ASN007 is a selective ERK1/2 inhibitor with preferential activity against RAS-and RAF-mutant tumors
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V. Seshan | E. de Stanchina | A. Younes | A. Knezevic | Sanjeeva P. Reddy | R. Smith | Scott Thompson | A. Portelinha | L. Denis | Mariana da Silva Ferreira | Zahra Asgari | Sandeep Gupta | Ana Portelinha
[1] N. Chen,et al. Discovery of a covalent inhibitor of KRASG12C (AMG 510) for the treatment of solid tumors. , 2019, Journal of medicinal chemistry.
[2] J. Fernandez-Banet,et al. The KRASG12C Inhibitor, MRTX849, Provides Insight Toward Therapeutic Susceptibility of KRAS Mutant Cancers in Mouse Models and Patients. , 2019, Cancer discovery.
[3] Shan Zhu,et al. Co-targeting PI3K/Akt and MAPK/ERK pathways leads to an enhanced antitumor effect on human hypopharyngeal squamous cell carcinoma , 2019, Journal of Cancer Research and Clinical Oncology.
[4] R. Yaeger,et al. Targeting Alterations in the RAF-MEK Pathway. , 2019, Cancer discovery.
[5] L. Bryan,et al. Spotlight on copanlisib and its potential in the treatment of relapsed/refractory follicular lymphoma: evidence to date , 2018, OncoTargets and therapy.
[6] S. Cook,et al. ERK1/2 inhibitors: New weapons to inhibit the RAS‐regulated RAF‐MEK1/2‐ERK1/2 pathway , 2018, Pharmacology & therapeutics.
[7] Ton Wang,et al. BRAF and MEK Inhibitors: Use and Resistance in BRAF-Mutated Cancers , 2018, Drugs.
[8] Jeffrey W. Clark,et al. Convergent Therapeutic Strategies to Overcome the Heterogeneity of Acquired Resistance in BRAFV600E Colorectal Cancer. , 2018, Cancer discovery.
[9] Min Huang,et al. Targeting ERK, an Achilles' Heel of the MAPK pathway, in cancer therapy , 2018, Acta pharmaceutica Sinica. B.
[10] A. Markham. Copanlisib: First Global Approval , 2017, Drugs.
[11] R. Sullivan,et al. Phase I Dose-Escalation and -Expansion Study of the BRAF Inhibitor Encorafenib (LGX818) in Metastatic BRAF-Mutant Melanoma , 2017, Clinical Cancer Research.
[12] A. Azmi,et al. Targeting ERK enhances the cytotoxic effect of the novel PI3K and mTOR dual inhibitor VS-5584 in preclinical models of pancreatic cancer , 2017, Oncotarget.
[13] M. Souweidane,et al. Dual Inhibition of PI3K/AKT and MEK/ERK Pathways Induces Synergistic Antitumor Effects in Diffuse Intrinsic Pontine Glioma Cells , 2017, Translational oncology.
[14] R. Scolyer,et al. Resistance to combination BRAF and MEK inhibition in metastatic melanoma: Where to next? , 2016, European journal of cancer.
[15] Dolores Diaz,et al. Discovery of (S)-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Development. , 2016, Journal of medicinal chemistry.
[16] S. Rajagopal,et al. Determination of ulixertinib in mice plasma by LC-MS/MS and its application to a pharmacokinetic study in mice. , 2016, Journal of pharmaceutical and biomedical analysis.
[17] S. Cook,et al. MEK1 and MEK2 inhibitors and cancer therapy: the long and winding road , 2015, Nature Reviews Cancer.
[18] P. Poulikakos,et al. Targeting RAS–ERK signalling in cancer: promises and challenges , 2014, Nature Reviews Drug Discovery.
[19] P. Ascierto,et al. Combined vemurafenib and cobimetinib in BRAF-mutated melanoma. , 2014, The New England journal of medicine.
[20] H. Soares,et al. Suppression of Feedback Loops Mediated by PI3K/mTOR Induces Multiple Overactivation of Compensatory Pathways: An Unintended Consequence Leading to Drug Resistance , 2014, Molecular Cancer Therapeutics.
[21] R. Neve,et al. AXL inhibition sensitizes mesenchymal cancer cells to antimitotic drugs. , 2014, Cancer research.
[22] Dirk Schadendorf,et al. Safety and efficacy of vemurafenib in BRAF(V600E) and BRAF(V600K) mutation-positive melanoma (BRIM-3): extended follow-up of a phase 3, randomised, open-label study. , 2014, The Lancet. Oncology.
[23] K. Flaherty,et al. BRAF in Melanoma: Current Strategies and Future Directions , 2013, Clinical Cancer Research.
[24] V. Sondak,et al. Paradoxical oncogenesis—the long-term effects of BRAF inhibition in melanoma , 2013, Nature Reviews Clinical Oncology.
[25] Shuxia Zhao,et al. Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors. , 2013, Cancer discovery.
[26] R. Sullivan,et al. Resistance to BRAF-targeted therapy in melanoma. , 2013, European journal of cancer.
[27] K. Kinzler,et al. Cancer Genome Landscapes , 2013, Science.
[28] K. Flaherty,et al. Activity of the oral MEK inhibitor trametinib in patients with advanced melanoma: a phase 1 dose-escalation trial. , 2012, The Lancet. Oncology.
[29] A. Hauschild,et al. Dabrafenib in BRAF-mutated metastatic melanoma: a multicentre, open-label, phase 3 randomised controlled trial , 2012, The Lancet.
[30] Kwang-Hyun Cho,et al. The crossregulation between ERK and PI3K signaling pathways determines the tumoricidal efficacy of MEK inhibitor. , 2012, Journal of molecular cell biology.
[31] L. Donehower,et al. Mouse Tissues that Undergo Neoplastic Progression after K-Ras Activation Are Distinguished by Nuclear Translocation of phospho-Erk1/2 and Robust Tumor Suppressor Responses , 2012, Molecular Cancer Research.
[32] A. Hauschild,et al. Improved survival with vemurafenib in melanoma with BRAF V600E mutation. , 2011, The New England journal of medicine.
[33] Stephen L. Abrams,et al. Ras/Raf/MEK/ERK and PI3K/PTEN/Akt/mTOR Inhibitors: Rationale and Importance to Inhibiting These Pathways in Human Health , 2011, Oncotarget.
[34] Rony Seger,et al. The ERK Cascade: Distinct Functions within Various Subcellular Organelles. , 2011, Genes & cancer.
[35] J. Settleman,et al. Targeting the RAF-MEK-ERK pathway in cancer therapy. , 2009, Cancer letters.
[36] J. Lehár,et al. High-order combination effects and biological robustness , 2008, Molecular systems biology.
[37] P. Pandolfi,et al. Identification of S664 TSC2 phosphorylation as a marker for extracellular signal-regulated kinase mediated mTOR activation in tuberous sclerosis and human cancer. , 2007, Cancer research.
[38] O. Rath,et al. MAP kinase signalling pathways in cancer , 2007, Oncogene.
[39] L. Cantley,et al. ERK Negatively Regulates the Epidermal Growth Factor-mediated Interaction of Gab1 and the Phosphatidylinositol 3-Kinase* , 2002, The Journal of Biological Chemistry.
[40] Dennis C. Friedrich,et al. MAP kinase pathway alterations in BRAF-mutant melanoma patients with acquired resistance to combined RAF/MEK inhibition. , 2014, Cancer discovery.
[41] A. McKenna,et al. The genetic landscape of clinical resistance to RAF inhibition in metastatic melanoma. , 2014, Cancer discovery.