Search Results - "Mathews Griner, Lesley A"
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High-throughput combinatorial screening identifies drugs that cooperate with ibrutinib to kill activated B-cell–like diffuse large B-cell lymphoma cells
Published in Proceedings of the National Academy of Sciences - PNAS (11-02-2014)“…The clinical development of drug combinations is typically achieved through trial-and-error or via insight gained through a detailed molecular understanding of…”
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Selective targeting of JAK/STAT signaling is potentiated by Bcl-xL blockade in IL-2–dependent adult T-cell leukemia
Published in Proceedings of the National Academy of Sciences - PNAS (06-10-2015)“…Adult T-cell leukemia (ATL) develops in individuals infected with human T-cell lymphotropic virus-1 (HTLV-1). Presently there is no curative therapy for ATL…”
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Blockade of oncogenic IκB kinase activity in diffuse large B-cell lymphoma by bromodomain and extraterminal domain protein inhibitors
Published in Proceedings of the National Academy of Sciences - PNAS (05-08-2014)“…In the activated B-cell–like (ABC) subtype of diffuse large B-cell lymphoma (DLBCL), NF-κB activity is essential for viability of the malignant cells and is…”
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Antitumor Properties of RAF709, a Highly Selective and Potent Inhibitor of RAF Kinase Dimers, in Tumors Driven by Mutant RAS or BRAF
Published in Cancer research (Chicago, Ill.) (15-03-2018)“…Resistance to the RAF inhibitor vemurafenib arises commonly in melanomas driven by the activated BRAF oncogene. Here, we report antitumor properties of RAF709,…”
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Large-scale pharmacological profiling of 3D tumor models of cancer cells
Published in Cell death & disease (01-12-2016)“…The discovery of chemotherapeutic agents for the treatment of cancer commonly uses cell proliferation assays in which cells grow as two-dimensional (2D)…”
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Aurora B kinase is a potent and selective target in MYCN-driven neuroblastoma
Published in Oncotarget (03-11-2015)“…Despite advances in multimodal treatment, neuroblastoma (NB) is often fatal for children with high-risk disease and many survivors need to cope with long-term…”
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A high throughput screening assay system for the identification of small molecule inhibitors of gsp
Published in PloS one (25-03-2014)“…Mis-sense mutations in the α-subunit of the G-protein, Gsα, cause fibrous dysplasia of bone/McCune-Albright syndrome. The biochemical outcome of these…”
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Scaffolding Protein Connector Enhancer of Kinase Suppressor of Ras 1 (CNKSR1) Regulates MAPK Inhibition Responsiveness in Pancreas Cancer via Crosstalk with AKT Signaling
Published in Molecular cancer research (01-04-2023)“…Combinatorial molecular therapy in pancreatic ductal adenocarcinoma (PDAC) has yielded largely disappointing results in clinical testing to-date as a multitude…”
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Discovery and Optimization of Pyrrolopyrimidine Derivatives as Selective Disruptors of the Perinucleolar Compartment, a Marker of Tumor Progression toward Metastasis
Published in Journal of medicinal chemistry (23-06-2022)“…The perinucleolar compartment (PNC) is a dynamic subnuclear body found at the periphery of the nucleolus. The PNC is enriched with RNA transcripts and…”
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High-throughput matrix screening identifies synergistic and antagonistic antimalarial drug combinations
Published in Scientific reports (25-09-2015)“…Drug resistance in Plasmodium parasites is a constant threat. Novel therapeutics, especially new drug combinations, must be identified at a faster rate. In…”
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Target Deconvolution of a Multikinase Inhibitor with Antimetastatic Properties Identifies TAOK3 as a Key Contributor to a Cancer Stem Cell-Like Phenotype
Published in Molecular cancer therapeutics (01-11-2019)“…Pancreatic cancer remains an incurable condition. Its progression is driven, in part, by subsets of cancer cells that evade the cytotoxic effects of…”
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Design and Discovery of N‑(2-Methyl-5′-morpholino-6′-((tetrahydro‑2H‑pyran-4-yl)oxy)-[3,3′-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers
Published in Journal of medicinal chemistry (22-06-2017)“…RAS oncogenes have been implicated in >30% of human cancers, all representing high unmet medical need. The exquisite dependency on CRAF kinase in KRAS mutant…”
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Identification of Small Molecule Enhancers of Immunotherapy for Melanoma
Published in Scientific reports (30-03-2020)“…Small molecule based targeted therapies for the treatment of metastatic melanoma hold promise but responses are often not durable, and tumors frequently…”
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Ranking Differential Drug Activities from Dose-Response Synthetic Lethality Screens
Published in Journal of biomolecular screening (01-10-2016)“…Synthetic lethal screens are used to discover new combination treatments for cancer. In traditional high-throughput synthetic lethal screens, compounds are…”
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Design and Discovery of N‑(3-(2-(2-Hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide, a Selective, Efficacious, and Well-Tolerated RAF Inhibitor Targeting RAS Mutant Cancers: The Path to the Clinic
Published in Journal of medicinal chemistry (12-03-2020)“…Direct pharmacological inhibition of RAS has remained elusive, and efforts to target CRAF have been challenging due to the complex nature of RAF signaling,…”
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SU9516 Increases α7β1 Integrin and Ameliorates Disease Progression in the mdx Mouse Model of Duchenne Muscular Dystrophy
Published in Molecular therapy (07-06-2017)“…Duchenne muscular dystrophy (DMD) is a fatal muscle disease caused by mutations in the dystrophin gene, resulting in a complete loss of the dystrophin protein…”
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Mutation Profiles in Glioblastoma 3D Oncospheres Modulate Drug Efficacy
Published in SLAS technology (01-02-2019)“…Glioblastoma (GBM) is a lethal brain cancer with a median survival time of approximately 15 months following treatment. Common in vitro GBM models for drug…”
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Target deconvolution of a multikinase inhibitor with anti-metastatic properties identifies TAOK3 as a key contributor to a cancer stem cell-like phenotype
Published in Molecular cancer therapeutics (08-08-2019)“…Pancreatic cancer remains an incurable condition. Its progression is driven, in part, by subsets of cancer cells that evade the cytotoxic effects of…”
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Abstract DDT01-04: Pharmacological profile and anti-tumor properties of LXH254, a highly selective RAF kinase inhibitor
Published in Cancer research (Chicago, Ill.) (01-07-2018)“…Abstract The mitogen-activated protein kinase (MAPK) signaling pathway is frequently activated in human cancers due to genetic alterations that can occur at…”
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Abstract B31: Combined siRNA and small molecule screening identifies Aurora B kinase as an effective target in MYCN-driven neuroblastoma
Published in Cancer research (Chicago, Ill.) (01-03-2016)“…Abstract Despite advances in multimodal treatment, neuroblastoma (NB) is often fatal for children with high-risk disease and many survivors need to cope with…”
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