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Human ATAC Is a GCN5/PCAF-containing Acetylase Complex with a Novel NC2-like Histone Fold Module That Interacts with the TATA-binding Protein

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LncRNA HOTTIP modulates cancer stem cell properties in human pancreatic cancer by regulating HOXA9

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lncRNA HOXD-AS1 Regulates Proliferation and Chemo-Resistance of Castration-Resistant Prostate Cancer via Recruiting WDR5

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A TGFβ-PRMT5-MEP50 axis regulates cancer cell invasion through histone H3 and H4 arginine methylation coupled transcriptional activation and repression

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Identification of the MLL2 Complex as a Coactivator for Estrogen Receptor α

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Moonlighting with WDR5: A Cellular Multitasker

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Jmjd3 Inhibits Reprogramming by Upregulating Expression of INK4a/Arf and Targeting PHF20 for Ubiquitination

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In Vivo Functional Platform Targeting Patient-Derived Xenografts Identifies WDR5-Myc Association as a Critical Determinant of Pancreatic Cancer

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Mission Possible: Advances in MYC Therapeutic Targeting in Cancer

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An Lnc RNA (GAS5)/SnoRNA-derived piRNA induces activation of TRAIL gene by site-specifically recruiting MLL/COMPASS-like complexes

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ACK1/TNK2 Regulates Histone H4 Tyr88-phosphorylation and AR Gene Expression in Castration-Resistant Prostate Cancer

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TWIST1-WDR5- Hottip Regulates Hoxa9 Chromatin to Facilitate Prostate Cancer Metastasis

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The plasticity of WDR5 peptide-binding cleft enables the binding of the SET1 family of histone methyltransferases

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Characterization of a Novel WDR5-binding Site That Recruits RbBP5 through a Conserved Motif to Enhance Methylation of Histone H3 Lysine 4 by Mixed Lineage Leukemia Protein-1*

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Structural and Biochemical Insights into MLL1 Core Complex Assembly

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Biochemical Reconstitution and Phylogenetic Comparison of Human SET1 Family Core Complexes Involved in Histone Methylation

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Structural analysis of the KANSL1/WDR5/KANSL2 complex reveals that WDR5 is required for efficient assembly and chromatin targeting of the NSL complexPreprint

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A Role for WDR5 in Integrating Threonine 11 Phosphorylation to Lysine 4 Methylation on Histone H3 during Androgen Signaling and in Prostate Cancer

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WDR5 Supports an N-Myc Transcriptional Complex That Drives a Protumorigenic Gene Expression Signature in Neuroblastoma

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Pax3/7BP Is a Pax7- and Pax3-Binding Protein that Regulates the Proliferation of Muscle Precursor Cells by an Epigenetic Mechanism

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X-Linked Mental Retardation Gene CUL4B Targets Ubiquitylation of H3K4 Methyltransferase Component WDR5 and Regulates Neuronal Gene Expression

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Discovery of a Highly Potent, Cell-Permeable Macrocyclic Peptidomimetic (MM-589) Targeting the WD Repeat Domain 5 Protein (WDR5)–Mixed Lineage Leukemia (MLL) Protein–Protein Interaction

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Histone Methylation and STAT‐3 Differentially Regulate Interleukin‐6–Induced Matrix Metalloproteinase Gene Activation in Rheumatoid Arthritis Synovial Fibroblasts

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A Linc1405/Eomes Complex Promotes Cardiac Mesoderm Specification and Cardiogenesis

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

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A crosstalk between chromatin remodeling and histone H3K4 methyltransferase complexes in endothelial cells regulates angiotensin II-induced cardiac hypertrophy

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MLL/WDR5 Complex Regulates Kif2A Localization to Ensure Chromosome Congression and Proper Spindle Assembly during Mitosis

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WDR5 is essential for assembly of the VISA-associated signaling complex and virus-triggered IRF3 and NF-κB activation

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Cbx8 Acts Non-canonically with Wdr5 to Promote Mammary Tumorigenesis

