Sulfonyl fluorides as privileged warheads in chemical biology

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

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

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

(2014) Jiajia Dong et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Selective Inhibition of the Immunoproteasome by Ligand-Induced Crosslinking of the Active Site

(2014) Christian Dubiella et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Site-Selective Protein Immobilization by Covalent Modification of GST Fusion Proteins

(2014) Yiqing Zhou et al.   BIOCONJUGATE CHEMISTRY

A chemical “hub” for absolute quantification of a targeted protein: orthogonal integration of elemental and molecular mass spectrometry

(2014) Xiaowen Yan et al.   CHEMICAL COMMUNICATIONS

Understanding and applying tyrosine biochemical diversity

(2014) Lyn H. Jones et al.   Molecular BioSystems

Broad-Spectrum Antimalarial Activity of Peptido Sulfonyl Fluorides, a New Class of Proteasome Inhibitors

(2013) Serena Tschan et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Fluorogenic small molecules requiring reaction with a specific protein to create a fluorescent conjugate for biological imaging-what we know and what we need to learn

(2013) Aleksandra Baranczak et al.   BIOPOLYMERS

Chemical Proteomics with Sulfonyl Fluoride Probes Reveals Selective Labeling of Functional Tyrosines in Glutathione Transferases

(2013) Christian Gu et al.   CHEMISTRY & 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

(2013) Neil P. Grimster et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Synthesis and Evaluation of Activity-Based Probes Carrying a 5′-Fluorosulfonylbenzoyl Adenosine Moiety for Protein Kinases

(2013) Yu-Ling Hsu et al.   JOURNAL OF THE CHINESE CHEMICAL SOCIETY

Target validation using chemical probes

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

MEROPS: the database of proteolytic enzymes, their substrates and inhibitors

(2013) Neil D. Rawlings et al.   NUCLEIC ACIDS RESEARCH

Structural basis for the specific recognition of dual receptors by the homopolymeric pH 6 antigen (Psa) fimbriae of Yersinia pestis

(2013) R. Bao et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Activity-based probes for rhomboid proteases discovered in a mass spectrometry-based assay

(2013) O. Vosyka et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Target validation using in-cell small molecule clickable imaging probes

(2013) Brahma Ghosh et al.   MedChemComm

Affinity-based target identification for bioactive small molecules

(2013) Makoto Kawatani et al.   MedChemComm

Europium-Labeled Activity-Based Probe through Click Chemistry: Absolute Serine Protease Quantification Using 153Eu Isotope Dilution ICP/MS

(2012) Xiaowen Yan et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Affinity Labeling of Hepatitis C Virus Replicase with a Nucleotide Analogue: Identification of Binding Site

(2012) Dinesh Manvar et al.   BIOCHEMISTRY

How Chemoproteomics Can Enable Drug Discovery and Development

(2012) Raymond E. Moellering et al.   CHEMISTRY & BIOLOGY

Peptido Sulfonyl Fluorides as New Powerful Proteasome Inhibitors

(2012) Arwin J. Brouwer et al.   JOURNAL OF MEDICINAL CHEMISTRY

Sulfonyl Fluoride Inhibitors of Fatty Acid Amide Hydrolase

(2012) Shakiru O. Alapafuja et al.   JOURNAL OF MEDICINAL CHEMISTRY

Selective Targeting of Distinct Active Site Nucleophiles by Irreversible Src-Family Kinase Inhibitors

(2012) Nathan N. Gushwa et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Convergent translational evidence of a role for anandamide in amygdala-mediated fear extinction, threat processing and stress-reactivity

(2012) O Gunduz-Cinar et al.   MOLECULAR PSYCHIATRY

Selective Pressure Causes an RNA Virus to Trade Reproductive Fitness for Increased Structural and Thermal Stability of a Viral Enzyme

(2012) Moshe Dessau et al.   PLoS Genetics

An activity-based probe for high-throughput measurements of triacylglycerol lipases

(2011) John Tam et al.   ANALYTICAL BIOCHEMISTRY

Inhibition of Multidrug Resistance-Linked P-Glycoprotein (ABCB1) Function by 5′-Fluorosulfonylbenzoyl 5′-Adenosine: Evidence for an ATP Analogue That Interacts with Both Drug-Substrate-and Nucleotide-Binding Sites

(2011) Shinobu Ohnuma et al.   BIOCHEMISTRY

Synthesis and biological evaluation of novel irreversible serine protease inhibitors using amino acid based sulfonyl fluorides as an electrophilic trap

(2011) Arwin J. Brouwer et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Inhibiting fatty acid amide hydrolase normalizes endotoxin-induced enhanced gastrointestinal motility in mice

(2011) M Bashashati et al.   BRITISH JOURNAL OF PHARMACOLOGY

Polyisoprenylation Potentiates the Inhibition of Polyisoprenylated Methylated Protein Methyl Esterase and the Cell Degenerative Effects of Sulfonyl Fluorides

(2011) B. Aguilar et al.   CURRENT CANCER DRUG TARGETS

The resurgence of covalent drugs

(2011) Juswinder Singh et al.   NATURE REVIEWS DRUG DISCOVERY

Inhibitor of Fatty Acid Amide Hydrolase Normalizes Cardiovascular Function in Hypertension without Adverse Metabolic Effects

(2010) Grzegorz Godlewski et al.   CHEMISTRY & BIOLOGY

Chemical mutagenesis: selective post-expression interconversion of protein amino acid residues

(2010) Justin M Chalker et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Tyrosine 8 contributes to catalysis but is not required for activity of rat liver glutathione S-transferase, 1-1

(2010) Jibo Wang et al.   PROTEIN SCIENCE

Active-Site Motions and Polarity Enhance Catalytic Turnover of Hydrated Subtilisin Dissolved in Organic Solvents

(2009) Elton P. Hudson et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Structural and Kinetic Analyses of Macrophage Migration Inhibitory Factor Active Site Interactions†‡

(2008) Gregg V. Crichlow et al.   BIOCHEMISTRY