Publications by authors named "Adrian Gill"

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Correction: Translational and Therapeutic Evaluation of RAS-GTP Inhibition by RMC-6236 in RAS-Driven Cancers.
Jingjing Jiang, Lingyan Jiang, Benjamin J Maldonato, Yingyun Wang, Matthew Holderfield, Adrian L Gill

Cancer Discov· October 2025

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Targeting the MYC oncogene with a selective bi-steric mTORC1 inhibitor elicits tumor regression in MYC-driven cancers.
Wadie D Mahauad-Fernandez, Yu Chi Yang, Ian Lai, Jangho Park, Lilian Yao, Adrian L Gill

Cell Chem Biol· August 2025

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A neomorphic protein interface catalyzes covalent inhibition of RAS aspartic acid in tumors.
Caroline Weller, G Leslie Burnett, Lingyan Jiang, Sujata Chakraborty, Dongyu Zhang, Adrian L Gill

Science· July 2025

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Discovery of Elironrasib (RMC-6291), a Potent and Orally Bioavailable, RAS(ON) G12C-Selective, Covalent Tricomplex Inhibitor for the Treatment of Patients with RAS G12C-Addicted Cancers.
James Cregg, Kristof Pota, Aidan C A Tomlinson, Jason Yano, Abby Marquez, Adrian L Gill

J Med Chem· March 2025

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Discovery of Daraxonrasib (RMC-6236), a Potent and Orally Bioavailable RAS(ON) Multi-selective, Noncovalent Tri-complex Inhibitor for the Treatment of Patients with Multiple RAS-Addicted Cancers.
James Cregg, Anne V Edwards, Stephanie Chang, Bianca J Lee, John E Knox, Adrian L Gill

J Med Chem· March 2025

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Translational and Therapeutic Evaluation of RAS-GTP Inhibition by RMC-6236 in RAS-Driven Cancers.
Jingjing Jiang, Lingyan Jiang, Benjamin J Maldonato, Yingyun Wang, Matthew Holderfield, Adrian L Gill

Cancer Discov· June 2024

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Concurrent inhibition of oncogenic and wild-type RAS-GTP for cancer therapy.
Matthew Holderfield, Bianca J Lee, Jingjing Jiang, Aidan Tomlinson, Kyle J Seamon, Adrian L Gill

Nature· May 2024

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Chemical remodeling of a cellular chaperone to target the active state of mutant KRAS.
Christopher J Schulze, Kyle J Seamon, Yulei Zhao, Yu C Yang, Jim Cregg, Adrian L Gill

Science· August 2023

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Discovery of RMC-5552, a Selective Bi-Steric Inhibitor of mTORC1, for the Treatment of mTORC1-Activated Tumors.
G Leslie Burnett, Yu C Yang, James B Aggen, Jennifer Pitzen, Micah K Gliedt, Adrian L Gill

J Med Chem· January 2023

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Automated iterative Csp-C bond formation.
Daniel J Blair, Sriyankari Chitti, Melanie Trobe, David M Kostyra, Hannah M S Haley, Adrian L Gill

Nature· April 2022

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Small molecule Son of Sevenless 1 (SOS1) inhibitors: a review of the patent literature.
Severin K Thompson, Andreas Buckl, Alexander G Dossetter, Ed Griffen, Adrian Gill

Expert Opin Ther Pat· December 2021

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Author Correction: Selective inhibitors of mTORC1 activate 4EBP1 and suppress tumor growth.
Bianca J Lee, Jacob A Boyer, G Leslie Burnett, Arun P Thottumkara, Nidhi Tibrewal, Adrian L Gill

Nat Chem Biol· November 2021

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Selective inhibitors of mTORC1 activate 4EBP1 and suppress tumor growth.
Bianca J Lee, Jacob A Boyer, G Leslie Burnett, Arun P Thottumkara, Nidhi Tibrewal, Adrian L Gill

Nat Chem Biol· October 2021

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Author Correction: Selective inhibitors of mTORC1 activate 4EBP1 and suppress tumor growth.
Bianca J Lee, Jacob A Boyer, G Leslie Burnett, Arun P Thottumkara, Nidhi Tibrewal, Adrian L Gill

Nat Chem Biol· August 2021

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Allosteric Inhibition of SHP2 Stimulates Antitumor Immunity by Transforming the Immunosuppressive Environment.
Elsa Quintana, Christopher J Schulze, Darienne R Myers, Tiffany J Choy, Kasia Mordec, Adrian L Gill

Cancer Res· July 2020

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RAS nucleotide cycling underlies the SHP2 phosphatase dependence of mutant BRAF-, NF1- and RAS-driven cancers.
Robert J Nichols, Franziska Haderk, Carlos Stahlhut, Christopher J Schulze, Golzar Hemmati, Adrian L Gill

Nat Cell Biol· September 2018

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Structure guided lead generation for M. tuberculosis thymidylate kinase (Mtb TMK): discovery of 3-cyanopyridone and 1,6-naphthyridin-2-one as potent inhibitors.
Maruti Naik, Anandkumar Raichurkar, Balachandra S Bandodkar, Begur V Varun, Shantika Bhat, Adrian Gill

J Med Chem· January 2015

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Heart regeneration: opportunities and challenges for drug discovery with novel chemical and therapeutic methods or agents.
Alleyn T Plowright, Ola Engkvist, Adrian Gill, Laurent Knerr, Qing-Dong Wang

Angew Chem Int Ed Engl· April 2014

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Using matched molecular series as a predictive tool to optimize biological activity.
Noel M O'Boyle, Jonas Boström, Roger A Sayle, Adrian Gill

J Med Chem· March 2014

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Stapled Vasoactive Intestinal Peptide (VIP) Derivatives Improve VPAC2 Agonism and Glucose-Dependent Insulin Secretion.
Fabrizio Giordanetto, Jefferson D Revell, Laurent Knerr, Marie Hostettler, Amalia Paunovic, Adrian Gill

ACS Med Chem Lett· December 2013

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What is the most important approach in current drug discovery: doing the right things or doing things right?
Thomas Elebring, Adrian Gill, Alleyn T Plowright

Drug Discov Today· November 2012

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Optimisation of pharmacokinetic properties in a neutral series of 11β-HSD1 inhibitors.
James S Scott, Adrian L Gill, Linda Godfrey, Sam D Groombridge, Amanda Rees

Bioorg Med Chem Lett· November 2012

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Kinetic efficiency: the missing metric for enhancing compound quality?
Geoffrey A Holdgate, Adrian L Gill

Drug Discov Today· November 2011

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A novel series of IKKβ inhibitors part II: description of a potent and pharmacologically active series of analogs.
Timothy D Cushing, Vijay Baichwal, Karen Berry, Roland Billedeau, Viola Bordunov, Adrian Gill

Bioorg Med Chem Lett· January 2011

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A novel series of IKKβ inhibitors part I: Initial SAR studies of a HTS hit.
Timothy D Cushing, Vijay Baichwal, Karen Berry, Roland Billedeau, Viola Bordunov, Adrian Gill

Bioorg Med Chem Lett· January 2011

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