High-Throughput Kinetic Analysis for Target-Directed Covalent Ligand Discovery

Proteome-wide covalent ligand discovery in native biological systems

(2016) Keriann M. Backus et al.   NATURE

Irreversible inhibitors of the 3C protease of Coxsackie virus through templated assembly of protein-binding fragments

(2016) Daniel Becker et al.   Nature Communications

A Small Molecule That Switches a Ubiquitin Ligase From a Processive to a Distributive Enzymatic Mechanism

(2015) Stefan G. Kathman et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

The history and future of targeting cyclin-dependent kinases in cancer therapy

(2015) Uzma Asghar et al.   NATURE REVIEWS DRUG DISCOVERY

Hope and Disappointment: Covalent Inhibitors to Overcome Drug Resistance in Non-Small Cell Lung Cancer

(2015) Julian Engel et al.   ACS Medicinal Chemistry Letters

Rapid and Thiol-Specific High-Throughput Assay for Simultaneous Relative Quantification of Total Thiols, Protein Thiols, and Nonprotein Thiols in Cells

(2014) Yang Yang et al.   ANALYTICAL CHEMISTRY

Structure-based discovery of the first allosteric inhibitors of cyclin-dependent kinase 2

(2014) Giulio Rastelli et al.   CELL CYCLE

Cyclin-Dependent Kinase-2 as a Target for Cancer Therapy: Progress in the Development of CDK2 Inhibitors as Anti-Cancer Agents

(2014) Tahir Chohan et al.   CURRENT MEDICINAL CHEMISTRY

Chemical and Computational Methods for the Characterization of Covalent Reactive Groups for the Prospective Design of Irreversible Inhibitors

(2014) Mark E. Flanagan et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Fragment-Based Method to Discover Irreversible Covalent Inhibitors of Cysteine Proteases

(2014) Stefan G. Kathman et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design of Reversible, Cysteine-Targeted Michael Acceptors Guided by Kinetic and Computational Analysis

(2014) Shyam Krishnan et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Comparative studies of thiol-sensitive fluorogenic probes for HAT assays

(2012) Tielong Gao et al.   ANALYTICAL AND BIOANALYTICAL CHEMISTRY

Fragment-Based Approaches in Drug Discovery and Chemical Biology

(2012) Duncan E. Scott et al.   BIOCHEMISTRY

Structural Biology and Drug Discovery of Difficult Targets: The Limits of Ligandability

(2012) Sachin Surade et al.   CHEMISTRY & BIOLOGY

Kinetic Template-Guided Tethering of Fragments

(2012) Rebecca H. Nonoo et al.   ChemMedChem

αC helix displacement as a general approach for allosteric modulation of protein kinases

(2012) Lorenzo Palmieri et al.   DRUG DISCOVERY TODAY

Discovery of a Potential Allosteric Ligand Binding Site in CDK2

(2011) Stephane Betzi et al.   ACS Chemical Biology

Copper-catalyzed azide–alkyne cycloaddition (CuAAC) and beyond: new reactivity of copper(i) acetylides

(2010) Jason E. Hein et al.   CHEMICAL SOCIETY REVIEWS

Fluorescent and colorimetric probes for detection of thiols

(2010) Xiaoqiang Chen et al.   CHEMICAL SOCIETY REVIEWS

A miniaturized technique for assessing protein thermodynamics and function using fast determination of quantitative cysteine reactivity

(2010) Daniel G. Isom et al.   PROTEINS-STRUCTURE FUNCTION AND BIOINFORMATICS

Selective Identification of Cooperatively Binding Fragments in a High-Throughput Ligation Assay Enables Development of a Picomolar Caspase-3 Inhibitor

(2009) Marco F. Schmidt et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Sensitized Detection of Inhibitory Fragments and Iterative Development of Non-Peptidic Protease Inhibitors by Dynamic Ligation Screening

(2008) Marco Florian Schmidt et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION