Tunable Methacrylamides for Covalent Ligand Directed Release Chemistry

Newly Developed Prodrugs and Prodrugs in Development; an Insight of the Recent Years

(2020) Anas Najjar et al.   MOLECULES

Efficient Targeted Degradation via Reversible and Irreversible Covalent PROTACs

(2020) Ronen Gabizon et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Alkynyl Benzoxazines and Dihydroquinazolines as Cysteine Targeting Covalent Warheads and Their Application in Identification of Selective Irreversible Kinase Inhibitors

(2020) Kirsten McAulay et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

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

(2020) Ekaterina V. Vinogradova et al.   CELL

Systematic Study of the Glutathione Reactivity of N-Phenylacrylamides: 2. Effects of Acrylamide Substitution

(2020) Adam Birkholz et al.   JOURNAL OF MEDICINAL CHEMISTRY

Bicyclobutane Carboxylic Amide as a Cysteine-Directed Strained Electrophile for Selective Targeting of Proteins

(2020) Keisuke Tokunaga et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

The Alkyne Moiety as a Latent Electrophile in Irreversible Covalent Small Molecule Inhibitors of Cathepsin K

(2019) Elma Mons et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Characterising covalent warhead reactivity

(2019) James S. Martin et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Recent Advances and Challenges in Luminescent Imaging: Bright Outlook for Chemiluminescence of Dioxetanes in Water

(2019) Nir Hananya et al.   ACS Central Science

Activity-Based Optical Sensing Enabled by Self-Immolative Scaffolds: Monitoring of Release Events by Fluorescence or Chemiluminescence Output

(2019) Samer Gnaim et al.   ACCOUNTS OF CHEMICAL RESEARCH

An Activatable Chemiluminescent Probe for Sensitive Detection of γ-Glutamyl Transpeptidase Activity in Vivo

(2019) Ruibing An et al.   ANALYTICAL CHEMISTRY

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

(2019) Patrick R. A. Zanon et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Covalent-Allosteric Inhibitors to Achieve Akt Isoform-Selectivity

(2019) Lena Quambusch et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Enzyme-Activated Fluorogenic Probes for Live-Cell and in Vivo Imaging

(2018) Wen Chyan et al.   ACS Chemical Biology

Quinone-based fluorophores for imaging biological processes

(2018) Gleiston G. Dias et al.   CHEMICAL SOCIETY REVIEWS

Progress with covalent small-molecule kinase inhibitors

(2018) Zheng Zhao et al.   DRUG DISCOVERY TODAY

Novel K-Ras G12C Switch-II Covalent Binders Destabilize Ras and Accelerate Nucleotide Exchange

(2018) Chimno I. Nnadi et al.   Journal of Chemical Information and Modeling

Chemo- and Regioselective Lysine Modification on Native Proteins

(2018) Maria J. Matos et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

The expanding role of prodrugs in contemporary drug design and development

(2018) Jarkko Rautio et al.   NATURE REVIEWS DRUG DISCOVERY

BODIPY-based turn-on fluorescent probes for cysteine and homocysteine

(2018) Jinhua Gao et al.   SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY

Allenamide as a bioisostere of acrylamide in the design and synthesis of targeted covalent inhibitors

(2018) Deheng Chen et al.   MedChemComm

Rapid labelling and covalent inhibition of intracellular native proteins using ligand-directed N-acyl-N-alkyl sulfonamide

(2018) Tomonori Tamura et al.   Nature Communications

Chemiluminescent Probe for the In Vitro and In Vivo Imaging of Cancers Over-Expressing NQO1

(2018) Subin Son et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Molecular Imaging: In Vivo Agents for the Diagnosis and Treatment of Cancer

(2018) D. Haeusler et al.   Contrast Media & Molecular Imaging

Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology

(2018) Matthias Gehringer et al.   JOURNAL OF MEDICINAL CHEMISTRY

Chemistry for Covalent Modification of Endogenous/Native Proteins: From Test Tubes to Complex Biological Systems

