Publications by authors named "Darrin Stuart"

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STX-721, a Covalent EGFR/HER2 Exon 20 Inhibitor, Utilizes Exon 20-Mutant Dynamic Protein States and Achieves Unique Mutant Selectivity Across Human Cancer Models.
Raymond A Pagliarini, Jack A Henderson, Benjamin C Milgram, Deanna R Borrelli, Natasja Brooijmans, Darrin D Stuart

Clin Cancer Res· July 2025

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Discovery of STX-721, a Covalent, Potent, and Highly Mutant-Selective EGFR/HER2 Exon20 Insertion Inhibitor for the Treatment of Non-Small Cell Lung Cancer.
Benjamin C Milgram, Deanna R Borrelli, Natasja Brooijmans, Jack A Henderson, Brendan J Hilbert, Darrin D Stuart

J Med Chem· February 2025

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STX-478, a Mutant-Selective, Allosteric PI3Kα Inhibitor Spares Metabolic Dysfunction and Improves Therapeutic Response in PI3Kα-Mutant Xenografts.
Leonard Buckbinder, David J St Jean, Trang Tieu, Brendon Ladd, Brendan Hilbert, Darrin D Stuart

Cancer Discov· November 2023

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Precision Oncology Comes of Age: Designing Best-in-Class Small Molecules by Integrating Two Decades of Advances in Chemistry, Target Biology, and Data Science.
Darrin D Stuart, Angel Guzman-Perez, Natasja Brooijmans, Erica L Jackson, Gregory V Kryukov

Cancer Discov· October 2023

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RAF-Mutant Melanomas Differentially Depend on ERK2 Over ERK1 to Support Aberrant MAPK Pathway Activation and Cell Proliferation.
Matthew S Crowe, Tatiana Zavorotinskaya, Charles F Voliva, Matthew D Shirley, Yanqun Wang, Darrin D Stuart

Mol Cancer Res· June 2021

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LXH254, a Potent and Selective ARAF-Sparing Inhibitor of BRAF and CRAF for the Treatment of MAPK-Driven Tumors.
Kelli-Ann Monaco, Scott Delach, Jing Yuan, Yuji Mishina, Paul Fordjour, Darrin D Stuart

Clin Cancer Res· April 2021

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Design and Discovery of -(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.
Savithri Ramurthy, Benjamin R Taft, Robert J Aversa, Paul A Barsanti, Matthew T Burger, Darrin D Stuart

J Med Chem· March 2020

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Tumor Intrinsic Efficacy by SHP2 and RTK Inhibitors in KRAS-Mutant Cancers.
Huai-Xiang Hao, Hongyun Wang, Chen Liu, Steven Kovats, Roberto Velazquez, Darrin D Stuart

Mol Cancer Ther· December 2019

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Distinct Transcriptional Programming Drive Response to MAPK Inhibition in -Mutant Melanoma Patient-Derived Xenografts.
Tianshu Feng, Javad Golji, Ailing Li, Xiamei Zhang, David A Ruddy, Darrin D Stuart

Mol Cancer Ther· December 2019

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Hyperactivation of MAPK Signaling Is Deleterious to RAS/RAF-mutant Melanoma.
Grace P Leung, Tianshu Feng, Frederic D Sigoillot, Felipe C Geyer, Matthew D Shirley, Darrin D Stuart

Mol Cancer Res· January 2019

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Allele-Specific Mechanisms of Activation of MEK1 Mutants Determine Their Properties.
Yijun Gao, Matthew T Chang, Daniel McKay, Na Na, Bing Zhou, Darrin Stuart

Cancer Discov· May 2018

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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.
Wenlin Shao, Yuji M Mishina, Yun Feng, Giordano Caponigro, Vesselina G Cooke, Darrin D Stuart

Cancer Res· March 2018

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Imidazo[1,2-a]pyridin-6-yl-benzamide analogs as potent RAF inhibitors.
Aaron Smith, Zhi-Jie Ni, Daniel Poon, Zilin Huang, Zheng Chen, Darrin Stuart

Bioorg Med Chem Lett· December 2017

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Inhibition of prenylated KRAS in a lipid environment.
Johanna M Jansen, Charles Wartchow, Wolfgang Jahnke, Susan Fong, Tiffany Tsang, Darrin Stuart

PLoS One· September 2017

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Phase I Dose-Escalation and -Expansion Study of the BRAF Inhibitor Encorafenib (LGX818) in Metastatic -Mutant Melanoma.
Jean-Pierre Delord, Caroline Robert, Marta Nyakas, Grant A McArthur, Ragini Kudchakar, Darrin D Stuart

Clin Cancer Res· September 2017

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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.
Gisele A Nishiguchi, Alice Rico, Huw Tanner, Robert J Aversa, Benjamin R Taft, Darrin D Stuart

J Med Chem· June 2017

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Discovery of a Selective and Potent Inhibitor of Mitogen-Activated Protein Kinase-Interacting Kinases 1 and 2 (MNK1/2) Utilizing Structure-Based Drug Design.
Wooseok Han, Yu Ding, Yongjin Xu, Keith Pfister, Shejin Zhu, Darrin D Stuart

J Med Chem· April 2016

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Discovery of RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma.
Teresa E Williams, Sharadha Subramanian, Joelle Verhagen, Christopher M McBride, Abran Costales, Darrin Stuart

ACS Med Chem Lett· September 2015

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Ligand-independent EPHA2 signaling drives the adoption of a targeted therapy-mediated metastatic melanoma phenotype.
Kim H T Paraiso, Meghna Das Thakur, Bin Fang, John M Koomen, Inna V Fedorenko, Darrin Stuart

Cancer Discov· March 2015

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Correction to Design and Synthesis of Orally Bioavailable Benzimidazole Reverse Amides as Pan RAF Kinase Inhibitors.
Sharadha Subramanian, Abran Costales, Teresa E Williams, Barry Levine, Christopher M McBride, Darrin Stuart

ACS Med Chem Lett· December 2014

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Molecular profiling of patient-matched brain and extracranial melanoma metastases implicates the PI3K pathway as a therapeutic target.
Guo Chen, Nitin Chakravarti, Kimberly Aardalen, Alexander J Lazar, Michael T Tetzlaff, Darrin Stuart

Clin Cancer Res· November 2014

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Design and Synthesis of Orally Bioavailable Benzimidazole Reverse Amides as Pan RAF Kinase Inhibitors.
Sharadha Subramanian, Abran Costales, Teresa E Williams, Barry Levine, Christopher M McBride, Darrin Stuart

ACS Med Chem Lett· September 2014

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Vemurafenib cooperates with HPV to promote initiation of cutaneous tumors.
Matthew Holderfield, Edward Lorenzana, Ben Weisburd, Lisa Lomovasky, Lise Boussemart, Darrin Stuart

Cancer Res· April 2014

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Molecular pathways: response and resistance to BRAF and MEK inhibitors in BRAF(V600E) tumors.
Meghna Das Thakur, Darrin D Stuart

Clin Cancer Res· March 2014

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The evolution of melanoma resistance reveals therapeutic opportunities.
Meghna Das Thakur, Darrin D Stuart

Cancer Res· October 2013

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