Publications by authors named "Lars D Engstrom"

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Combination of the MTA-Cooperative PRMT5 Inhibitor BMS-986504 and KRAS Inhibitors Is an Effective Treatment Strategy for MTAP-Deleted KRAS-Mutant Pancreatic Cancer.
Kristina Drizyte-Miller, Lars D Engstrom, Jeffrey A Klomp, Clint A Stalnecker, Addison G Stamey

Cancer Res· September 2025

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The SOS1 Inhibitor MRTX0902 Blocks KRAS Activation and Demonstrates Antitumor Activity in Cancers Dependent on KRAS Nucleotide Loading.
Niranjan Sudhakar, Larry Yan, Fadia Qiryaqos, Lars D Engstrom, Jade Laguer

Mol Cancer Ther· October 2024

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Discovery of Pyridopyrimidinones that Selectively Inhibit the H1047R PI3Kα Mutant Protein.
John M Ketcham, Stephen J Harwood, Ruth Aranda, Athenea N Aloiau, Briana M Bobek, Lars D Engstrom

J Med Chem· March 2024

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MRTX1719 Is an MTA-Cooperative PRMT5 Inhibitor That Exhibits Synthetic Lethality in Preclinical Models and Patients with MTAP-Deleted Cancer.
Lars D Engstrom, Ruth Aranda, Laura Waters, Krystal Moya, Vickie Bowcut

Cancer Discov· November 2023

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Design and evaluation of achiral, non-atropisomeric 4-(aminomethyl)phthalazin-1(2H)-one derivatives as novel PRMT5/MTA inhibitors.
Christopher R Smith, Ruth Aranda, James G Christensen, Lars D Engstrom, Robin J Gunn

Bioorg Med Chem· October 2022

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Anti-tumor efficacy of a potent and selective non-covalent KRAS inhibitor.
Jill Hallin, Vickie Bowcut, Andrew Calinisan, David M Briere, Lauren Hargis, Lars D Engstrom

Nat Med· October 2022

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Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of -Deleted Cancers.
Christopher R Smith, Ruth Aranda, Thomas P Bobinski, David M Briere, Aaron C Burns, Lars D Engstrom

J Med Chem· February 2022

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The KRAS Inhibitor MRTX849 Reconditions the Tumor Immune Microenvironment and Sensitizes Tumors to Checkpoint Inhibitor Therapy.
David M Briere, Shuai Li, Andrew Calinisan, Niranjan Sudhakar, Ruth Aranda, Lars D Engstrom

Mol Cancer Ther· June 2021

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Acquired Resistance to KRAS Inhibition in Cancer.
Mark M Awad, Shengwu Liu, Igor I Rybkin, Kathryn C Arbour, Julien Dilly, Lars D Engstrom

N Engl J Med· June 2021

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The KRAS Inhibitor MRTX849 Provides Insight toward Therapeutic Susceptibility of KRAS-Mutant Cancers in Mouse Models and Patients.
Jill Hallin, Lars D Engstrom, Lauren Hargis, Andrew Calinisan, Ruth Aranda

Cancer Discov· January 2020

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The class I/IV HDAC inhibitor mocetinostat increases tumor antigen presentation, decreases immune suppressive cell types and augments checkpoint inhibitor therapy.
David Briere, Niranjan Sudhakar, David M Woods, Jill Hallin, Lars D Engstrom

Cancer Immunol Immunother· March 2018

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Glesatinib Exhibits Antitumor Activity in Lung Cancer Models and Patients Harboring Exon 14 Mutations and Overcomes Mutation-mediated Resistance to Type I MET Inhibitors in Nonclinical Models.
Lars D Engstrom, Ruth Aranda, Matthew Lee, Elizabeth A Tovar, Curt J Essenburg

Clin Cancer Res· November 2017

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PF-06463922, an ALK/ROS1 Inhibitor, Overcomes Resistance to First and Second Generation ALK Inhibitors in Preclinical Models.
Helen Y Zou, Luc Friboulet, David P Kodack, Lars D Engstrom, Qiuhua Li

Cancer Cell· July 2015

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PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations.
Helen Y Zou, Qiuhua Li, Lars D Engstrom, Melissa West, Vicky Appleman

Proc Natl Acad Sci U S A· March 2015

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Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain exposure and broad-spectrum potency against ALK-resistant mutations.
Ted W Johnson, Paul F Richardson, Simon Bailey, Alexei Brooun, Benjamin J Burke, Lars D Engstrom

J Med Chem· June 2014

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Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib.
Qinhua Huang, Ted W Johnson, Simon Bailey, Alexei Brooun, Kevin D Bunker, Lars D Engstrom

J Med Chem· February 2014

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Sensitivity of selected human tumor models to PF-04217903, a novel selective c-Met kinase inhibitor.
Helen Y Zou, Qiuhua Li, Joseph H Lee, Maria E Arango, Kristina Burgess, Lars D Engstrom

Mol Cancer Ther· April 2012

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Mxi1-0, an alternatively transcribed Mxi1 isoform, is overexpressed in glioblastomas.
Lars D Engstrom, Andrew S Youkilis, Judith L Gorelick, Datong Zheng, Valerie Ackley

Neoplasia· April 2005

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A novel chromosomal inversion at 11q23 in infant acute myeloid leukemia fuses MLL to CALM, a gene that encodes a clathrin assembly protein.
Daniel S Wechsler, Lars D Engstrom, Brian M Alexander, David G Motto, Diane Roulston

Genes Chromosomes Cancer· January 2003

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