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Design, Synthesis and Evaluation of WD-repeat containing protein 5 (WDR5) degradersPreprint

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Crystal structures of Kif2A complexed with WDR5 reveal the structural plasticity of WIN-S7 sites

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Cache: Utilizing ultra-large library screening in Rosetta to identify novel binders of the WD-repeat domain of Leucine-Rich Repeat Kinase 2

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Strategies for rapid production of crystallization quality coatomer WD40 domains

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Transcription factor 12‐mediated self‐feedback regulatory mechanism is required in DUX4 fusion leukaemia

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Expression of WD Repeat Domain 5 (WDR5) is Associated with Progression and Reduced Prognosis in Papillary Thyroid Carcinoma

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Therapeutic Opportunities of Targeting Canonical and Noncanonical PcG/TrxG Functions in Acute Myeloid Leukemia

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Cancer and aging: complex associations and therapeutic targets

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CDC40 suppression induces CDCA5 splicing defects and anti-proliferative effects in lung cancer cells

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Nuclear-localized HKDC1 promotes hepatocellular carcinoma through phosphorylating RBBP5 to upregulate H3K4me3

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Deep multilayer brain omics identifies the potential involvement of menopause molecular networks in Gliomas’ disease progression

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Discovery of an exquisitely selective WDR5 chemical probe accelerated by a high-quality DEL–ML Hit

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WDR5‐H3K4me3 Epigenetic Axis Promotes TRMT6‐Dependent tRNA M 1 A Modification to Facilitate Triple‐Negative Breast Cancer Progression by Suppressing Ferroptosis

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Massive barcode-free chemical screenings enable the discovery of bioactive macrocycles with passive membrane permeability

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WDR54 exerts oncogenic roles in T‐cell acute lymphoblastic leukemia

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Unraveling MLL1-fusion leukemia: Epigenetic revelations from an iPS cell point mutation

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KBG syndrome-associated protein ANKRD11 regulates SETD5 expression to modulate rRNA levels and translation

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A screen for MeCP2-TBL1 interaction inhibitors using a luminescence-based assay

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3D environment controls H3K4 methylation and the mechanical response of the nucleus in acute lymphoblastic leukemia cells

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Disrupting histone lysine methylation

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CCAAT/enhancer binding protein beta (C/EBPβ) regulates the formation of the ovarian reserve

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Chromatin Regulatory Targets for Anticancer Therapeutics

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Renal IGFBP6 Interacts With THBS1 to Drive Renal Cellular Senescence and Fibrosis

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Small Molecule Inhibitors Targeting New Targets of Protein-Protein Interactions

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ProxyBind: A compendium of binding sites for proximity-induced pharmacology

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A TOX-ic axis of epigenetic stem cell maintenance and chemoresistance in colon cancer

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The COMPASS complex maintains the metastatic capacity imparted by a subpopulation of cells in UPS

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Cellular functions of MLL/SET-family histone H3 lysine 4 methyltransferase components

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The AML-associated K313 mutation enhances C/EBPα activity by leading to C/EBPα overexpression

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

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Targeting SAGA/ATAC complexes disrupts chromatin regulation and cholesterol metabolism in diffuse midline gliomaPreprint

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Tissue‐Resident Macrophage‐Derived E3 Ligase SMURF2 Restricts Autoimmune Inflammation by Mediating the Degradation of p‐TBK1

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WDR5-targeted activatable fluorescent probes for tumor-specific imaging in live cells and in vivo

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Targeting the MYCN interaction network in neuroblastoma

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WDR5 remodels NANOG condensates to drive transcriptional programs and sustain stem cell identity

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

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

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Epigenetic priming of embryonic enhancer elements coordinates developmental gene networksPreprint

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Nuclear Histone 3 Post-Translational Modification Profiling in Whole Cells using Spectral Flow CytometryPreprint

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WDR5 regulates epithelial-to-mesenchymal transition in breast cancer cells via TGFβPreprint

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Lysine Reader Proteins

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MLL1 minimal catalytic complex is a dynamic conformational ensemble susceptible to pharmacological allosteric disruptionPreprint

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Lysine Methyltransferases and Their Inhibitors

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Computational Methods for the Discovery of Chemical Probes

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Structure-Based Survey of the Human Proteome for Opportunities in Proximity PharmacologyPreprint

