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References from Molecular reprogramming in cutaneous melanoma: the central role of G9a and EZH2 methyltransferase inhibitors in tumor plasticity, immune evasion, and therapeutic resistance. Local targets link to admitted publications; unresolved targets remain external evidence.
Histone methyl-transferase G9a inhibition boosts the efficacy of immune checkpoint inhibitors in experimental hepatocellular carcinoma
10.1016/j.xcrm.2026.102717 · 2026 · External reference
The molecular hallmarks of epigenetic control
10.1038/nrg.2016.59 · 2016 · External reference
Global burden of cutaneous melanoma in 2020 and projections to 2040
10.1001/jamadermatol.2022.0160 · 2022 · External reference
The molecular pathology of melanoma: an integrated taxonomy of melanocytic neoplasia
10.1146/annurev-pathol-012513-104658 · 2014 · External reference
Cancer cell phenotype plasticity as a driver of immune escape in melanoma
10.3389/fimmu.2022.873116 · 2022 · External reference
Melanoma skin cancer: a comprehensive review of current knowledge
10.3390/cancers17172920 · 2025 · External reference
Acral melanoma: new insights into the immune and genomic landscape
10.1016/j.neo.2023.100947 · 2023 · External reference
Functional role of G9a histone methyltransferase in cancer
10.3389/fimmu.2015.00487 · 2015 · External reference
Combined inhibition of G9a and EZH2 suppresses tumor growth via synergistic induction of IL24-mediated apoptosis
10.1158/0008-5472.can-21-2218 · 2022 · External reference
Unique tructural platforms of Suz12 dictate distinct classes of PRC2 for chromatin binding
10.1016/j.molcel.2018.01.039 · 2018 · External reference
Tazemetostat for tumors harboring SMARCB1/SMARCA4 or EZH2 alterations: results from NCI-COG pediatric MATCH APEC1621C
10.1093/jnci/djad085 · 2023 · External reference
A phase I/II study of valemetostat (DS-3201b), an EZH1/2 inhibitor, in combination with irinotecan in patients with recurrent small-cell lung cancer
10.1158/1078-0432.ccr-23-3383 · 2024 · External reference
Abnormal overexpression of G9a in melanoma cells promotes cancer progression via upregulation of the Notch1 signaling pathway
10.18632/aging.102750 · 2020 · External reference
Inhibiting histone and DNA methylation improves cancer vaccination in an experimental model of melanoma
10.3389/fimmu.2022.799636 · 2022 · External reference
Epigenetic regulation during melanocyte development and homeostasis
10.1111/exd.14391 · 2021 · External reference
HIF1α epigenetically repressed macrophages via CRISPR/Cas9-EZH2 system for enhanced cancer immunotherapy
10.1016/j.bioactmat.2021.02.008 · 2021 · External reference
EZH2 inhibition promotes tumor immunogenicity in lung squamous cell carcinomas
10.1158/2767-9764.crc-23-0399 · 2024 · External reference
Targeting DNA methylation and EZH2 activity to overcome melanoma resistance to immunotherapy
10.1016/j.it.2019.02.004 · 2019 · External reference
Molecular and functional anticancer effects of GLP/G9a inhibition by UNC0646 in MeWo melanoma cells
10.1016/j.heliyon.2024.e27085 · 2024 · External reference
The Ezh2 polycomb group protein drives an aggressive phenotype in melanoma cancer stem cells and is a target of diet derived sulforaphane
10.1002/mc.22448 · 2016 · External reference
G9a: an emerging epigenetic target for melanoma therapy
10.3390/epigenomes5040023 · 2021 · External reference
Epigenetic regulation in melanoma: facts and hopes
10.3390/cells10082048 · 2021 · External reference
Modulation of EZH2 expression in T cells improves efficacy of anti-CTLA-4 therapy
10.1172/jci99760 · 2018 · External reference
EZH2 is a negative prognostic biomarker associated with immunosuppression in hepatocellular carcinoma
10.1371/journal.pone.0242191 · 2020 · External reference
Dissecting mechanisms of melanoma resistance to BRAF and MEK inhibitors revealed genetic and non-genetic patient- and drug-specific alterations and remarkable phenotypic plasticity
10.3390/cells9010142 · 2020 · External reference
Epigenetic control of antigen presentation failure in osteosarcoma: from single-cell chromatin maps to therapeutic strategies
