Cited by 278Melanoma and MAPK PathwaysProtein Kinase Regulation and GTPase SignalingProtein Tyrosine Phosphatases

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Transcriptional Pathway Signatures Predict MEK Addiction and Response to Selumetinib (AZD6244)

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Dry, Jonathan R., Pavey, Sandra, Pratilas, Christine A., Harbron, Chris, Runswick, Sarah, Hodgson, Darren, Chresta, Christine, McCormack, Rose, Byrne, Natalie, Cockerill, Mark, Graham, Alexander, Beran, Garry, Cassidy, Andrew, Haggerty, Carolyn, Brown, Helen, Ellison, Gillian, Dering, Judy, Taylor, Barry S., Stark, Mitchell, Bonazzi, Vanessa, Ravishankar, Sugandha, Packer, Leisl, Xing, Feng, Solit, David B., Finn, Richard S., Rosen, Neal, Hayward, Nicholas K., French, Tim, Smith, Paul D.·2010·Cancer Research

DOI 10.1158/0008-5472.can-09-1577PMC PMC3166660

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Abstract

Selumetinib (AZD6244, ARRY-142886) is a selective, non–ATP-competitive inhibitor of mitogen-activated protein/extracellular signal–regulated kinase kinase (MEK)-1/2. The range of antitumor activity seen preclinically and in patients highlights the importance of identifying determinants of response to this drug. In large tumor cell panels of diverse lineage, we show that MEK inhibitor response does not have an absolute correlation with mutational or phospho-protein markers of BRAF/MEK, RAS, or phosphoinositide 3-kinase (PI3K) activity. We aimed to enhance predictivity by measuring pathway output through coregulated gene networks displaying differential mRNA expression exclusive to resistant cell subsets and correlated to mutational or dynamic pathway activity. We discovered an 18-gene signature enabling measurement of MEK functional output independent of tumor genotype. Where the MEK pathway is activated but the cells remain resistant to selumetinib, we identified a 13-gene signature that implicates the existence of compensatory signaling from RAS effectors other than PI3K. The ability of these signatures to stratify samples according to functional activation of MEK and/or selumetinib sensitivity was shown in multiple independent melanoma, colon, breast, and lung tumor cell lines and in xenograft models. Furthermore, we were able to measure these signatures in fixed archival melanoma tumor samples using a single RT-qPCR–based test and found intergene correlations and associations with genetic markers of pathway activity to be preserved. These signatures offer useful tools for the study of MEK biology and clinical application of MEK inhibitors, and the novel approaches taken may benefit other targeted therapies. Cancer Res; 70(6); 2264–73

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Additional file 5 of snRNA-seq of human cutaneous neurofibromas before and after selumetinib treatment implicates role of altered Schwann cell states, inter-cellular signaling, and extracellular matrix in treatment response
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Additional file 9 of snRNA-seq of human cutaneous neurofibromas before and after selumetinib treatment implicates role of altered Schwann cell states, inter-cellular signaling, and extracellular matrix in treatment response
Church, C., Fay, C., Kriukov, E., Liu, H., Cannon, A. D., Baldwin, L. A., Crossman, D. K., Korf, B., Wallace, M. R., Gross, A. M., et al. (2024) · Figshare · doi:10.6084/m9.figshare.26737407
Additional file 4 of snRNA-seq of human cutaneous neurofibromas before and after selumetinib treatment implicates role of altered Schwann cell states, inter-cellular signaling, and extracellular matrix in treatment response
Church, C., Fay, C., Kriukov, E., Liu, H., Cannon, A. D., Baldwin, L. A., Crossman, D. K., Korf, B., Wallace, M. R., Gross, A. M., et al. (2024) · Figshare · doi:10.6084/m9.figshare.26737392
Additional file 13 of snRNA-seq of human cutaneous neurofibromas before and after selumetinib treatment implicates role of altered Schwann cell states, inter-cellular signaling, and extracellular matrix in treatment response
Church, C., Fay, C., Kriukov, E., Liu, H., Cannon, A. D., Baldwin, L. A., Crossman, D. K., Korf, B., Wallace, M. R., Gross, A. M., et al. (2024) · Figshare · doi:10.6084/m9.figshare.26737419
Additional file 1 of snRNA-seq of human cutaneous neurofibromas before and after selumetinib treatment implicates role of altered Schwann cell states, inter-cellular signaling, and extracellular matrix in treatment response
Church, C., Fay, C., Kriukov, E., Liu, H., Cannon, A. D., Baldwin, L. A., Crossman, D. K., Korf, B., Wallace, M. R., Gross, A. M., et al. (2024) · Figshare · doi:10.6084/m9.figshare.26082662
Additional file 7 of snRNA-seq of human cutaneous neurofibromas before and after selumetinib treatment implicates role of altered Schwann cell states, inter-cellular signaling, and extracellular matrix in treatment response
Church, C., Fay, C., Kriukov, E., Liu, H., Cannon, A. D., Baldwin, L. A., Crossman, D. K., Korf, B., Wallace, M. R., Gross, A. M., et al. (2024) · Figshare · doi:10.6084/m9.figshare.26737401
Additional file 6 of snRNA-seq of human cutaneous neurofibromas before and after selumetinib treatment implicates role of altered Schwann cell states, inter-cellular signaling, and extracellular matrix in treatment response
Church, C., Fay, C., Kriukov, E., Liu, H., Cannon, A. D., Baldwin, L. A., Crossman, D. K., Korf, B., Wallace, M. R., Gross, A. M., et al. (2024) · Figshare · doi:10.6084/m9.figshare.26737398
Additional file 8 of snRNA-seq of human cutaneous neurofibromas before and after selumetinib treatment implicates role of altered Schwann cell states, inter-cellular signaling, and extracellular matrix in treatment response
Church, C., Fay, C., Kriukov, E., Liu, H., Cannon, A. D., Baldwin, L. A., Crossman, D. K., Korf, B., Wallace, M. R., Gross, A. M., et al. (2024) · Figshare · doi:10.6084/m9.figshare.26737404
Additional file 2 of snRNA-seq of human cutaneous neurofibromas before and after selumetinib treatment implicates role of altered Schwann cell states, inter-cellular signaling, and extracellular matrix in treatment response
Church, C., Fay, C., Kriukov, E., Liu, H., Cannon, A. D., Baldwin, L. A., Crossman, D. K., Korf, B., Wallace, M. R., Gross, A. M., et al. (2024) · Figshare · doi:10.6084/m9.figshare.26082690
Additional file 11 of snRNA-seq of human cutaneous neurofibromas before and after selumetinib treatment implicates role of altered Schwann cell states, inter-cellular signaling, and extracellular matrix in treatment response
Church, C., Fay, C., Kriukov, E., Liu, H., Cannon, A. D., Baldwin, L. A., Crossman, D. K., Korf, B., Wallace, M. R., Gross, A. M., et al. (2024) · Figshare · doi:10.6084/m9.figshare.26737413
Additional file 3 of snRNA-seq of human cutaneous neurofibromas before and after selumetinib treatment implicates role of altered Schwann cell states, inter-cellular signaling, and extracellular matrix in treatment response
Church, C., Fay, C., Kriukov, E., Liu, H., Cannon, A. D., Baldwin, L. A., Crossman, D. K., Korf, B., Wallace, M. R., Gross, A. M., et al. (2024) · Figshare · doi:10.6084/m9.figshare.26737389
Additional file 10 of snRNA-seq of human cutaneous neurofibromas before and after selumetinib treatment implicates role of altered Schwann cell states, inter-cellular signaling, and extracellular matrix in treatment response
Church, C., Fay, C., Kriukov, E., Liu, H., Cannon, A. D., Baldwin, L. A., Crossman, D. K., Korf, B., Wallace, M. R., Gross, A. M., et al. (2024) · Figshare · doi:10.6084/m9.figshare.26737410
Additional file 12 of snRNA-seq of human cutaneous neurofibromas before and after selumetinib treatment implicates role of altered Schwann cell states, inter-cellular signaling, and extracellular matrix in treatment response
Church, C., Fay, C., Kriukov, E., Liu, H., Cannon, A. D., Baldwin, L. A., Crossman, D. K., Korf, B., Wallace, M. R., Gross, A. M., et al. (2024) · Figshare · doi:10.6084/m9.figshare.26737416
MAPK pathway modulation and its implications in KRAS mutant lung adenocarcinoma
Román, S. D. H. (2023) · theses.fr (ABES) · doi:10.70675/8eaccae1ze96bz4279zb69fzaafa5e50c341
Drug response profile-based machine learning enables strategic cell line and compound selection for drug development
Abdel‐Rehim, A., Tate, E., Soldatova, L., & King, R. D. (2026) · Bioinformatics · doi:10.1093/bioinformatics/btag293
A pathway-dependency framework for acquired resistance to targeted therapy in EGFR-mutant, KRAS G12C-mutant, and BRAF V600E-mutant NSCLC
Li, X., Guo, Y., & Yang, S. (2026) · Pharmacological Research · doi:10.1016/j.phrs.2026.108367 · Cited by 1
Spatial modulation of RAF by RAF/MEK glue enables full-dose combination with pan-RAF inhibitor and potent RAS-mutant tumor-selective MAPK and growth inhibition
Orive-Ramos, A., Gaire, B., Adamopoulos, C., Baars, B., Desaunay, M., Kou, Z., Matenoglou, E., Coma, S., Gutiérrez, N., Mohammed, K., et al. (2026) · Cancer Discovery · doi:10.1158/2159-8290.cd-25-1596 · Cited by 1
BindingDB Entry 50000418: Design of a Chemical Probe for the Bromodomain and Plant Homeodomain Finger-Containing (BRPF) Family of Proteins.
BindingDB (2019) · UC San Diego · doi:10.7270/q2p55qzp
BindingDB Entry 50009311: Structure-Based Design and Pharmacokinetic Optimization of Covalent Allosteric Inhibitors of the Mutant GTPase KRAS
BindingDB (2021) · UC San Diego · doi:10.7270/q2f76h10
BindingDB Entry 50000989: Design of a Biased Potent Small Molecule Inhibitor of the Bromodomain and PHD Finger-Containing (BRPF) Proteins Suitable for Cellular and in Vivo Studies.
BindingDB (2020) · UC San Diego · doi:10.7270/q29k4dq5
BindingDB Entry 50017856: Discovery of AZD4625, a Covalent Allosteric Inhibitor of the Mutant GTPase KRAS
BindingDB (2023) · UC San Diego · doi:10.7270/q2w09b1p
BindingDB Entry 50019559: Discovery of AZD4747, a Potent and Selective Inhibitor of Mutant GTPase KRAS
BindingDB (2024) · UC San Diego · doi:10.7270/q2hh6qf7
Targeting Apoptotic Pathways in Melanoma
Hersey, P., & Zhang, X. D. (2011) · Springer eBooks · doi:10.1007/978-1-61779-407-0_9

