WD repeat domain 5 inhibitors for cancer therapy: not what you think

AM Weissmiller, SW Fesik, WP Tansey - Journal of Clinical Medicine, 2024 - mdpi.com
WDR5 is a conserved nuclear protein that scaffolds the assembly of epigenetic regulatory
complexes and moonlights in functions ranging from recruiting MYC oncoproteins to …

KMT2C and KMT2D aberrations in breast cancer

E Tinsley, P Bredin, S Toomey, BT Hennessy… - Trends in Cancer, 2024 - cell.com
Abstract KMT2C and KMT2D are histone lysine methyltransferases responsible for the
monomethylation of histone 3 lysine 4 (H3K4) residues at gene enhancer sites. KMT2C/D …

Discovery of potent and selective WDR5 proteolysis targeting chimeras as potential therapeutics for pancreatic cancer

X Yu, D Li, J Kottur, HS Kim, LE Herring… - Journal of Medicinal …, 2023 - ACS Publications
As a core chromatin-regulatory scaffolding protein, WDR5 mediates numerous protein–
protein interactions (PPIs) with other partner oncoproteins. However, small-molecule …

Collagen-induced DDR1 upregulates CXCL5 to promote neutrophil extracellular traps formation and Treg infiltration in breast cancer

H Li, J Li, Z Bai, S Yan, J Li - International Immunopharmacology, 2023 - Elsevier
Neutrophil extracellular traps (NETs) have been implicated in many cancers, but the
regulatory mechanisms in the context of breast cancer have not been thoroughly discussed …

Ribosome subunit attrition and activation of the p53–MDM4 axis dominate the response of MLL-rearranged cancer cells to WDR5 WIN site inhibition

GC Howard, J Wang, KL Rose, C Jones, P Patel, T Tsui… - Elife, 2024 - elifesciences.org
The chromatin-associated protein WD Repeat Domain 5 (WDR5) is a promising target for
cancer drug discovery, with most efforts blocking an arginine-binding cavity on the protein …

Epigenetic markers and therapeutic targets for metastasis

CJ Kravitz, Q Yan, DX Nguyen - Cancer and Metastasis Reviews, 2023 - Springer
The last few years have seen an increasing number of discoveries which collectively
demonstrate that histone and DNA modifying enzyme modulate different stages of …

[HTML][HTML] Loss of Wdr5 attenuates MLL-rearranged leukemogenesis by suppressing Myc targets

L Liu, X Guo, Y Wang, G Li, Y Yu, Y Song… - Biochimica et biophysica …, 2023 - Elsevier
Abstract WD repeat domain 5 (WDR5) is a prominent target for pharmacological inhibition in
cancer through its scaffolding role with various oncogenic partners such as MLL and MYC …

MBD2 regulates the progression and chemoresistance of cholangiocarcinoma through interaction with WDR5

D Wang, J Chen, G Wu, F Xiong, W Liu, Q Wang… - Journal of Experimental …, 2024 - Springer
Background Cholangiocarcinoma (CCA) is a highly malignant, rapidly progressing tumor of
the bile duct. Owing to its chemoresistance, it always has an extremely poor prognosis …

Targeting WDR5/ATAD2 signaling by the CK2/Ikaros axis demonstrates therapeutic efficacy in T-ALL

Q Han, Y Gu, H Xiang, L Zhang, Y Wang, C Yang, J Li… - Blood, 2024 - Elsevier
T-cell acute lymphoblastic leukemia (T-ALL) is an aggressive hematological malignancy
with a poor prognosis and limited options for targeted therapies. Identifying new molecular …

The role of histone post-translational modifications in cancer and cancer immunity: functions, mechanisms and therapeutic implications

X Duan, Z Xing, L Qiao, S Qin, X Zhao… - Frontiers in …, 2024 - frontiersin.org
Histones play crucial roles in both promoting and repressing gene expression, primarily
regulated through post-translational modifications (PTMs) at specific amino acid residues …