10.3389/fimmu.2025.1728091 · 2025 · External reference
Current and emerging approaches targeting G9a for the treatment of various diseases
10.1021/acs.jmedchem.4c02781 · 2025 · External reference
H3K27me3 and EZH2 expression in melanoma: relevance for melanoma progression and response to immune checkpoint blockade
10.1186/s13148-020-0818-7 · 2020 · External reference
Transient EZH2 suppression by tazemetostat during in vitro expansion maintains T-cell stemness and improves adoptive T-cell therapy
10.1158/2326-6066.cir-24-0089 · 2025 · External reference
Tazemetostat: first approval
10.1007/s40265-020-01288-x · 2020 · External reference
Melanoma plasticity: promoter of metastasis and resistance to therapy
10.3389/fonc.2021.756001 · 2021 · External reference
Tazemetostat, an EZH2 inhibitor, in relapsed or refractory B-cell Non-Hodgkin lymphoma and advanced solid tumours: a first-in-human, open-label, phase 1 study
10.1016/s1470-2045(18)30145-1 · 2018 · External reference
Phase 1b study of EZH1/2 inhibitor valemetostat in combination with trastuzumab deruxtecan in patients with HER2 low/ultra-low/null metastatic breast cancer
10.1200/jco.2024.42.16_suppl.tps1120 · 2024 · External reference
Polycomb repressor complex 2 suppresses interferon-responsive MHC-II expression in melanoma cells and is associated with anti-PD-1 resistance
10.1136/jitc-2023-007736 · 2023 · External reference
Targeting EHMT2/G9a for cancer therapy: progress and perspective
10.1016/j.ejphar.2020.173827 · 2021 · External reference
Discovery of novel histone lysine methyltransferase G9a/GLP (EHMT2/1) inhibitors: design, synthesis, and structure-activity relationships of 2,4-diamino-6-methylpyrimidines
10.1016/j.bmcl.2020.127475 · 2020 · External reference
The cancer epigenome: non-cell autonomous player in tumor immunity
10.1111/cas.15681 · 2023 · External reference
Overcoming clinical resistance to EZH2 inhibition using rational epigenetic combination therapy
10.1158/2159-8290.cd-23-0110 · 2024 · External reference
G9a inhibition enhances checkpoint inhibitor blockade response in melanoma
10.1158/1078-0432.ccr-20-3463 · 2021 · External reference
Targeting EZH2 in cancer
10.1038/nm.4036 · 2016 · External reference
Acral melanoma: a review of its pathogenesis, progression, and management
10.3390/biom15010120 · 2025 · External reference
Polycomb repressive complex 1 generates discrete compacted domains that change during differentiation
10.1016/j.molcel.2017.01.009 · 2017 · External reference
Mi-2β promotes immune evasion in melanoma by activating EZH2 methylation
10.1038/s41467-024-46422-5 · 2024 · External reference
Enhancing anti-tumor immune responses through combination therapies: epigenetic drugs and immune checkpoint inhibitors
10.3389/fimmu.2023.1308264 · 2023 · External reference
Epigenetic modifiers to enhance the efficacy of immune checkpoint inhibitors for the treatment of melanoma
10.1016/j.tranon.2025.102452 · 2025 · External reference
The molecular and functional landscape of resistance to immune checkpoint blockade in melanoma
10.1038/s41467-023-36979-y · 2023 · External reference
Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP
10.1021/jm401480r · 2013 · External reference
H3K27me3-mediated PGC1α gene silencing promotes melanoma invasion through WNT5A and YAP
10.1172/jci130038 · 2020 · External reference
The polycomb complex PRC2 and its mark in life
10.1038/nature09784 · 2011 · External reference
Single-cell profiling of acral melanoma infiltrating lymphocytes reveals a suppressive tumor microenvironment
10.1126/scitranslmed.adk8832 · 2024 · External reference
The histone H3 lysine 9 methyltransferases G9a and GLP regulate polycomb repressive complex 2-mediated gene silencing
10.1016/j.molcel.2013.12.005 · 2014 · External reference
G9a in cancer: mechanisms, therapeutic advancements, and clinical implications
10.3390/cancers16122175 · 2024 · External reference
Dual targeting of G9a and DNMTs induces antitumor effects in multiple myeloma
10.1182/bloodadvances.2023010571 · 2025 · External reference
Tazemetostat, a selective EZH2 inhibitor, in combination with pembrolizumab for recurrent or metastatic head and neck squamous cell carcinoma: a phase 1 trial
