Profiling Sulfur(VI) Fluorides as Reactive Functionalities for Chemical Biology Tools and Expansion of the Ligandable Proteome

RBMX suppresses tumorigenicity and progression of bladder cancer by interacting with the hnRNP A1 protein to regulate PKM alternative splicing

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One‐Step Synthesis of Photoaffinity Probes for Live‐Cell MS‐Based Proteomics

(2021) David J. Fallon et al.   CHEMISTRY-A EUROPEAN JOURNAL

Density functional theory studies of the antioxidants—a review

(2021) Samira Mahmoudi et al.   JOURNAL OF MOLECULAR MODELING

A sulfonyl fluoride derivative inhibits EGFRL858R/T790M/C797S by covalent modification of the catalytic lysine

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Discovery of Lysine-Targeted eIF4E Inhibitors through Covalent Docking

(2020) Xiaobo Wan et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Ligand Conformational Bias Drives Enantioselective Modification of a Surface-Exposed Lysine on Hsp90

(2020) Adolfo Cuesta et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Liganding Functional Tyrosine Sites on Proteins Using Sulfur–Triazole Exchange Chemistry

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Rationally Designed Covalent BCL6 Inhibitor That Targets a Tyrosine Residue in the Homodimer Interface

(2020) Mingxing Teng et al.   ACS Medicinal Chemistry Letters

PhotoAffinity Bits: A photoaffinity‐based fragment screening platform for efficient identification of protein ligands

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An Activity-Guided Map of Electrophile-Cysteine Interactions in Primary Human T Cells

(2020) Ekaterina V. Vinogradova et al.   CELL

Sulfonamide Inhibitors of Human Carbonic Anhydrases Designed through a Three-Tails Approach: Improving Ligand/Isoform Matching and Selectivity of Action

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Using sulfuramidimidoyl fluorides that undergo sulfur(vi) fluoride exchange for inverse drug discovery

(2020) Gabriel J. Brighty et al.   Nature Chemistry

Kinase inhibition in autoimmunity and inflammation

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Fragment-based screening sees the light

(2020) Asher Mullard   NATURE REVIEWS DRUG DISCOVERY

Fragment-based covalent ligand screening enables rapid discovery of inhibitors for the RBR E3 ubiquitin ligase HOIP

(2019) Henrik Johansson et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Rapid covalent-probe discovery by electrophile-fragment screening

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The Proteome-Wide Potential for Reversible Covalency at Cysteine

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SuFEx-enabled, agnostic discovery of covalent inhibitors of human neutrophil elastase

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Discovery of N-(1-Acryloylazetidin-3-yl)-2-(1H-indol-1-yl)acetamides as Covalent Inhibitors of KRASG12C

(2019) Youngsook Shin et al.   ACS Medicinal Chemistry Letters

A Photoaffinity Displacement Assay and Probes to Study the Cyclin-Dependent Kinase Family

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Isotopically Labeled Desthiobiotin Azide (isoDTB) Tags Enable Global Profiling of the Bacterial Cysteinome

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Global targeting of functional tyrosines using sulfur-triazole exchange chemistry

(2019) Heung Sik Hahm et al.   Nature Chemical Biology

Kinetic Optimization of Lysine-Targeting Covalent Inhibitors of HSP72

(2019) Jonathan Pettinger et al.   JOURNAL OF MEDICINAL CHEMISTRY

Chemoproteomics-Enabled Covalent Ligand Screening Reveals ALDH3A1 as a Lung Cancer Therapy Target

(2018) Jessica L. Counihan et al.   ACS Chemical Biology

Arylfluorosulfate-Based Warheads for Covalent Protein Labeling: A New Addition to the Arsenal

(2018) Pablo Martin-Gago et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Selectively Targeting the Kinome-Conserved Lysine of PI3Kδ as a General Approach to Covalent Kinase Inhibition

(2018) Samuel E. Dalton et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Genetically Encoding Fluorosulfate-l-tyrosine To React with Lysine, Histidine, and Tyrosine via SuFEx in Proteins in Vivo

(2018) Nanxi Wang et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Unexplored therapeutic opportunities in the human genome

(2018) Tudor I. Oprea et al.   NATURE REVIEWS DRUG DISCOVERY

Proximity-enhanced SuFEx chemical cross-linker for specific and multitargeting cross-linking mass spectrometry

(2018) Bing Yang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Broad-Spectrum Kinase Profiling in Live Cells with Lysine-Targeted Sulfonyl Fluoride Probes

(2017) Qian Zhao et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

“Inverse Drug Discovery” Strategy To Identify Proteins That Are Targeted by Latent Electrophiles As Exemplified by Aryl Fluorosulfates

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Global profiling of lysine reactivity and ligandability in the human proteome

(2017) Stephan M. Hacker et al.   Nature Chemistry

A study of the reactivity of S(VI)–F containing warheads with nucleophilic amino-acid side chains under physiological conditions

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Proteome-wide covalent ligand discovery in native biological systems

(2016) Keriann M. Backus et al.   NATURE

Rational Targeting of Active-Site Tyrosine Residues Using Sulfonyl Fluoride Probes

(2015) Erik C. Hett et al.   ACS Chemical Biology

The ERCC1 and ERCC4 (XPF) genes and gene products

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Sulfonyl fluorides as privileged warheads in chemical biology

(2015) Arjun Narayanan et al.   Chemical Science

Sulfur(VI) Fluoride Exchange (SuFEx): Another Good Reaction for Click Chemistry

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Targeting the LKB1 Tumor Suppressor

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Targeting transcription regulation in cancer with a covalent CDK7 inhibitor

(2014) Nicholas Kwiatkowski et al.   NATURE

Covalent docking of large libraries for the discovery of chemical probes

(2014) Nir London et al.   Nature Chemical Biology

Developing Irreversible Inhibitors of the Protein Kinase Cysteinome

(2013) Qingsong Liu et al.   CHEMISTRY & BIOLOGY

Aromatic Sulfonyl Fluorides Covalently Kinetically Stabilize Transthyretin to Prevent Amyloidogenesis while Affording a Fluorescent Conjugate

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Target validation using chemical probes

(2013) Mark E Bunnage et al.   Nature Chemical Biology

The Ugi four-component reaction enables expedient synthesis and comparison of photoaffinity probes

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Amino acids: Chemistry, functionality and selected non-enzymatic post-translational modifications

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FT-IR, FT-Raman, ab initio, HF and DFT studies, NBO, HOMO–LUMO and electronic structure calculations on 4-chloro-3-nitrotoluene

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Quantitative reactivity profiling predicts functional cysteines in proteomes

(2010) Eranthie Weerapana et al.   NATURE