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    GENE:

    MAP2K2 (Mitogen-activated protein kinase kinase 2)

    i
    Other names: MAP2K2, MEK2, PRKMK2, Mitogen-activated protein kinase kinase 2
    10d
    Baicalein inhibits the progression of thyroid cancer by suppressing the TPL2/MEK2/ERK2 pathway. (PubMed, Front Endocrinol (Lausanne))
    BA treatment upregulates PLAU gene expression, but this increased PLAU protein subsequently interacts with and inhibited by BA, leading to downstream pathway suppression. It was concluded it could be served as a promising therapeutic strategy for the treatment of PTC.
    Journal
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    BRAF (B-raf proto-oncogene) • MAP2K2 (Mitogen-activated protein kinase kinase 2) • PLAU (Plasminogen Activator)
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    BRAF mutation
    16d
    Gecko protein F2 inhibits tumor angiogenesis by suppressing the VEGF/MAPK/ERK signaling pathway. (PubMed, Med Oncol)
    In conclusion, F2 has significant antitumor activity. One of its mechanisms of action is to suppress angiogenesis in tumor tissue and surrounding tissues by inhibiting the VEGF/ERK/MAP signaling pathway.
    Journal
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    MAP2K2 (Mitogen-activated protein kinase kinase 2) • MAPK1 (Mitogen-activated protein kinase 1) • PECAM1 (Platelet And Endothelial Cell Adhesion Molecule 1)
    2ms
    Phase Ib Study of Avutometinib, Defactinib, and Everolimus in RAS Pathway Mutant Endometrial Cancer (clinicaltrials.gov)
    P1, N=31, Not yet recruiting, M.D. Anderson Cancer Center
    New P1 trial
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    KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog) • HRAS (Harvey rat sarcoma viral oncogene homolog) • MAP2K2 (Mitogen-activated protein kinase kinase 2)
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    KRAS mutation • BRAF mutation • NRAS mutation • RAS mutation • HRAS mutation
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    everolimus • Avmapki (avutometinib) • Fakzynja (defactinib)
    2ms
    Discovery of Potent Antibacterial and Anticancer Flavonoids from Beehive-Associated Streptomyces griseoaurantiacus HNF214. (PubMed, Pak J Biol Sci)
    <b></b> <i>Streptomyces griseoaurantiacus</i> HNF214 from beehives produces quercetin and isoquercetin, exhibiting both antibacterial and anticancer activities, likely via MAPK/ERK pathway inhibition. While promising, further safety and <i>in vivo</i> studies are crucial before therapeutic development.
    Journal
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    MAP2K1 (Mitogen-activated protein kinase kinase 1) • MAP2K2 (Mitogen-activated protein kinase kinase 2)
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    Kinisoquin (isoquercetin)
    3ms
    Phytochemicals From Houttuynia cordata Thunb as Potential Inhibitors of BRAF, MEK, and ERK: Insights From Molecular Docking. (PubMed, J Skin Cancer)
    Quercitrin has the lowest binding energy against MEK-1 (-9.963 kcal/mol), 3-hydroxy-β-sitost-5-en-7-one demonstrated the lowest binding energy to ERK-1 (-10.495 kcal/mol), and rutin was best against MEK-2 with a calculated binding energy value of -9.963 kcal/mol. The binding modes of these compounds are compared with the known inhibitors of the oncoprotein targets that showed similar interactions to key amino acid residues indicating their inhibitory potential and are suggested as promising candidates for melanoma treatment.
    Journal
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    BRAF (B-raf proto-oncogene) • MAP2K1 (Mitogen-activated protein kinase kinase 1) • MAP2K2 (Mitogen-activated protein kinase kinase 2)
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    BRAF V600E • BRAF V600
    3ms
    Germline activating sequence variations in RASopathy spectrum genes: genotype-phenotype correlation in a North Indian cohort. (PubMed, Front Genet)
    Our findings underscore the clinical and genetic diversity of RASopathies in the Indian population and highlight the role of next-generation sequencing in early and accurate diagnosis. While exploratory drug-gene interaction analysis provides hypothesis-generating insights, clinical translation requires rigorous validation in functional studies and clinical trials.
    Journal
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    BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog) • HRAS (Harvey rat sarcoma viral oncogene homolog) • PTPN11 (Protein Tyrosine Phosphatase Non-Receptor Type 11) • MAP2K2 (Mitogen-activated protein kinase kinase 2) • RAF1 (Raf-1 Proto-Oncogene Serine/Threonine Kinase) • MAPK1 (Mitogen-activated protein kinase 1) • RIT1 (Ras Like Without CAAX 1) • LZTR1 (Leucine Zipper Like Transcription Regulator 1)
    4ms
    Neoadjuvant Antiandrogen Therapy With or Without MEK or SRC Inhibition for Unfavorable-risk Prostate Cancer: A Phase 2 Randomized Clinical Trial. (PubMed, Eur Urol Oncol)
    Neoadjuvant SRC or MEK inhibition does not appear to mitigate the EMT response to ADT or influence clinical or pathological outcomes.
    Clinical • P2 data • Journal
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    MAP2K1 (Mitogen-activated protein kinase kinase 1) • MAP2K2 (Mitogen-activated protein kinase kinase 2) • VIM (Vimentin) • CDH2 (Cadherin 2)
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    Mekinist (trametinib) • dasatinib • Xtandi (enzalutamide) • Firmagon (degarelix)
    4ms
    Langerhans Cell Histiocytosis in Cardiofaciocutaneous Syndrome. (PubMed, Am J Med Genet A)
    However, despite the association of somatic BRAF variants and LCH, individuals with CFC syndrome are not thought to have higher rates of LCH. Here, we report two individuals with CFC syndrome and LCH and review the literature examining this potential association.
    Journal
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    KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • MAP2K1 (Mitogen-activated protein kinase kinase 1) • NF1 (Neurofibromin 1) • MAP2K2 (Mitogen-activated protein kinase kinase 2)
    4ms
    SCAMP3-Driven Regulation of ERK1/2 and Autophagy Phosphoproteomics Signatures in Triple-Negative Breast Cancer. (PubMed, Int J Mol Sci)
    Here, we investigated the role of SCAMP3 in ERK1/2 signaling and therapeutic response using TMT-based LC-MS/MS phosphoproteomics of wild-type (WT) and SCAMP3 knockout (SC3KO) SUM-149 cells under basal conditions, after epidermal growth factor (EGF) stimulation, and during ERK1/2 inhibition with MK-8353...These findings position SCAMP3 as a central coordinator of ERK signaling and autophagy. Our results support SCAMP3 as a potential therapeutic target to enhance ERK1/2 inhibitor clinical efficacy and overcome adaptive resistance mechanisms in TNBC.
    Journal
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    MAP2K2 (Mitogen-activated protein kinase kinase 2) • SQSTM1 (Sequestosome 1) • EGF (Epidermal growth factor)
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    MK-8353
    5ms
    Targeting JNK1/2 and P38 Mitogen-Activated Protein Kinases With Pazopanib Mitigates Bleomycin-Induced Lung Fibrosis. (PubMed, Arch Pharm (Weinheim))
    Remarkably, pazopanib treatment reversed the bleomycin-induced elevation in transforming growth factor-beta-1 (TGF-β1) and α-smooth muscle actin (α-SMA) levels. Our research highlighted the beneficial role of pazopanib in attenuating bleomycin-elicited lung fibrosis through the suppression of MEKK2 and MEKK3 and the modulation of JNK and P38 cascades.
    Journal
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    MAP2K2 (Mitogen-activated protein kinase kinase 2) • TNFA (Tumor Necrosis Factor-Alpha) • TGFB1 (Transforming Growth Factor Beta 1) • IL13 (Interleukin 13) • IL33 (Interleukin 33) • MAPK8 (Mitogen-activated protein kinase 8)
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    pazopanib • bleomycin
    5ms
    Biphasic (squamoid) papillary renal cell carcinoma: a distinct molecular and morphologic subtype within the PRCC spectrum. (PubMed, Virchows Arch)
    Targeted NGS revealed MET amplification (2 cases), MET mutation (1 case), NOTCH1 mutations (9 cases), and alterations in MAP2K2, FGFR4, DDR pathway genes (e.g., PMS2, CDK12R44W, RAD51C/D), and chromatin remodeling genes (EZH2, ARID1A). These findings support BPRCC as a distinct subtype of papillary RCC with consistent biphasic morphology, immunophenotypic divergence, and a unique molecular profile enriched for NOTCH, MAPK, and DDR pathway alterations.
    Journal
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    MET (MET proto-oncogene, receptor tyrosine kinase) • RB1 (RB Transcriptional Corepressor 1) • ARID1A (AT-rich interaction domain 1A) • NOTCH1 (Notch 1) • CCND1 (Cyclin D1) • FGFR4 (Fibroblast growth factor receptor 4) • CDK12 (Cyclin dependent kinase 12) • MAP2K2 (Mitogen-activated protein kinase kinase 2) • PMS2 (PMS1 protein homolog 2) • CDH1 (Cadherin 1) • RAD51C (RAD51 paralog C) • RAD51D (RAD51 paralog D) • CA9 (Carbonic anhydrase 9) • TP63 (Tumor protein 63) • GATA3 (GATA binding protein 3) • PAX8 (Paired box 8)
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    MET amplification • CDK12 mutation • MET mutation • RAD51C mutation
    5ms
    SYNERGY-AI: Artificial Intelligence Based Precision Oncology Clinical Trial Matching and Registry (clinicaltrials.gov)
    P=N/A, N=50000, Recruiting, Massive Bio, Inc. | Trial completion date: Jun 2027 --> Jun 2040 | Trial primary completion date: Dec 2026 --> Dec 2038
    Trial completion date • Trial primary completion date
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    EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2) • PD-L1 (Programmed death ligand 1) • KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • ER (Estrogen receptor) • ALK (Anaplastic lymphoma kinase) • TP53 (Tumor protein P53) • TMB (Tumor Mutational Burden) • FLT3 (Fms-related tyrosine kinase 3) • ABL1 (ABL proto-oncogene 1) • NRAS (Neuroblastoma RAS viral oncogene homolog) • BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • FGFR2 (Fibroblast growth factor receptor 2) • PTEN (Phosphatase and tensin homolog) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS) • IDH1 (Isocitrate dehydrogenase (NADP(+)) 1) • NTRK1 (Neurotrophic tyrosine kinase, receptor, type 1) • BCL2 (B-cell CLL/lymphoma 2) • IDH2 (Isocitrate Dehydrogenase (NADP(+)) 2) • NTRK3 (Neurotrophic tyrosine kinase, receptor, type 3) • NTRK2 (Neurotrophic tyrosine kinase, receptor, type 2) • STK11 (Serine/threonine kinase 11) • NPM1 (Nucleophosmin 1) • HRAS (Harvey rat sarcoma viral oncogene homolog) • DNMT3A (DNA methyltransferase 1) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3) • RB1 (RB Transcriptional Corepressor 1) • CLDN18 (Claudin 18) • PDGFRA (Platelet Derived Growth Factor Receptor Alpha) • NF1 (Neurofibromin 1) • JAK2 (Janus kinase 2) • NRG1 (Neuregulin 1) • POLE (DNA Polymerase Epsilon) • AKT1 (V-akt murine thymoma viral oncogene homolog 1) • PD-1 (Programmed cell death 1) • CCND1 (Cyclin D1) • MCL1 (Myeloid cell leukemia 1) • KDR (Kinase insert domain receptor) • PBRM1 (Polybromo 1) • BAP1 (BRCA1 Associated Protein 1) • VEGFA (Vascular endothelial growth factor A) • BCL6 (B-cell CLL/lymphoma 6) • PDGFRB (Platelet Derived Growth Factor Receptor Beta) • PTCH1 (Patched 1) • FGFR4 (Fibroblast growth factor receptor 4) • MSH6 (MutS homolog 6) • CDK4 (Cyclin-dependent kinase 4) • MSH2 (MutS Homolog 2) • CTNNB1 (Catenin (cadherin-associated protein), beta 1) • MAP2K2 (Mitogen-activated protein kinase kinase 2) • FBXW7 (F-Box And WD Repeat Domain Containing 7) • WT1 (WT1 Transcription Factor) • ATRX (ATRX Chromatin Remodeler) • BRCA (Breast cancer early onset) • RAF1 (Raf-1 Proto-Oncogene Serine/Threonine Kinase) • TSC2 (TSC complex subunit 2) • CHEK2 (Checkpoint kinase 2) • PD-L2 (Programmed Cell Death 1 Ligand 2) • ERBB4 (erb-b2 receptor tyrosine kinase 4) • JAK1 (Janus Kinase 1) • FANCA (FA Complementation Group A) • TSC1 (TSC complex subunit 1) • MDM4 (The mouse double minute 4) • POLD1 (DNA Polymerase Delta 1) • CDK6 (Cyclin-dependent kinase 6) • CEBPA (CCAAT Enhancer Binding Protein Alpha) • PARP1 (Poly(ADP-Ribose) Polymerase 1) • AURKA (Aurora kinase A) • JAK3 (Janus Kinase 3) • RICTOR (RPTOR Independent Companion Of MTOR Complex 2) • CHEK1 (Checkpoint kinase 1) • GATA6 (GATA Binding Protein 6) • MSH3 (MutS Homolog 3) • TGFBR2 (Transforming Growth Factor Beta Receptor 2) • GNAS (GNAS Complex Locus) • MYCL (MYCL Proto-Oncogene BHLH Transcription Factor) • AKT2 (V-akt murine thymoma viral oncogene homolog 2) • CCND2 (Cyclin D2) • CCND3 (Cyclin D3) • CSF1R (Colony stimulating factor 1 receptor) • MAP3K1 (Mitogen-Activated Protein Kinase Kinase Kinase 1) • ERCC4 (ERCC Excision Repair 4, Endonuclease Catalytic Subunit) • HDAC1 (Histone Deacetylase 1) • PRDM1 (PR/SET Domain 1) • ZNF217 (Zinc Finger Protein 217) • CDKN1A (Cyclin-dependent kinase inhibitor 1A) • GATA3 (GATA binding protein 3) • PARP2 (Poly(ADP-Ribose) Polymerase 2) • PARP3 (Poly(ADP-Ribose) Polymerase Family Member 3) • SDHA (Succinate Dehydrogenase Complex Flavoprotein Subunit A) • ACVR1B (Activin A Receptor Type 1B) • ZNF703 (Zinc Finger Protein 703)
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    HER-2 mutation • AKT1 mutation