Publications by authors named "Gregory Locke"

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Design, Synthesis, and T Cell Checkpoint Combination Potential Of First-In-Class DGKα/ζ Inhibitor BMS-986408.
Denise C Grünenfelder, Upender Velaparthi, Jayakumar S Warrier, Louis Chupak, Chetan Padmakar Darne, Gregory Locke

J Med Chem· October 2025

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Discovery of BMS-986408, a First-In-Class Dual DGKα and DGKζ Inhibitor that Unleashes PD-1 Checkpoint and CAR T-cell Immunotherapies.
Michael Wichroski, Si-Qi Liu, Lauren M Zasadil, Joseph L Benci, Patrick C Gedeon, Gregory Locke

Cancer Immunol Res· September 2025

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Discovery and Synthesis of Heterobifunctional Degraders of Rearranged during Transfection (RET) Kinase.
Jennifer X Qiao, David Williams, Patrice Gill, Ling Li, Derek Norris, Gregory Locke

J Med Chem· November 2024

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DGKα/ζ inhibitors combine with PD-1 checkpoint therapy to promote T cell-mediated antitumor immunity.
Michael Wichroski, Joseph Benci, Si-Qi Liu, Louis Chupak, Jie Fang, Gregory Locke

Sci Transl Med· October 2023

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Identification and characterization of TYK2 pseudokinase domain stabilizers that allosterically inhibit TYK2 signaling.
Gregory A Locke, Jodi Muckelbauer, John S Tokarski, Christopher M Barbieri, Stefan Belić

Methods Enzymol· May 2022

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Discovery of Non-Nucleotide Small-Molecule STING Agonists Chemotype Hybridization.
Emily C Cherney, Liping Zhang, Julian Lo, Tram Huynh, Donna Wei, Gregory A Locke

J Med Chem· February 2022

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Small molecule and macrocyclic pyrazole derived inhibitors of myeloperoxidase (MPO).
Carol H Hu, Meriah W Neissel Valente, O Scott Halpern, Sutjano Jusuf, Javed A Khan, Gregory A Locke

Bioorg Med Chem Lett· June 2021

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Discovery of Orally Active Isofuranones as Potent, Selective Inhibitors of Hematopoetic Progenitor Kinase 1.
Andrew P Degnan, Godwin K Kumi, Christopher W Allard, Erika V Araujo, Walter L Johnson, Gregory A Locke

ACS Med Chem Lett· March 2021

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Enhanced antitumor immunity by a novel small molecule HPK1 inhibitor.
Dan You, Stephen Hillerman, Gregory Locke, Charu Chaudhry, Caitlyn Stromko

J Immunother Cancer· January 2021

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Discovery and structure activity relationships of 7-benzyl triazolopyridines as stable, selective, and reversible inhibitors of myeloperoxidase.
Scott A Shaw, Benjamin P Vokits, Andrew K Dilger, Andrew Viet, Charles G Clark, Gregory A Locke

Bioorg Med Chem· November 2020

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Identification of Reversible Small Molecule Inhibitors of Endothelial Lipase (EL) That Demonstrate HDL-C Increase In Vivo.
George Tora, Soong-Hoon Kim, Zulan Pi, James A Johnson, Ji Jiang, Gregory Locke

J Med Chem· February 2020

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Benzothiazole-based compounds as potent endothelial lipase inhibitors.
Wei Meng, Leonard P Adam, Kamelia Behnia, Lei Zhao, Richard Yang, Gregory A Locke

Bioorg Med Chem Lett· October 2019

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Corrigendum to "Identification of substituted benzothiazole sulfones as potent and selective inhibitors of endothelial lipase" [Bioorg. Med. Chem. Lett. 29 (2019) 1918-1921].
Soong-Hoon Kim, James A Johnson, Ji Jiang, Brandon Parkhurst, Monique Phillips, Gregory Locke

Bioorg Med Chem Lett· September 2019

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Identification of substituted benzothiazole sulfones as potent and selective inhibitors of endothelial lipase.
Soong-Hoon Kim, James A Johnson, Ji Jiang, Brandon Parkhurst, Monique Phillips, Gregory Locke

Bioorg Med Chem Lett· August 2019

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Potent Triazolopyridine Myeloperoxidase Inhibitors.
Nicholas R Wurtz, Andrew Viet, Scott A Shaw, Andrew Dilger, Meriah N Valente, Gregory A Locke

ACS Med Chem Lett· December 2018

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Sulfonylated Benzothiazoles as Inhibitors of Endothelial Lipase.
James A Johnson, George Tora, Zulan Pi, Monique Phillips, Xiaohong Yin, Gregory Locke

ACS Med Chem Lett· December 2018

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Triazolopyrimidines identified as reversible myeloperoxidase inhibitors.
Franck Duclos, Lynn M Abell, David G Harden, Kristen Pike, Kimberly Nowak, Gregory A Locke

Medchemcomm· November 2017

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Potency, selectivity and prolonged binding of saxagliptin to DPP4: maintenance of DPP4 inhibition by saxagliptin in vitro and ex vivo when compared to a rapidly-dissociating DPP4 inhibitor.
Aiying Wang, Charles Dorso, Lisa Kopcho, Gregory Locke, Robert Langish

BMC Pharmacol· April 2012

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Differential activation of recombinant human acetyl-CoA carboxylases 1 and 2 by citrate.
Gregory A Locke, Dong Cheng, Mark R Witmer, James K Tamura, Tasir Haque

Arch Biochem Biophys· July 2008

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Expression, purification, and characterization of human and rat acetyl coenzyme A carboxylase (ACC) isozymes.
Dong Cheng, Ching-Hsuen Chu, Luping Chen, John N Feder, Gabe A Mintier, Gregory A Locke

Protein Expr Purif· January 2007

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