancers and a potential epi...
WD repeat domain 5 (WDR5) is a member of the WD40-repeat protein family that plays a critical role i...
WDR5 is a chromatin-regulatory scaffold protein overexpressed in various cancers and a potential epi...
The WD40-repeat protein WDR5 scaffolds various epigenetic writers and is a critical component of the...
The chromatin-associated protein WDR5 is a promising target for pharmacological inhibition in cancer...
The frequent deregulation of MYC and its elevated expression via multiple mechanisms drives cells to...
The chromatin-associated protein WDR5 is a promising target for pharmacological inhibition in cancer...
SummaryDNA-encoded chemical libraries are promising tools for the discovery of ligands toward protei...
WD repeat domain 5 (WDR5) is a prominent target for pharmacological inhibition in cancer through its...
Protein kinases are essential in cell signaling pathways and are well-validated targets for cancer t...
The chromatin-associated protein WDR5 (WD repeat domain 5) is an essential cofactor for MYC and a co...
The discovery of small organic ligands or biologics capable of modulating biological processes remai...
Werner syndrome (WS), an autosomal recessive genetic disorder, displays accelerated clinical symptom...
The DNA methyltransferases (DNMTs) found in mammals include DNMT1, DNMT3A, and DNMT3B and are attrac...