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“Sleeping Beauty” Phenomenon: SuFEx-Enabled Discovery of Selective Covalent Inhibitors of Human Neutrophil Elastase

Qinheng Zheng, Jordan L. Woehl, Seiya Kitamura, Diogo Santos-Martins, Christopher J. Smedley, Gencheng Li, Stefano Forli, John E. Moses, Dennis W. Wolan, K. Barry Sharpless

Version 1 posted 15 March 2019

1,592

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2

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Biological and Medicinal Chemistry

Working Paper

Discovery of a Potent and Selective Covalent Inhibitor and Activity-Based Probe for the Deubiquitylating Enzyme UCHL1, with Anti-Fibrotic Activity

Nattawadee Panyain, Aurélien Godinat, Thomas Lanyon-Hogg, Sofía Lachiondo-Ortega, Edward J. Will, Christelle Soudy, Katie Mason, Sarah Elkhalifa, Lisa M. Smith, Jeanine A. Harrigan, Edward Tate

Version 1 posted 31 October 2019

1,103

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2

Citations

Biological and Medicinal Chemistry

Working Paper

Targeted Covalent Inhibition of Telomerase

Rick Betori, Yue Liu, Ding Wu, Rama Mishra, Scott Cohen, Stephen J. Kron, Karl Scheidt

Version 1 posted 23 July 2019

898

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Biological and Medicinal Chemistry

Working Paper

Diacylfuroxans Are Masked Nitrile Oxides That Inhibit GPX4 Covalently

John Eaton, Richard A. Ruberto, Anneke Kramm, Vasanthi S. Viswanathan, Stuart Schreiber

Version 1 posted 23 January 2019

828

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Organic Chemistry

Working Paper

Diversity Oriented Clicking: Synthesis of beta-Substituted Alkenyl Sulfonyl Fluorides as Covalent Human Neutrophil Elastase Inhibitors

Yunfei Cheng, Gencheng Li, Christopher J. Smedley, Marie-Claire Giel, Seiya Kitamura, Jordan L. Woehl, Giulia Bianco, Stefano Forli, Joshua A. Homer, John R. Cappiello, Dennis W. Wolan, John E. Moses, K. Barry Sharpless

Version 1 posted 25 April 2022

605

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Biological and Medicinal Chemistry

Working Paper

Fluoromethylketone-fragment conjugates designed as covalent modifiers of EcDsbA are atypical substrates

Bradley Doak, Rebecca Whitehouse, Kieran Rimmer, Martin Williams, Begona Heras, Sofia Caria, Olga Ilyichova, Mansha Vazirani, Biswaranjan Mohanty, Jason Harper, Martin Scanlon, Jamie Simpson

Version 1 posted 17 February 2022

285

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1

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Biological and Medicinal Chemistry

Working Paper

α-Methylene-β-Lactone Probe for Measuring Live-Cell Reactions of Small Molecules

Lei Wang, Louis Riel, Bekim Bajrami, Bin Deng, Amy Howell, Xudong Yao

Version 2 posted 13 April 2020

797

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Biological and Medicinal Chemistry

Working Paper

Pitfalls and considerations in determining the potency and mutant selectivity of covalent epidermal growth factor receptor inhibitors

Kristopher W Hoyt, Daniel A Urul, Blessing C Ogboo, Florian Wittlinger, Stefan A Laufer, Erik M Schaefer, Earl W May, David E Heppner

Version 1 posted 24 August 2023

273

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Biological and Medicinal Chemistry

Working Paper

Structure-based design of a phosphotyrosine-masked covalent ligand targeting the E3 ligase SOCS2

Sarath Ramachandran, Nikolai Makukhin, Kevin Haubrich, Manjula Nagala, Beth Forrester, Dylan Lynch, Ryan Casement, Andrea Testa, Elvira Bruno, Rosaria Gitto, Alessio Ciulli

Version 2 posted 16 August 2023

2,405

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Biological and Medicinal Chemistry

Working Paper

Covalent Bonding Aptamer with Enhanced SARS-CoV-2 RBD-ACE2 Blocking and Pseudovirus Neutralization Activities

Zichen Qin, Yiying Zhu, Yu Xiang

Version 2 posted 28 December 2021

1,708

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1

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Refine Search

12 results in Covalent Inhibitor in Keywords: Covalent Inhibitor

“Sleeping Beauty” Phenomenon: SuFEx-Enabled Discovery of Selective Covalent Inhibitors of Human Neutrophil Elastase

Discovery of a Potent and Selective Covalent Inhibitor and Activity-Based Probe for the Deubiquitylating Enzyme UCHL1, with Anti-Fibrotic Activity

Targeted Covalent Inhibition of Telomerase

Diacylfuroxans Are Masked Nitrile Oxides That Inhibit GPX4 Covalently

Diversity Oriented Clicking: Synthesis of beta-Substituted Alkenyl Sulfonyl Fluorides as Covalent Human Neutrophil Elastase Inhibitors

Fluoromethylketone-fragment conjugates designed as covalent modifiers of EcDsbA are atypical substrates

α-Methylene-β-Lactone Probe for Measuring Live-Cell Reactions of Small Molecules

Pitfalls and considerations in determining the potency and mutant selectivity of covalent epidermal growth factor receptor inhibitors

Structure-based design of a phosphotyrosine-masked covalent ligand targeting the E3 ligase SOCS2

Covalent Bonding Aptamer with Enhanced SARS-CoV-2 RBD-ACE2 Blocking and Pseudovirus Neutralization Activities

12 results in Keywords: Covalent Inhibitor