Authors: Dry, J. R., Pavey, S., Pratilas, C. A., Harbron, C., Runswick, S., Hodgson, D., Chresta, C., McCormack, R., Byrne, N., Cockerill, M., Graham, A., Beran, G., Cassidy, A., Haggerty, C., Brown, H., Ellison, G., Dering, J., Taylor, B. S., Stark, M., Bonazzi, V., Ravishankar, S., Packer, L., Xing, F., Solit, D. B., Finn, R. S., Rosen, N., Hayward, N. K., French, T., & Smith, P. D.
Affiliations: AstraZeneca (United Kingdom) (GB)
Corresponding author: Dry, Jonathan R.
ORCID: Dry, Jonathan R.
Pavey, Sandra
Pratilas, Christine A.
Harbron, Chris
Runswick, Sarah
Hodgson, Darren
Cassidy, Andrew
Brown, Helen
Taylor, Barry S.
Stark, Mitchell
Bonazzi, Vanessa
Xing, Feng
Solit, David B.
Finn, Richard S.
Rosen, Neal
Hayward, Nicholas K.
French, Tim
Smith, Paul D.
Venue: Cancer Research
Publisher: American Association for Cancer Research (AACR)
Published: 2010-03-14
Volume: 70
Issue: 6
Pages: 2264-2273
ISSN: 0008-5472 (ISSN-L)
1538-7445
DOI: 10.1158/0008-5472.can-09-1577
PMC: PMC3166660
OpenAlex: W2128445526
Cited by: 262
References: 46
Citations by year: 2026: 7 · 2025: 11 · 2024: 11 · 2023: 23 · 2022: 13 · 2021: 11 · 2020: 11 · 2019: 17 · 2018: 16 · 2017: 22 · 2016: 17 · 2015: 14 · 2014: 16 · 2013: 23 · 2012: 23
FWCI: 9.50
Type: journal article
Language: en
Open access: green
www.ncbi.nlm.nih.gov
Locations: Cancer Research (publishedVersion)
PubMed (publishedVersion)
Europe PMC (PubMed Central) (acceptedVersion)
PubMed Central (acceptedVersion)
Funders: National Cancer Institute (K08CA127350)
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Melanoma and MAPK Pathways
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Kinase Regulation and GTPase Signaling
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Tyrosine Phosphatases
Keywords: selumetinib, MEK inhibitors, drug resistance, gene expression signatures, phosphatidylinositol 3-kinase, melanoma, cancer cell lines, xenograft models, predictive biomarkers, targeted therapy
MeSH terms: Benzimidazoles, Humans, Neoplasms, Phosphatidylinositol 3-Kinases, Reverse Transcriptase Polymerase Chain Reaction, Gene Expression Profiling, MAP Kinase Kinase Kinases, MAP Kinase Signaling System, Cell Line, Tumor, Proto-Oncogene Proteins B-raf, Proto-Oncogene Proteins c-akt, PTEN Phosphohydrolase

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Transcriptional Pathway Signatures Predict MEK Addiction and Response to Selumetinib (AZD6244)

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