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WDR5 Expression Is Prognostic of Breast Cancer Outcome

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WDR5 is a conserved regulator of protein synthesis gene expression

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Glucagon regulates gluconeogenesis through KAT2B- and WDR5-mediated epigenetic effects

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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

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Wdr5 Is Essential for Osteoblast Differentiation

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lncRNA GCAWKR Promotes Gastric Cancer Development by Scaffolding the Chromatin Modification Factors WDR5 and KAT2A

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Discovery of DDO-2213 as a Potent and Orally Bioavailable Inhibitor of the WDR5–Mixed Lineage Leukemia 1 Protein–Protein Interaction for the Treatment of MLL Fusion Leukemia

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Synergistic Effect of SRY and Its Direct Target, WDR5, on Sox9 Expression

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WD Repeat-containing Protein 5 (WDR5) Localizes to the Midbody and Regulates Abscission

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KAT8 Regulates Androgen Signaling in Prostate Cancer Cells

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WD Repeat-containing Protein 5, a Ubiquitously Expressed Histone Methyltransferase Adaptor Protein, Regulates Smooth Muscle Cell-selective Gene Activation through Interaction with Pituitary Homeobox 2

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Gene expression profiling of WDR5 regulated genes in bladder cancer

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The role of WDR5 in silencing human fetal globin gene expression

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PHF20L1 antagonizes SOX2 proteolysis triggered by the MLL1/WDR5 complexes

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LincRNA1230 inhibits the differentiation of mouse ES cells towards neural progenitors

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Epigenetic and transcriptional modulation of WDR5 , a chromatin remodeling protein, in Huntington's disease human induced pluripotent stem cell (hiPSC) model

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Three calcium-sensitive genes, fus, brd3 and wdr5, are highly expressed in neural and renal territories during amphibian development

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CCCTC-Binding Factor Transcriptionally Targets Wdr5 to Mediate Somatic Cell Reprogramming

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The TrxG Complex Mediates Cytokine Induced De Novo Enhancer Formation in Islets

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Discovery of Potent Small-Molecule Inhibitors of WDR5-MYC Interaction

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Discovery of Potent and Selective WDR5 Proteolysis Targeting Chimeras as Potential Therapeutics for Pancreatic Cancer

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WIN site inhibition disrupts a subset of WDR5 function

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Discovery of Potent Orally Bioavailable WD Repeat Domain 5 (WDR5) Inhibitors Using a Pharmacophore-Based Optimization

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

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NSUN5 Facilitates Hepatocellular Carcinoma Progression by Increasing SMAD3 Expression

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Recent Progress in Modulation of WD40-Repeat Domain 5 Protein (WDR5): Inhibitors and Degraders

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Pocket Crafter: a 3D generative modeling based workflow for the rapid generation of hit molecules in drug discovery

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Enhancing the Predictive Power of Machine Learning Models through a Chemical Space Complementary DEL Screening Strategy

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Structural studies of WDR5 in complex with MBD3C WIN motif reveal a unique binding mode

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Discovery and Optimization of WDR5 Inhibitors via Cascade Deoxyribonucleic Acid-Encoded Library Selection Approach

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The NTE domain of PTENα/β promotes cancer progression by interacting with WDR5 via its SSSRRSS motif

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Liquid-liquid phase separation in viral infection: From the occurrence and function to treatment potentials

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Therapeutic targeting of WDR5-MLL1 by EMBOW-derived peptides suppresses leukemia progression

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Small molecule WDR5 inhibitors down-regulate lncRNA expression

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The WD repeat-containing protein 5 (WDR5) antagonist WDR5-0103 restores the efficacy of cytotoxic drugs in multidrug-resistant cancer cells overexpressing ABCB1 or ABCG2

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Mechanism of Resistance to the WDR5 Inhibitor in MLL-Rearranged Leukemia

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Macrocyclic peptides as inhibitors of WDR5–lncRNA interactions

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

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Structural insights into lysine-mediated WIN site recognition reveal an alternative “AK” motif for WDR5 binding

