Imidazoles as potential anticancer agents: An update on recent studies
P Sharma, C LaRosa, J Antwi, R Govindarajan… - Molecules, 2021 - mdpi.com
Nitrogen-containing heterocyclic rings are common structural components of marketed
drugs. Among these heterocycles, imidazole/fused imidazole rings are present in a wide …
drugs. Among these heterocycles, imidazole/fused imidazole rings are present in a wide …
Direct mapping of ligandable tyrosines and lysines in cells with chiral sulfonyl fluoride probes
Advances in chemoproteomic technology have revealed covalent interactions between
small molecules and protein nucleophiles, primarily cysteine, on a proteome-wide scale …
small molecules and protein nucleophiles, primarily cysteine, on a proteome-wide scale …
Targeting WD repeat-containing protein 5 (WDR5): a medicinal chemistry perspective
X Chen, J Xu, X Wang, G Long, Q You… - Journal of medicinal …, 2021 - ACS Publications
WD repeat-containing protein 5 (WDR5) is a member of the WD40 protein family, and it is
widely involved in various biological activities and not limited to epigenetic regulation in …
widely involved in various biological activities and not limited to epigenetic regulation in …
A selective WDR5 degrader inhibits acute myeloid leukemia in patient-derived mouse models
Interactions between WD40 repeat domain protein 5 (WDR5) and its various partners such
as mixed lineage leukemia (MLL) and c-MYC are essential for sustaining oncogenesis in …
as mixed lineage leukemia (MLL) and c-MYC are essential for sustaining oncogenesis in …
Discovery of a dual WDR5 and Ikaros PROTAC degrader as an anti-cancer therapeutic
Abstract WD repeat domain 5 (WDR5), an integral component of the MLL/KMT2A lysine
methyltransferase complex, is critically involved in oncogenesis and represents an attractive …
methyltransferase complex, is critically involved in oncogenesis and represents an attractive …
Structure-based discovery of potent WD repeat domain 5 inhibitors that demonstrate efficacy and safety in preclinical animal models
KB Teuscher, S Chowdhury… - Proceedings of the …, 2023 - National Acad Sciences
WD repeat domain 5 (WDR5) is a core scaffolding component of many multiprotein
complexes that perform a variety of critical chromatin-centric processes in the nucleus …
complexes that perform a variety of critical chromatin-centric processes in the nucleus …
Discovery, evaluation and mechanism study of WDR5-targeted small molecular inhibitors for neuroblastoma
Q Han, X Zhang, P Ren, L Mei, W Lin, L Wang… - Acta Pharmacologica …, 2023 - nature.com
Neuroblastoma is the most common and deadliest tumor in infancy. WDR5 (WD Repeat
Domain 5), a critical factor supporting an N-myc transcriptional complex via its WBM site and …
Domain 5), a critical factor supporting an N-myc transcriptional complex via its WBM site and …
Discovery of potent and selective WDR5 proteolysis targeting chimeras as potential therapeutics for pancreatic cancer
As a core chromatin-regulatory scaffolding protein, WDR5 mediates numerous protein–
protein interactions (PPIs) with other partner oncoproteins. However, small-molecule …
protein interactions (PPIs) with other partner oncoproteins. However, small-molecule …
Discovery of potent orally bioavailable WD repeat domain 5 (WDR5) inhibitors using a pharmacophore-based optimization
WD repeat domain 5 (WDR5) is a nuclear scaffolding protein that forms many biologically
important multiprotein complexes. The WIN site of WDR5 represents a promising …
important multiprotein complexes. The WIN site of WDR5 represents a promising …
WDR5 represents a therapeutically exploitable target for cancer stem cells in glioblastoma
Glioblastomas (GBMs) are heterogeneous, treatment-resistant tumors driven by populations
of cancer stem cells (CSCs). However, few molecular mechanisms critical for CSC …
of cancer stem cells (CSCs). However, few molecular mechanisms critical for CSC …