Moonlighting with WDR5: a cellular multitasker
AP Guarnaccia, WP Tansey - Journal of clinical medicine, 2018 - mdpi.com
WDR5 is a highly conserved WD40 repeat-containing protein that is essential for proper
regulation of multiple cellular processes. WDR5 is best characterized as a core scaffolding …
regulation of multiple cellular processes. WDR5 is best characterized as a core scaffolding …
Structure, function and inhibition of critical protein–protein interactions involving mixed lineage leukemia 1 and its fusion oncoproteins
Abstract Mixed lineage leukemia 1 (MLL1, also known as MLL or KMT2A) is an important
transcription factor and histone-H3 lysine-4 (H3K4) methyltransferase. It is a master …
transcription factor and histone-H3 lysine-4 (H3K4) methyltransferase. It is a master …
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 …
Displacement of WDR5 from chromatin by a WIN site inhibitor with picomolar affinity
ER Aho, J Wang, RD Gogliotti, GC Howard, J Phan… - Cell reports, 2019 - cell.com
The chromatin-associated protein WDR5 is a promising target for pharmacological inhibition
in cancer. Drug discovery efforts center on the blockade of the" WIN site" of WDR5, a well …
in cancer. Drug discovery efforts center on the blockade of the" WIN site" of WDR5, a well …
Modes of interaction of KMT2 histone H3 lysine 4 methyltransferase/COMPASS complexes with chromatin
A Bochynska, J Lüscher-Firzlaff, B Lüscher - Cells, 2018 - mdpi.com
Regulation of gene expression is achieved by sequence-specific transcriptional regulators,
which convey the information that is contained in the sequence of DNA into RNA …
which convey the information that is contained in the sequence of DNA into RNA …
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 …