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WDR54 exerts oncogenic roles in T‐cell acute lymphoblastic leukemia

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Generative Design of High-Affinity Peptides Using BindCraftPreprint

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Cyclic mechanical stress promotes osteogenic differentiation of periodontal ligament stem cells via KAT2A-mediated succinylation of WDR5

Guo, X., & Zhuge, N. (2025) · Tissue and Cell · doi:10.1016/j.tice.2025.102839 · Cited by 3 · see citing works

Structural characterization of endogenous microprotein EMBOW reveals an alternative MRT motif for WDR5 ‐interacting site recognition

Yang, Y., Pan, Y., Zhang, S., Wang, H., Sun, X., Hang, T., & Xu, L. (2026) · FEBS Journal · doi:10.1111/febs.70450 · Cited by 3 · see citing works

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

Mata, J. M., Liu, J., McKenna, S. M., van der Nol, E., Havermans, M., Delwel, R., Filius, M., Joo, C., Vallaro, M., Caron, G., et al. (2026) · Nature Communications · doi:10.1038/s41467-026-71641-3 · Cited by 3 · see citing works

WD repeat domain 5 (WDR5) inhibitors: a patent review (2016-present)

Coker, J. A., & Stauffer, S. R. (2024) · Expert Opinion on Therapeutic Patents · doi:10.1080/13543776.2024.2441658 · Cited by 3 · see citing works

Comparative RNA-Seq analysis to understand anthocyanin biosynthesis and regulations in Curcuma alismatifolia

Li, Y., Chen, X.-H., Yu, H., Tian, Q.-L., & Lu, L. (2022) · Folia Horticulturae · doi:10.2478/fhort-2022-0007 · Cited by 3 · see citing works

Isotopologues of a Metabolic Precursor for Selective N-15 and C-13 Histidine Labeling

Brüschweiler, S., Hlavac, M., Kratzwald, S. E., Schörghuber, J., Siess, K. M., Wimmer, A., Platzer, G., Konrat, R., & Lichtenecker, R. J. (2025) · Journal of Molecular Biology · doi:10.1016/j.jmb.2025.169347 · Cited by 2 · see citing works

Participation of host cell proteins in inclusion bodies of non-segmented RNA virus infected cells: a molecular insight

Sarkar, S., Biligiri, K. K., Vats, N., Rampalli, S., Ganguly, S., Kumar, N., Sarkar, D. P., Ganguly, N. K., & Sharma, N. R. (2025) · Virology Journal · doi:10.1186/s12985-025-02784-w · Cited by 2 · see citing works

Chromatin Regulatory Targets for Anticancer Therapeutics

Barta, P. A., Carter, T. R., & Erb, M. A. (2025) · Chemical Reviews · doi:10.1021/acs.chemrev.5c00231 · Cited by 2 · see citing works

Multitargeted protein degradation: Integrating small-molecule, biomacromolecular, and nano-PROTACs for paradigm shifts in drug discovery

Yang, J., Zhang, Y., Zhang, M., Xing, D., & Wang, C. (2025) · Materials Today Advances · doi:10.1016/j.mtadv.2025.100644 · Cited by 3 · see citing works

Targeting bromodomian-containing protein 8 (BRD8): An advanced tool to interrogate BRD8

Wu, T., Chen, Y., You, Q., Jiang, Z., & Chen, X. (2024) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2024.116271 · Cited by 2 · see citing works

Identification and validation of WDR5 WIN-site ligands via DNA-encoded chemical library screening

Ding, B., Li, L., Hu, J., Zhang, R., Wang, F., Zhou, Z., Lin, Y., Pan, C., Zhou, Y., Yang, B., et al. (2024) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2024.107948 · Cited by 2 · see citing works

Screening and optimization of phage display cyclic peptides against the WDR5 WBM site

Song, L., Cao, J., Chen, L., Du, Z., Zhang, N., Cao, D., & Xiong, B. (2023) · RSC Medicinal Chemistry · doi:10.1039/d3md00288h · Cited by 2 · see citing works