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Targeting H3K4 methylation as a novel therapeutic strategy against tumor infiltration and nuclear changes of acute lymphoblastic leukemia cellsPreprint

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FBXW7 triggers degradation of WDR5 to prevent mitotic slippagePreprint

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Structural insights on the KMT2–NCP interaction

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Differentiating Acute Myeloid Leukemia Stem Cells/Blasts

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Additional file 4 of WD40 repeat 43 mediates cell survival, proliferation, migration and invasion via vimentin in colorectal cancer

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Additional file 10 of WD40 repeat 43 mediates cell survival, proliferation, migration and invasion via vimentin in colorectal cancer

Li, Z., Feng, M., Zhang, J., Wang, X., Xu, E., Wang, C., Lin, F., Yang, Z., Heng, Y., Guan, W., et al. (2021) · Figshare · doi:10.6084/m9.figshare.15139112

Additional file 7 of WD40 repeat 43 mediates cell survival, proliferation, migration and invasion via vimentin in colorectal cancer

Li, Z., Feng, M., Zhang, J., Wang, X., Xu, E., Wang, C., Lin, F., Yang, Z., Heng, Y., Guan, W., et al. (2021) · Figshare · doi:10.6084/m9.figshare.15139151

Additional file 3 of WD40 repeat 43 mediates cell survival, proliferation, migration and invasion via vimentin in colorectal cancer

Li, Z., Feng, M., Zhang, J., Wang, X., Xu, E., Wang, C., Lin, F., Yang, Z., Yu, H., Guan, W., et al. (2021) · Figshare · doi:10.6084/m9.figshare.15139130

Additional file 6 of WD40 repeat 43 mediates cell survival, proliferation, migration and invasion via vimentin in colorectal cancer

Li, Z., Feng, M., Zhang, J., Wang, X., Xu, E., Wang, C., Lin, F., Yang, Z., Heng, Y., Guan, W., et al. (2021) · Figshare · doi:10.6084/m9.figshare.15139145

Additional file 9 of WD40 repeat 43 mediates cell survival, proliferation, migration and invasion via vimentin in colorectal cancer

Li, Z., Feng, M., Zhang, J., Wang, X., Xu, E., Wang, C., Lin, F., Yang, Z., Yu, H., Guan, W., et al. (2021) · Figshare · doi:10.6084/m9.figshare.15139160

Initial Characterization of WDR5B Reveals a Role in the Proliferation of Retinal Pigment Epithelial Cells

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Targeting Histone Readers: Non-bromodomain Readers

Huang, X., Chen, Y., Xiao, Q., Shang, X., & Liu, Y. (2024) · Royal Society of Chemistry eBooks · doi:10.1039/9781837674916-00440

Drug Discovery for Chromatin Readers, Writers, Erasers, Remodelers and Epitranscriptomic Targets

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Arginine methylation of the p30 C/EBPα oncoprotein regulates progenitor proliferation and myeloid differentiation

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Development and characterization of triazole-based WDR5 inhibitors for the treatment of glioblastoma

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Inhibitors and degraders of epigenetic regulation in cancer

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Additional file 1 of WD40 repeat 43 mediates cell survival, proliferation, migration and invasion via vimentin in colorectal cancer

Li, Z., Feng, M., Zhang, J., Wang, X., Xu, E., Wang, C., Lin, F., Yang, Z., Yu, H., Guan, W., et al. (2021) · Figshare · doi:10.6084/m9.figshare.15139118

Additional file 5 of WD40 repeat 43 mediates cell survival, proliferation, migration and invasion via vimentin in colorectal cancer

Li, Z., Feng, M., Zhang, J., Wang, X., Xu, E., Wang, C., Lin, F., Yang, Z., Yu, H., Guan, W., et al. (2021) · Figshare · doi:10.6084/m9.figshare.15139142

Additional file 1 of Targeting WD repeat domain 5 enhances chemosensitivity and inhibits proliferation and programmed death-ligand 1 expression in bladder cancer

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Additional file 2 of WD40 repeat 43 mediates cell survival, proliferation, migration and invasion via vimentin in colorectal cancer

Li, Z., Feng, M., Zhang, J., Wang, X., Xu, E., Wang, C., Lin, F., Yang, Z., Yu, H., Guan, W., et al. (2021) · Figshare · doi:10.6084/m9.figshare.15139124