10.3390/cancers17030437 · 2025 · External reference
Targeting epigenetic mechanisms: a boon for cancer immunotherapy
10.3390/biomedicines11010169 · 2023 · External reference
An actionable axis linking NFATc2 to EZH2 controls the EMT-like program of melanoma cells
10.1038/s41388-019-0729-2 · 2019 · External reference
Relapse-free survival in a pediatric patient with recurrent EZH2-mutant melanoma treated with adjuvant tazemetostat
10.1038/s41698-025-00826-8 · 2025 · External reference
Notch signaling pathway in cancer: from mechanistic insights to targeted therapies
10.1038/s41392-024-01828-x · 2024 · External reference
Epigenetics of human cutaneous melanoma: setting the stage for new therapeutic strategies
10.1186/1479-5876-8-56 · 2010 · External reference
GLP and G9a histone methyltransferases as potential therapeutic targets for lymphoid neoplasms
10.1186/s12935-024-03441-y · 2024 · External reference
SWI/SNF complex, promising target in melanoma therapy: snapshot view
10.3389/fmed.2023.1096615 · 2023 · External reference
Cancer epigenetics: promises and pitfalls for cancer therapy
10.1111/febs.16395 · 2022 · External reference
Histone methyltransferases G9a and GLP form heteromeric complexes and are both crucial for methylation of euchromatin at H3-K9
10.1101/gad.1284005 · 2005 · External reference
Safety, tolerability, and pharmacokinetics of valemetostat tablets and the effect of food on valemetostat pharmacokinetics in healthy subjects: two phase 1 studies
10.1002/cpdd.1315 · 2024 · External reference
Chromatin state profiling reveals PRC2 inhibition as a therapeutic target in NRAS-mutant melanoma
10.1080/23723556.2021.1986350 · 2021 · External reference
Genomic classification of cutaneous melanoma
10.1016/j.cell.2015.05.044 · 2015 · External reference
EZH2: an emerging role in melanoma biology and strategies for targeted therapy
10.1111/pcmr.12280 · 2015 · External reference
EZH2 as a mediator of treatment resistance in melanoma
10.1111/pcmr.12481 · 2016 · External reference
Epigenetic therapies in melanoma-targeting DNA methylation and histone modification
10.3390/biomedicines13051188 · 2025 · External reference
Resistance to BRAF inhibitors: EZH2 and its downstream targets as potential therapeutic options in melanoma
10.3390/ijms24031963 · 2023 · External reference
A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells
10.1038/nchembio.599 · 2011 · External reference
EZH2 dysregulation and its oncogenic role in human cancers
10.3390/cancers17193111 · 2025 · External reference
Epigenetic drivers of chromosomal instability
10.1016/j.trecan.2025.11.010 · 2026 · External reference
Epigenetically programmed resistance to chemo- and immuno-therapies
10.1016/bs.acr.2022.12.001 · 2023 · External reference
Comprehensive profiling of acral lentiginous melanoma reveals downregulated immune activation compared to cutaneous melanoma
10.1111/pcmr.70027 · 2025 · External reference
EZH2 inhibitor enhances the STING agonist-induced antitumor immunity in melanoma
10.1016/j.jid.2021.08.437 · 2022 · External reference
Phase I study of the novel enhancer of zeste homolog 2 (EZH2) inhibitor GSK2816126 in patients with advanced hematologic and solid tumors
10.1158/1078-0432.ccr-18-4121 · 2019 · External reference
TRLS-15. “TAZNI”: a phase I/II combination trial of tazemetostat with nivolumab and ipilimumab for children with INI1-negative or SMARCA4-deficient tumors (NCT05407441)
10.1093/neuonc/noae064.168 · 2024 · External reference
Epigenetic modulation of immunotherapy and implications in head and neck cancer
10.1007/s10555-020-09944-0 · 2021 · External reference
A methyl-to-acetyl switch in H3K27 drives metabolic reprogramming and resistance to BRAFV600E inhibition in melanoma
10.1016/j.neo.2025.101223 · 2025 · External reference
The epigenetic modifier EZH2 controls melanoma growth and metastasis through silencing of distinct tumour suppressors
10.1038/ncomms7051 · 2015 · External reference
The histone methyltransferase Ezh2 controls mechanisms of adaptive resistance to tumor immunotherapy
10.1016/j.celrep.2017.07.007 · 2017 · External reference