Targeting Epigenetic Readers Using Small Molecule Binders and PROTAC Degraders

Boccia, E., Gazzillo, E., Chini, M. G., Bifulco, G., & Lauro, G. (2024) · Interdisciplinary cancer research · doi:10.1007/16833_2024_240 · Cited by 1 · see citing works

Design, Synthesis, and Inhibitory Activity of Benzimidazole‐2‐thiol Derivatives on SHSY‐5Y Neuroblastoma Cancer Cell Line

Suryavanshi, H., Chabukswar, A. R., Meshram, R. J., Waghmare, P., Jagdale, S. C., Sakharkar, A. J., Patil, V., & Navin, J. (2025) · ChemistrySelect · doi:10.1002/slct.202406047 · Cited by 1 · see citing works

Molecular genetic characteristics and clinical significance of childhood acute lymphoblastic leukemia

Zhu, Z., & Yan, J. (2025) · Frontiers in Pediatrics · doi:10.3389/fped.2025.1665431 · Cited by 1 · see citing works

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

Chen, X., He, L., Lv, X., Liu, S., Song, J., Min, J., Sun, P., Li, J., Shi, D., & Huang, Y. (2025) · Chinese Chemical Letters · doi:10.1016/j.cclet.2025.112300 · Cited by 1 · see citing works

Structural Basis for Non-classical WIN Peptides Recognition by WDR5

Yang, Y., Pan, Y., Wang, Q., Li, H., Zhang, S., Sun, X., Xia, L., Xu, L., & Chen, X. (2026) · Journal of Molecular Biology · doi:10.1016/j.jmb.2026.169666 · Cited by 1 · see citing works

NSUN5 facilitates the progression of hepatocellular carcinoma by increasing the expression of SMAD3Preprint

Han, H., Du, Y., Zhao, Z., Wang, Y., Zhang, J., You, X., Zhou, G.-X., Zhou, H., Ye, J., Tian, W., et al. (2023) · Research Square · doi:10.21203/rs.3.rs-2853045/v1 · Cited by 1 · see citing works

A structural competition involving WDR5 times circadian oscillationsPreprint

Börgel, A., Rawleigh, A., Conrady, M., Hof, F., Ricci, K., Brown, S. A., & Wolf, E. (2023) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2023.06.05.543739

Immunoproteomic analyses identify broadly cross-reactive sporozoite immunogens of Eimeria maxima recognized by antisera from chickens infected with E. maxima, E. necatrix, E. tenella or E. acervulina

Gong, H., Deng, H., Song, F., Han, T., Wang, X., Feng, S., Chen, W., & Liu, L. (2025) · Veterinary Parasitology · doi:10.1016/j.vetpar.2025.110462

Astragaloside IV Alleviates Ulcerative Colitis Progression by Inhibiting WDR5 ‐Mediated ENO1 H3K4me3 Modification

Wu, S., Chen, Z., Wang, X., & Gu, J. (2025) · The Kaohsiung Journal of Medical Sciences · doi:10.1002/kjm2.70064

Inhibitors and degraders of epigenetic regulation in cancer

Gao, P., Kanıskan, H. Ü., & Jin, J. (2025) · Elsevier eBooks · doi:10.1016/b978-0-443-29808-0.00037-6

ChemScreener: an active learning enabled hit discovery workflow with WDR5 inhibitor case study

Shen, L., Fang, J., Liu, L., Wang, R., Jenkins, J. L., & Wang, H. (2026) · Journal of Cheminformatics · doi:10.1186/s13321-026-01204-7 · Cited by 1 · see citing works

Additional file 2 of Pocket Crafter: a 3D generative modeling based workflow for the rapid generation of hit molecules in drug discovery

Shen, L., Fang, J., Liu, L., Yang, F., Jenkins, J. L., Kutchukian, P. S., & Wang, H. (2024) · Figshare · doi:10.6084/m9.figshare.26696520

Additional file 3 of Pocket Crafter: a 3D generative modeling based workflow for the rapid generation of hit molecules in drug discovery