Additional file 8 of WD40 repeat 43 mediates cell survival, proliferation, migration and invasion via vimentin in colorectal cancer

Li, Z., Feng, M., Zhang, J., Wang, X., Xu, E., Wang, C., Lin, F., Yang, Z., Yu, H., Guan, W., et al. (2021) · Figshare · doi:10.6084/m9.figshare.15139154

Fusion oncoproteins orchestrate tumorigenesis and sustain malignant progression via a positive feedback mechanism

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Protein-protein interaction inhibitors in cancer

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Catalytic Proximal Protein Oligomerization as an Anti-Tumor Strategy Targeting WDR5

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The MLL1–MENIN complex preserves CD8 T cell memory through a TOX–BTLA-TCF1 axisPreprint

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The Histone‐Lysine N‐Methyltransferase (KMT2) Family in Health and Disease

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Structure-based design of the approved drug zafirlukast identifies HLC40 as a potent WDR5 WIN-site inhibitor with antitumor efficacy

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Self-Dimerization Induced Proximity Targeting Chimeras (SDIPTAC) Lead to DCAF1 Loss of Function and Inhibition of HIV Replication

Mabanglo, M. F., Srivastava, S., Matsui, Y., Li, Z., Noureldin, M., Pogmore, J. P., Hoffer, L., Taherian, F., Hajian, T., Tucker, S., et al. (2026) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6c00126

The role of the WD40-repeat protein family in cancer

李家乐, Zhou, H., Luo, Q., Wu, D., Lin, M., Mai, G., Xu, X., He, Y., Liu, Y., Wang, J., et al. (2026) · Molecular Cancer · doi:10.1186/s12943-026-02718-2

Mycobacterium tuberculosis manipulates host inflammation and lipid metabolism through the SET1-interacting protein Rv1075cPreprint

Coleman, A. K., Mabry, C. J., Chapman, M. J., Armijo, K. S., Smith, M. H., Huskey, J. B., Stranahan, L. W., Watson, R. O., & Patrick, K. L. (2026) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.64898/2026.08.21.746307

Disabling COMPASS Promoter Licensing Shifts HDAC‐Inhibited Gastric Cancer Toward Sustained Transcriptional Suppression During Recovery

Jintian, S., Yu, H., Jiang, J., Jiang, Z., Hong, Z., Zhang, X., Chen, L., Wei, S., & Wang, Y. (2026) · Advanced Science · doi:10.1002/advs.78255

BindingDB Entry 50017391: Design, Synthesis, and Evaluation of WD-Repeat-Containing Protein 5 (WDR5) Degraders.

BindingDB (2023) · UC San Diego · doi:10.7270/q20z77b9

BindingDB Entry 50014920: Discovery of

BindingDB (2023) · UC San Diego · doi:10.7270/q22b92x1

BindingDB Entry 50009676: Discovery and Optimization of Salicylic Acid-Derived Sulfonamide Inhibitors of the WD Repeat-Containing Protein 5-MYC Protein-Protein Interaction.

BindingDB (2021) · UC San Diego · doi:10.7270/q2b85cm0

BindingDB Entry 50047872: Discovery of a Potent, Selective, and Cell-Active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6.

BindingDB (2018) · UC San Diego · doi:10.7270/q2028tgj

BindingDB Entry 50014300: Discovery of a potent MLL1 and WDR5 protein-protein interaction inhibitor with in vivo antitumor activity.

BindingDB (2022) · UC San Diego · doi:10.7270/q2j38xcr

BindingDB Entry 50047391: Structure-Based Optimization of a Small Molecule Antagonist of the Interaction Between WD Repeat-Containing Protein 5 (WDR5) and Mixed-Lineage Leukemia 1 (MLL1).

BindingDB (2017) · UC San Diego · doi:10.7270/q2vt1v0c

BindingDB Entry 50007316: The identification of novel small-molecule inhibitors targeting WDR5-MLL1 interaction through fluorescence polarization based high-throughput screening.

BindingDB (2021) · UC San Diego · doi:10.7270/q26w9fc5

BindingDB Entry 50048213: High-affinity small molecular blockers of mixed lineage leukemia 1 (MLL1)-WDR5 interaction inhibit MLL1 complex H3K4 methyltransferase activity.

