Site-Specific Labeling of Endogenous Proteins Using CoLDR Chemistry

Tunable Methacrylamides for Covalent Ligand Directed Release Chemistry

(2021) Rambabu N. Reddi et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

The rise of covalent proteolysis targeting chimeras

(2021) Ronen Gabizon et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Exploring Ligand-Directed N-Acyl-N-alkylsulfonamide-Based Acylation Chemistry for Potential Targeted Degrader Development

(2021) Mingxing Teng et al.   ACS Medicinal Chemistry Letters

Proteolysis-Targeting Chimeras as Therapeutics and Tools for Biological Discovery

(2020) George M. Burslem et al.   CELL

Efficient Targeted Degradation via Reversible and Irreversible Covalent PROTACs

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

Environmentally Sensitive Color‐Shifting Fluorophores for Bioimaging

(2020) lu wang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Phosphorylation-Inducing Chimeric Small Molecules

(2020) Sachini U. Siriwardena et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Selective Degradation of GSPT1 by Cereblon Modulators Identified via a Focused Combinatorial Library

(2020) Chelsea E. Powell et al.   ACS Chemical Biology

Enhancing intracellular accumulation and target engagement of PROTACs with reversible covalent chemistry

(2020) Wen-Hao Guo et al.   Nature Communications

First targeted protein degrader hits the clinic

(2019) Asher Mullard   NATURE REVIEWS DRUG DISCOVERY

PROTAC-Mediated Degradation of Bruton’s Tyrosine Kinase Is Inhibited by Covalent Binding

(2019) Christopher P. Tinworth et al.   ACS Chemical Biology

Targeted protein degradation: elements of PROTAC design

(2019) Stacey-Lynn Paiva et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Single-site glycine-specific labeling of proteins

(2019) Landa Purushottam et al.   Nature Communications

Design, synthesis and biological evaluation of Proteolysis Targeting Chimeras (PROTACs) as a BTK degraders with improved pharmacokinetic properties

(2019) Saul Jaime-Figueroa et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

A general strategy to develop cell permeable and fluorogenic probes for multicolour nanoscopy

(2019) Lu Wang et al.   Nature Chemistry

Translation Termination Factor GSPT1 Is a Phenotypically Relevant Off-Target of Heterobifunctional Phthalimide Degraders

(2018) Mette Ishoey et al.   ACS Chemical Biology

Ligand-Directed Chemistry of AMPA Receptors Confers Live-Cell Fluorescent Biosensors

(2018) Shigeki Kiyonaka et al.   ACS Chemical Biology

The Cysteinome of Protein Kinases as a Target in Drug Development

(2018) Apirat Chaikuad et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Targeting the C481S Ibrutinib-Resistance Mutation in Bruton’s Tyrosine Kinase Using PROTAC-Mediated Degradation

(2018) Alexandru D. Buhimschi et al.   BIOCHEMISTRY

Development of a Selective Labeling Probe for Bruton’s Tyrosine Kinase Quantification in Live Cells

(2018) Jiahui Chen et al.   BIOCONJUGATE CHEMISTRY

PROTAC-induced BTK degradation as a novel therapy for mutated BTK C481S induced ibrutinib-resistant B-cell malignancies

(2018) Yonghui Sun et al.   CELL RESEARCH

Chemo- and Regioselective Lysine Modification on Native Proteins

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

Delineating the role of cooperativity in the design of potent PROTACs for BTK

(2018) Adelajda Zorba et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

(2018) Tomonori Tamura et al.   Nature Communications

Bruton's Tyrosine Kinase degradation as a therapeutic strategy for cancer

(2018) Dennis Dobrovolsky et al.   BLOOD

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

Single-Site Labeling of Native Proteins Enabled by a Chemoselective and Site-Selective Chemical Technology

(2018) Srinivasa Rao Adusumalli et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Acalabrutinib (ACP-196): A Covalent Bruton Tyrosine Kinase Inhibitor with a Differentiated Selectivity and In Vivo Potency Profile

(2017) Tjeerd Barf et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Genetically encoded fluorescent tags

(2017) Kurt Thorn   MOLECULAR BIOLOGY OF THE CELL

A novel cereblon modulator recruits GSPT1 to the CRL4CRBN ubiquitin ligase

(2016) Mary E. Matyskiela et al.   NATURE

Site-specific fluorescent labeling to visualize membrane translocation of a myristoyl switch protein

(2016) Sung-Tae Yang et al.   Scientific Reports

Advances in Chemical Protein Modification

(2015) Omar Boutureira et al.   CHEMICAL REVIEWS

Emerging fluorescent protein technologies

(2015) Jhon Ralph Enterina et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

CETSA: a target engagement assay with potential to transform drug discovery

(2015) Annika Jenmalm Jensen et al.   Future Medicinal Chemistry

Imaging and manipulating proteins in live cells through covalent labeling

(2015) Lin Xue et al.   Nature Chemical Biology

One-step site-specific modification of native proteins with 2-pyridinecarboxyaldehydes

(2015) James I MacDonald et al.   Nature Chemical Biology

π-Clamp-mediated cysteine conjugation

(2015) Chi Zhang et al.   Nature Chemistry

Selective, rapid and optically switchable regulation of protein function in live mammalian cells

(2015) Yu-Hsuan Tsai et al.   Nature Chemistry

Protein recognition by bivalent, ‘turn-on’ fluorescent molecular probes

(2015) Linor Unger-Angel et al.   Chemical Science

Ligand-directed dibromophenyl benzoate chemistry for rapid and selective acylation of intracellular natural proteins

(2015) Yousuke Takaoka et al.   Chemical Science

A general approach for the development of fluorogenic probes suitable for no-wash imaging of kinases in live cells

(2014) Qing Zhang et al.   CHEMICAL COMMUNICATIONS

Cellular Incorporation of Unnatural Amino Acids and Bioorthogonal Labeling of Proteins

(2014) Kathrin Lang et al.   CHEMICAL REVIEWS

Site-specific PEGylation of Proteins: Recent Developments

(2014) Nicole Nischan et al.   JOURNAL OF ORGANIC CHEMISTRY

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

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

Selective chemical protein modification

(2014) Christopher D. Spicer et al.   Nature Communications

Developing Irreversible Inhibitors of the Protein Kinase Cysteinome

(2013) Qingsong Liu et al.   CHEMISTRY & BIOLOGY

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

Native FKBP12 Engineering by Ligand-Directed Tosyl Chemistry: Labeling Properties and Application to Photo-Cross-Linking of Protein Complexes in Vitro and in Living Cells

(2012) Tomonori Tamura et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Chemical tags: Applications in live cell fluorescence imaging

(2011) Richard Wombacher et al.   Journal of Biophotonics

Autophagy: assays and artifacts

(2010) Sandra Barth et al.   JOURNAL OF PATHOLOGY

Bioorthogonal Chemistry: Fishing for Selectivity in a Sea of Functionality

(2009) Ellen M. Sletten et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Ligand-directed tosyl chemistry for protein labeling in vivo

(2009) Shinya Tsukiji et al.   Nature Chemical Biology

Target identification using drug affinity responsive target stability (DARTS)

(2009) B. Lomenick et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Monitoring protein interactions and dynamics with solvatochromic fluorophores

(2009) Galen S. Loving et al.   TRENDS IN BIOTECHNOLOGY

HaloTag: A Novel Protein Labeling Technology for Cell Imaging and Protein Analysis

(2008) Georgyi V. Los et al.   ACS Chemical Biology