(2018) Tomonori Tamura et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

A Turn-On Fluorescent Probe for Sensitive Detection of Cysteine in a Fully Aqueous Environment and in Living Cells

(2018) Xiaohua Ma et al.   Journal of Analytical Methods in Chemistry

Prodrug strategy for cancer cell-specific targeting: A recent overview

(2017) Xian Zhang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Affinity-Guided Oxime Chemistry for Selective Protein Acylation in Live Tissue Systems

(2017) Tomonori Tamura et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Targeted Covalent Inhibitors for Drug Design

(2016) Thomas A. Baillie   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Acalabrutinib (ACP-196): a selective second-generation BTK inhibitor

(2016) Jingjing Wu et al.   Journal of Hematology & Oncology

Covalent Modifiers: A Chemical Perspective on the Reactivity of α,β-Unsaturated Carbonyls with Thiols via Hetero-Michael Addition Reactions

(2016) Paul A. Jackson et al.   JOURNAL OF MEDICINAL CHEMISTRY

Metabolically Labile Fumarate Esters Impart Kinetic Selectivity to Irreversible Inhibitors

(2016) Balyn W. Zaro et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Remarkable Enhancement of Chemiluminescent Signal by Dioxetane–Fluorophore Conjugates: Turn-ON Chemiluminescence Probes with Color Modulation for Sensing and Imaging

(2016) Nir Hananya et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Proteome-wide covalent ligand discovery in native biological systems

(2016) Keriann M. Backus et al.   NATURE

Rapid Determination of the Specificity Constant of Irreversible Inhibitors (kinact/KI) by Means of an Endpoint Competition Assay

(2015) Ikuo Miyahisa et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Covalent-Allosteric Kinase Inhibitors

(2015) Jörn Weisner et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Covalent protein modification: the current landscape of residue-specific electrophiles

(2015) D Alexander Shannon et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Prolonged and tunable residence time using reversible covalent kinase inhibitors

(2015) J Michael Bradshaw et al.   Nature Chemical Biology

Prodrug Applications for Targeted Cancer Therapy

(2014) Irene Giang et al.   AAPS Journal

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

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

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

A road map to evaluate the proteome-wide selectivity of covalent kinase inhibitors

(2014) Bryan R Lanning et al.   Nature Chemical Biology

Developing Irreversible Inhibitors of the Protein Kinase Cysteinome

(2013) Qingsong Liu et al.   CHEMISTRY & BIOLOGY

Turn-ON fluorescent affinity labeling using a small bifunctional O-nitrobenzoxadiazole unit

(2013) Takao Yamaguchi et al.   Chemical Science

Ligand-Directed Acyl Imidazole Chemistry for Labeling of Membrane-Bound Proteins on Live Cells

(2012) Sho-hei Fujishima et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Reversible targeting of noncatalytic cysteines with chemically tuned electrophiles

(2012) Iana M Serafimova et al.   Nature Chemical Biology

Estimation of pKa values for carboxylic acids, alcohols, phenols and amines using changes in the relative Gibbs free energy

(2011) Yue Zeng et al.   FLUID PHASE EQUILIBRIA

Multicolor, One- and Two-Photon Imaging of Enzymatic Activities in Live Cells with Fluorescently Quenched Activity-Based Probes (qABPs)

(2011) Mingyu Hu et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

The resurgence of covalent drugs

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

Quantitative reactivity profiling predicts functional cysteines in proteomes

(2010) Eranthie Weerapana et al.   NATURE

The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy

(2010) L. A. Honigberg et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

New Strategies for Fluorescent Probe Design in Medical Diagnostic Imaging

(2009) Hisataka Kobayashi et al.   CHEMICAL REVIEWS

Real-Time Observation of Carbonic Acid Formation in Aqueous Solution

(2009) K. Adamczyk et al.   SCIENCE