BindingDB (2018) · UC San Diego · doi:10.7270/q2251m6g

BindingDB Entry 50002146: Targeting protein-protein interaction between MLL1 and reciprocal proteins for leukemia therapy.

BindingDB (2020) · UC San Diego · doi:10.7270/q2sq92zs

BindingDB Entry 50023013: A Target Class Ligandability Evaluation of WD40 Repeat-Containing Proteins.

BindingDB (2026) · UC San Diego · doi:10.7270/q2j1081p

BindingDB Entry 50017413: Targeting WD Repeat-Containing Protein 5 (WDR5): A Medicinal Chemistry Perspective.

BindingDB (2023) · UC San Diego · doi:10.7270/q2b85d61

BindingDB Entry 50047884: Structure-based design of ester compounds to inhibit MLL complex catalytic activity by targeting mixed lineage leukemia 1 (MLL1)-WDR5 interaction.

BindingDB (2018) · UC San Diego · doi:10.7270/q2f47r4k

BindingDB Entry 50022567: The MLL1 trimeric catalytic complex is a dynamic conformational ensemble stabilized by multiple weak interactions.

BindingDB (2025) · UC San Diego · doi:10.7270/q2p273w2

BindingDB Entry 50003006: Discovery of Potent 2-Aryl-6,7-dihydro-5 H-pyrrolo[1,2- a]imidazoles as WDR5-WIN-Site Inhibitors Using Fragment-Based Methods and Structure-Based Design.

BindingDB (2020) · UC San Diego · doi:10.7270/q2kd21kt

BindingDB Entry 50020603: Small molecule WDR5 inhibitors down-regulate lncRNA expression.

BindingDB (2024) · UC San Diego · doi:10.7270/q2833xh5

BindingDB Entry 50020581: Structure-Based Discovery of Potent, Orally Bioavailable Benzoxazepinone-Based WD Repeat Domain 5 Inhibitors.

BindingDB (2024) · UC San Diego · doi:10.7270/q2kh0ssw

BindingDB Entry 50017835: Discovery of Potent Orally Bioavailable WD Repeat Domain 5 (WDR5) Inhibitors Using a Pharmacophore-Based Optimization.

BindingDB (2023) · UC San Diego · doi:10.7270/q2jq153m

BindingDB Entry 50020560: Discovery of Potent and Selective WDR5 Proteolysis Targeting Chimeras as Potential Therapeutics for Pancreatic Cancer.

BindingDB (2024) · UC San Diego · doi:10.7270/q2hq44cm

Recruitment of the MLL complex via specific interaction of the p30 variant of C/EBPα with Wdr5 is essential for development of acute myeloid leukemia

Grebien, F., Giambruno, R., Grover, A., Vittori, S., Schönegger, A., Bilban, M., Bock, C., Zuber, J. A., Bennett, K. L., Nerlov, C., et al. (2013) · Experimental Hematology · doi:10.1016/j.exphem.2013.05.075

CEBPA-Mutant Acute Myeloid Leukemia is Sensitive to Small-Molecule-Mediated Inhibition of the Menin-MLL Interaction

Schmidt, L., Heyes, E. C., Scheiblecker, L., Eder, T., Volpe, G., Frampton, J., Nerlov, C., Valent, P., Grembecka, J. E., & Grebien, F. (2018) · Experimental Hematology · doi:10.1016/j.exphem.2018.06.142

CEBPA-mutated leukemia is sensitive to genetic and pharmacological targeting of the MLL1 complex

Schmidt, L., Heyes, E. C., Scheiblecker, L., Eder, T., Volpe, G., Frampton, J., Nerlov, C., Valent, P., Grembecka, J. E., & Grebien, F. (2019) · Leukemia · doi:10.1038/s41375-019-0382-3 · Cited by 35

Identification of gene targets of mutant C/EBPα reveals a critical role for MSI2 in CEBPA-mutated AML

Heyes, E. C., Schmidt, L., Manhart, G., Eder, T., Proietti, L., & Grebien, F. (2021) · Leukemia · doi:10.1038/s41375-021-01169-6 · Cited by 23

Dissecting the Molecular Mechanisms of Mutant C/EBPalpha (p30) in Normal and Malignant Human Hematopoiesis.

Cammenga, J., Niebuhr, B., Horn, S., Delwel, R., & Stocking, C. (2005) · Blood · doi:10.1182/blood.v106.11.2995.2995