Shen, L., Fang, J., Liu, L., Yang, F., Jenkins, J. L., Kutchukian, P. S., & Wang, H. (2024) · Figshare · doi:10.6084/m9.figshare.26696523

Additional file 1 of Pocket Crafter: a 3D generative modeling based workflow for the rapid generation of hit molecules in drug discovery

Shen, L., Fang, J., Liu, L., Yang, F., Jenkins, J. L., Kutchukian, P. S., & Wang, H. (2024) · Figshare · doi:10.6084/m9.figshare.26696517

Beyond neurotransmission: the roles of serotonylation in physiological and pathological processes

Wang, J.-M., Zhang, F.-H., Chen, Y.-R., Chen, D.-N., Wang, X. L., Xie, H., Jiang-Feng, L. I., Luo, J.-D., & Xie, L.-P. (2026) · Cellular & Molecular Biology Letters · doi:10.1186/s11658-026-00909-9

PRMT5 promotes ferroptosis in cisplatin-induced acute kidney injury through WDR5/ACSL4 pathway

Lin, J., Fang, J., Cui, T., Xu, J., Lin, W., Li, S., Sui, Y., Zheng, Z., Wu, K., & Huang, M. (2026) · Redox Biology · doi:10.1016/j.redox.2026.104421

BindingDB Entry 50020006: Discovery and Structure-Based Design of Inhibitors of the WD Repeat-Containing Protein 5 (WDR5)-MYC Interaction.

BindingDB (2024) · UC San Diego · doi:10.7270/q26d5zdg

BindingDB Entry 50019445: Screening and optimization of phage display cyclic peptides against the WDR5 WBM site.

BindingDB (2024) · UC San Diego · doi:10.7270/q20z77nb

BindingDB Entry 50022801: Targeting bromodomian-containing protein 8 (BRD8): An advanced tool to interrogate BRD8.

BindingDB (2026) · UC San Diego · doi:10.7270/q27m0ds8

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 50021611: Discovery and Optimization of WDR5 Inhibitors via Cascade Deoxyribonucleic Acid-Encoded Library Selection Approach.

BindingDB (2025) · UC San Diego · doi:10.7270/q2b280xj

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

Discovery of Potent Small-Molecule Inhibitors of WDR5-MYC Interaction

Ding, J. H., Li, G., Liu, H., Liu, L., Lin, Y., Gao, J., Zhou, G., Shen, L., Zhao, M., Yu, Y., et al. (2023) · ACS Chemical Biology · doi:10.1021/acschembio.2c00843 · Cited by 43 · see citing works

WD repeat domain 5 (WDR5) inhibitors: a patent review (2016-present)

Coker, J. A., & Stauffer, S. R. (2024) · Expert Opinion on Therapeutic Patents · doi:10.1080/13543776.2024.2441658 · Cited by 3 · see citing works

Discovery and Structure-Based Optimization of Potent and Selective WD Repeat Domain 5 (WDR5) Inhibitors Containing a Dihydroisoquinolinone Bicyclic Core

Tian, J., Teuscher, K. B., Aho, E. R., Alvarado, J., Mills, J. J., Meyers, K. M., Gogliotti, R. D., Han, C., Macdonald, J. D., Sai, J., et al. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b01608 · Cited by 65 · see citing works

WD40 repeat domain proteins: a novel target class?

Schapira, M., Tyers, M., Torrent, M., & Arrowsmith, C. H. (2017) · Nature Reviews Drug Discovery · doi:10.1038/nrd.2017.179 · Cited by 335 · see citing works

Discovery of Novel Inhibitors for WD Repeat‐Containing Protein 5 ( WDR5 )‐ MYC Protein–Protein Interaction

Sun, W., Yu, H., Ye, J., Qin, L., Wang, L., Yan, H., Zhang, Z., Aliper, A. M., Ren, F., Ding, X., et al. (2025) · Chemical Biology & Drug Design · doi:10.1111/cbdd.70129 · Cited by 1 · see citing works