Publications by authors named "John Sack"

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Orthosteric STING inhibition elucidates molecular correction of SAVI STING.
Tao Xie, Max Ruzanov, David Critton, Leidy Merselis, Joseph Naglich, John S Sack

Nat Commun· July 2025

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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, John S Sack

J Med Chem· February 2022

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X-ray structure of a human cardiac muscle troponin C/troponin I chimera in two crystal forms.
Chunhong Yan, John S Sack

Acta Crystallogr F Struct Biol Commun· January 2022

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Azatricyclic Inverse Agonists of RORγt That Demonstrate Efficacy in Models of Rheumatoid Arthritis and Psoriasis.
Qingjie Liu, Hai-Yun Xiao, Douglas G Batt, Zili Xiao, Yeheng Zhu, John S Sack

ACS Med Chem Lett· May 2021

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Substituted diaryl ether compounds as retinoic acid-related orphan Receptor-γt (RORγt) agonists.
Zheming Ruan, Peter K Park, Donna Wei, Ashok Purandare, Honghe Wan, John S Sack

Bioorg Med Chem Lett· March 2021

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Tricyclic-Carbocyclic RORγt Inverse Agonists-Discovery of BMS-986313.
Michael G Yang, Myra Beaudoin-Bertrand, Zili Xiao, David Marcoux, Carolyn A Weigelt, John S Sack

J Med Chem· March 2021

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Tricyclic sulfones as potent, selective and efficacious RORγt inverse agonists - Exploring C6 and C8 SAR using late-stage functionalization.
Qing Shi, Zili Xiao, Michael G Yang, David Marcoux, Robert J Cherney, John Sack

Bioorg Med Chem Lett· December 2020

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Novel Tricyclic Pyroglutamide Derivatives as Potent RORγt Inverse Agonists Identified using a Virtual Screening Approach.
Qingjie Liu, Douglas G Batt, Carolyn A Weigelt, Shiuhang Yip, Dauh-Rurng Wu, John S Sack

ACS Med Chem Lett· December 2020

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Discovery of a phenylpyrazole amide ROCK inhibitor as a tool molecule for in vivo studies.
Zilun Hu, Cailan Wang, Peter W Glunz, Julia Li, Nathan L Cheadle, John S Sack

Bioorg Med Chem Lett· November 2020

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Discovery of 2,6-difluorobenzyl ether series of phenyl ((R)-3-phenylpyrrolidin-3-yl)sulfones as surprisingly potent, selective and orally bioavailable RORγt inverse agonists.
James J-W Duan, Bin Jiang, Zhonghui Lu, Sylwia Stachura, Carolyn A Weigelt, John S Sack

Bioorg Med Chem Lett· October 2020

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Discovery of (3S,4S)-3-methyl-3-(4-fluorophenyl)-4-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxyprop-2-yl)phenyl)pyrrolidines as novel RORγt inverse agonists.
Bin Jiang, James J-W Duan, Sylwia Stachura, Ananta Karmakar, Hemalatha Hemagiri, John S Sack

Bioorg Med Chem Lett· September 2020

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Optimization of Nicotinamides as Potent and Selective IRAK4 Inhibitors with Efficacy in a Murine Model of Psoriasis.
Satheesh Nair, Sreekantha Ratna Kumar, Venkatram Reddy Paidi, Ramesh Sistla, Durgarao Kantheti, John Sack

ACS Med Chem Lett· July 2020

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Substituted benzyloxytricyclic compounds as retinoic acid-related orphan receptor gamma t (RORγt) agonists.
Lalgudi S Harikrishnan, Patrice Gill, Muthoni G Kamau, Lan-Ying Qin, Zheming Ruan, John S Sack

Bioorg Med Chem Lett· June 2020

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Discovery of BMS-986251: A Clinically Viable, Potent, and Selective RORγt Inverse Agonist.
Robert J Cherney, Lyndon A M Cornelius, Anurag Srivastava, Carolyn A Weigelt, David Marcoux, John Sack

ACS Med Chem Lett· June 2020

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Rationally Designed, Conformationally Constrained Inverse Agonists of RORγt-Identification of a Potent, Selective Series with Biologic-Like in Vivo Efficacy.
David Marcoux, James J-W Duan, Qing Shi, Robert J Cherney, Anurag S Srivastava, John S Sack

J Med Chem· November 2019

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Identification of potent, selective and orally bioavailable phenyl ((R)-3-phenylpyrrolidin-3-yl)sulfone analogues as RORγt inverse agonists.
Zhonghui Lu, James J-W Duan, Haiyun Xiao, James Neels, Dauh-Rurng Wu, John S Sack

Bioorg Med Chem Lett· August 2019

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Discovery of a JAK1/3 Inhibitor and Use of a Prodrug To Demonstrate Efficacy in a Model of Rheumatoid Arthritis.
Steven H Spergel, Michael E Mertzman, James Kempson, Junqing Guo, Sylwia Stachura, John S Sack

ACS Med Chem Lett· March 2019

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Structure-based Discovery of Phenyl (3-Phenylpyrrolidin-3-yl)sulfones as Selective, Orally Active RORγt Inverse Agonists.
James J-W Duan, Zhonghui Lu, Bin Jiang, Sylwia Stachura, Carolyn A Weigelt, John S Sack

ACS Med Chem Lett· March 2019

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How Herb Tabor's vision for timely and accessible research led scientific publishing into the online age.
John Sack

J Biol Chem· February 2019

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Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity.
Hua Gong, David S Weinstein, Zhonghui Lu, James J-W Duan, Sylwia Stachura, John S Sack

Bioorg Med Chem Lett· January 2018

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Discovery and structure-based design of 4,6-diaminonicotinamides as potent and selective IRAK4 inhibitors.
Rajeev S Bhide, Alec Keon, Carolyn Weigelt, John S Sack, Robert J Schmidt

Bioorg Med Chem Lett· November 2017

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Discovery of highly potent, selective, covalent inhibitors of JAK3.
James Kempson, Damaso Ovalle, Junqing Guo, Stephen T Wrobleski, Shuqun Lin, John S Sack

Bioorg Med Chem Lett· October 2017

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Discovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors.
John Hynes, Hong Wu, James Kempson, James J-W Duan, Zhonghui Lu, John S Sack

Bioorg Med Chem Lett· July 2017

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Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase δ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders.
Qingjie Liu, Qing Shi, David Marcoux, Douglas G Batt, Lyndon Cornelius, John S Sack

J Med Chem· June 2017

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Discovery of 7-(3-(piperazin-1-yl)phenyl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives as highly potent and selective PI3Kδ inhibitors.
Lan-Ying Qin, Zheming Ruan, Robert J Cherney, T G Murali Dhar, James Neels, John S Sack

Bioorg Med Chem Lett· February 2017

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