DCAF1-based PROTACs with activity against clinically validated targets overcoming intrinsic-and acquired-degrader resistance

M Schröder, M Renatus, X Liang, F Meili… - Nature …, 2024 - nature.com
Targeted protein degradation (TPD) mediates protein level through small molecule induced
redirection of E3 ligases to ubiquitinate neo-substrates and mark them for proteasomal …

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 …

Targeting myc interacting proteins as a winding path in cancer therapy

Y Zhou, X Gao, M Yuan, B Yang, Q He… - Frontiers in …, 2021 - frontiersin.org
MYC, as a well-known oncogene, plays essential roles in promoting tumor occurrence,
development, invasion and metastasis in many kinds of solid tumors and hematologic …

Unannotated microprotein EMBOW regulates the interactome and chromatin and mitotic functions of WDR5

Y Chen, H Su, J Zhao, Z Na, K Jiang, A Bacchiocchi… - Cell reports, 2023 - cell.com
The conserved WD40-repeat protein WDR5 interacts with multiple proteins both inside and
outside the nucleus. However, it is currently unclear whether and how the distribution of …

Human WDR5 promotes breast cancer growth and metastasis via KMT2-independent translation regulation

WL Cai, JFY Chen, H Chen, E Wingrove, SJ Kurley… - Elife, 2022 - elifesciences.org
Metastatic breast cancer remains a major cause of cancer-related deaths in women, and
there are few effective therapies against this advanced disease. Emerging evidence …

WDR5 represents a therapeutically exploitable target for cancer stem cells in glioblastoma

K Mitchell, SA Sprowls, S Arora, S Shakya… - Genes & …, 2023 - genesdev.cshlp.org
Glioblastomas (GBMs) are heterogeneous, treatment-resistant tumors driven by populations
of cancer stem cells (CSCs). However, few molecular mechanisms critical for CSC …

Expanded profiling of WD repeat domain 5 inhibitors reveals actionable strategies for the treatment of hematologic malignancies

CT Meyer, BN Smith, J Wang, KB Teuscher… - Proceedings of the …, 2024 - pnas.org
WD40 Repeat Domain 5 (WDR5) is a highly conserved nuclear protein that recruits MYC
oncoprotein transcription factors to chromatin to stimulate ribosomal protein gene …

Real-Time Measurement of a Weak Interaction of a Transcription Factor Motif with a Protein Hub at Single-Molecule Precision

LA Mayse, Y Wang, M Ahmad, L Movileanu - ACS nano, 2024 - ACS Publications
Transcription factors often interact with other protein cofactors, regulating gene expression.
Direct detection of these brief events using existing technologies remains challenging due to …

Disentangling the recognition complexity of a protein hub using a nanopore

LA Mayse, A Imran, MG Larimi, MS Cosgrove… - Nature …, 2022 - nature.com
WD40 repeat proteins are frequently involved in processing cell signaling and scaffolding
large multi-subunit machineries. Despite their significance in physiological and disease-like …

WIN site inhibition disrupts a subset of WDR5 function

AJ Siladi, J Wang, AC Florian, LR Thomas… - Scientific Reports, 2022 - nature.com
WDR5 nucleates the assembly of histone-modifying complexes and acts outside this context
in a range of chromatin-centric processes. WDR5 is also a prominent target for …