Publications by authors named "Timothy P Heffron"

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Discovery of GNE-6893, a Potent, Selective, Orally Bioavailable Small Molecule Inhibitor of HPK1.
John C Tellis, BinQing Wei, Michael Siu, Le An, Grace Kayan Chan, Timothy P Heffron

ACS Med Chem Lett· September 2024

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Assessment of KRAS G12C Target Engagement by a Covalent Inhibitor in Tumor Biopsies Using an Ultra-Sensitive Immunoaffinity 2D-LC-MS/MS Approach.
Lingyao Meng, Emily W Chan, Carl Ng, Junko Aimi, John C Tran, Timothy P Heffron

Anal Chem· September 2022

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RTK-Dependent Inducible Degradation of Mutant PI3Kα Drives GDC-0077 (Inavolisib) Efficacy.
Kyung W Song, Kyle A Edgar, Emily J Hanan, Marc Hafner, Jason Oeh, Timothy P Heffron

Cancer Discov· January 2022

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Discovery of Spiro-azaindoline Inhibitors of Hematopoietic Progenitor Kinase 1 (HPK1).
Bryan K Chan, Eileen Seward, Michael Lainchbury, Thomas F Brewer, Le An, Timothy P Heffron

ACS Med Chem Lett· January 2022

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Characterization of Antineovascularization Activity and Ocular Pharmacokinetics of Phosphoinositide 3-Kinase/Mammalian Target of Rapamycin Inhibitor GNE-947.
Xingrong Liu, Xiaorong Liang, Jenninfer LeCouter, Savita Ubhayakar, Jacob Chen, Timothy P Heffron

Drug Metab Dispos· May 2020

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Design of a brain-penetrant CDK4/6 inhibitor for glioblastoma.
Sarah M Bronner, Karl A Merrick, Jeremy Murray, Laurent Salphati, John G Moffat, Timothy P Heffron

Bioorg Med Chem Lett· August 2019

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Hematopoietic Progenitor Kinase-1 Structure in a Domain-Swapped Dimer.
Ping Wu, Christopher J Sneeringer, Keith E Pitts, Eric S Day, Bryan K Chan, Timothy P Heffron

Structure· January 2019

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Challenges of developing small-molecule kinase inhibitors for brain tumors and the need for emphasis on free drug levels.
Timothy P Heffron

Neuro Oncol· February 2018

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CNS Anticancer Drug Discovery and Development: 2016 conference insights.
Victor A Levin, Lauren E Abrey, Timothy P Heffron, Peter J Tonge, Arvin C Dar

CNS Oncol· July 2017

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Brain Distribution and Efficacy of the Brain Penetrant PI3K Inhibitor GDC-0084 in Orthotopic Mouse Models of Human Glioblastoma.
Laurent Salphati, Bruno Alicke, Timothy P Heffron, Sheerin Shahidi-Latham, Merry Nishimura

Drug Metab Dispos· December 2016

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Small Molecule Kinase Inhibitors for the Treatment of Brain Cancer.
Timothy P Heffron

J Med Chem· November 2016

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Discovery of a Noncovalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor.
Bryan K Chan, Emily J Hanan, Krista K Bowman, Marian C Bryan, Daniel Burdick, Timothy P Heffron

J Med Chem· October 2016

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Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR.
Timothy P Heffron, Chudi O Ndubaku, Laurent Salphati, Bruno Alicke, Jonathan Cheong

ACS Med Chem Lett· April 2016

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Correction to Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study.
Robert Heald, Krista K Bowman, Marian C Bryan, Daniel Burdick, Bryan Chan, Timothy P Heffron

J Med Chem· March 2016

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The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326).
Timothy P Heffron, Robert A Heald, Chudi Ndubaku, BinQing Wei, Martin Augistin

J Med Chem· February 2016

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4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase.
Emily J Hanan, Matt Baumgardner, Marian C Bryan, Yuan Chen, Charles Eigenbrot, Timothy P Heffron

Bioorg Med Chem Lett· January 2016

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Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR.
Marian C Bryan, Daniel J Burdick, Bryan K Chan, Yuan Chen, Saundra Clausen, Timothy P Heffron

ACS Med Chem Lett· January 2016

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CNS Anticancer Drug Discovery and Development Conference White Paper.
Victor A Levin, Peter J Tonge, James M Gallo, Marc R Birtwistle, Arvin C Dar, Timothy P Heffron

Neuro Oncol· November 2015

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Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study.
Robert Heald, Krista K Bowman, Marian C Bryan, Daniel Burdick, Bryan Chan, Timothy P Heffron

J Med Chem· November 2015

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Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation.
Emily J Hanan, Charles Eigenbrot, Marian C Bryan, Daniel J Burdick, Bryan K Chan, Timothy P Heffron

J Med Chem· December 2014

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Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
Anthony A Estrada, Bryan K Chan, Charles Baker-Glenn, Alan Beresford, Daniel J Burdick, Timothy P Heffron

J Med Chem· February 2014

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Prevalence of acid-reducing agents (ARA) in cancer populations and ARA drug-drug interaction potential for molecular targeted agents in clinical development.
Gillian S Smelick, Timothy P Heffron, Laura Chu, Brian Dean, David A West

Mol Pharm· November 2013

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Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity.
Chudi O Ndubaku, Timothy P Heffron, Steven T Staben, Matthew Baumgardner, Nicole Blaquiere

J Med Chem· June 2013

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Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinase β isoform.
Steven T Staben, Chudi Ndubaku, Nicole Blaquiere, Marcia Belvin, Richard J Bull, Timothy P Heffron

Bioorg Med Chem Lett· May 2013

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Cis-amide isosteric replacement in thienobenzoxepin inhibitors of PI3-kinase.
Steven T Staben, Nicole Blaquiere, Vickie Tsui, Aleksandr Kolesnikov, Steven Do, Timothy P Heffron

Bioorg Med Chem Lett· February 2013

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