In situ identification of cellular drug targets in mammalian tissue

Basic principles of hydrogel-based tissue transformation technologies and their applications

(2021) Seo Woo Choi et al.   CELL

Btk Inhibitors: A Medicinal Chemistry and Drug Delivery Perspective

(2021) Chiara Brullo et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Discovery of Cysteine-targeting Covalent Protein Kinase Inhibitors

(2021) Xiaoyun Lu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Click Chemistry in Proteomic Investigations

(2020) Christopher G. Parker et al.   CELL

Tissue clearing and its applications in neuroscience

(2020) Hiroki R. Ueda et al.   NATURE REVIEWS NEUROSCIENCE

Bioorthogonal reactions in animals

(2020) Karine Porte et al.   CHEMBIOCHEM

KRASG12C Inhibition with Sotorasib in Advanced Solid Tumors

(2020) David S. Hong et al.   NEW ENGLAND JOURNAL OF MEDICINE

10 years into the resurgence of covalent drugs

(2020) Elena De Vita   Future Medicinal Chemistry

FDISCO: Advanced solvent-based clearing method for imaging whole organs

(2019) Yisong Qi et al.   Science Advances

Covalent Inhibition in Drug Discovery

(2019) Avick Kumar Ghosh et al.   ChemMedChem

Global Portrait of Protein Targets of Metabolites of the Neurotoxic Compound BIA 10–2474

(2019) Zhen Huang et al.   ACS Chemical Biology

ABHD6: Its Place in Endocannabinoid Signaling and Beyond

(2019) Jessica K. Cao et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

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

(2019) Qinheng Zheng et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity

(2019) Jude Canon et al.   NATURE

Hippocampal vascular reserve associated with cognitive performance and hippocampal volume

(2019) Valentina Perosa et al.   BRAIN

Third-generationin situhybridization chain reaction: multiplexed, quantitative, sensitive, versatile, robust

(2018) Harry M. T. Choi et al.   DEVELOPMENT

Three-dimensional intact-tissue sequencing of single-cell transcriptional states

(2018) Xiao Wang et al.   SCIENCE

Discovery of a Potent, Long-Acting, and CNS-Active Inhibitor (BIA 10-2474) of Fatty Acid Amide Hydrolase

(2018) László E. Kiss et al.   ChemMedChem

New approaches and challenges to targeting the endocannabinoid system

(2018) Vincenzo Di Marzo   NATURE REVIEWS DRUG DISCOVERY

Chemical Landscape for Tissue Clearing Based on Hydrophilic Reagents

(2018) Kazuki Tainaka et al.   Cell Reports

Visualizing biologically active small molecules in cells using click chemistry

(2018) Tatiana Cañeque et al.   Nature Reviews Chemistry

Protection of tissue physicochemical properties using polyfunctional crosslinkers

(2018) Young-Gyun Park et al.   NATURE BIOTECHNOLOGY

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

Activity-based protein profiling reveals off-target proteins of the FAAH inhibitor BIA 10-2474

(2017) Annelot C. M. van Esbroeck et al.   SCIENCE

Target identification of covalently binding drugs by activity-based protein profiling (ABPP)

(2016) Christian M. Pichler et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Multiplexed Intact-Tissue Transcriptional Analysis at Cellular Resolution

(2016) Emily Lauren Sylwestrak et al.   CELL

Development and Applications of the Copper-Catalyzed Azide-Alkyne Cycloaddition (CuAAC) as a Bioorthogonal Reaction

(2016) Li Li et al.   MOLECULES

Shrinkage-mediated imaging of entire organs and organisms using uDISCO

(2016) Chenchen Pan et al.   NATURE METHODS

Small molecules, big targets: drug discovery faces the protein–protein interaction challenge

(2016) Duncan E. Scott et al.   NATURE REVIEWS DRUG DISCOVERY

Acute Neurologic Disorder from an Inhibitor of Fatty Acid Amide Hydrolase

(2016) Anne Kerbrat et al.   NEW ENGLAND JOURNAL OF MEDICINE

A Small-Molecule Probe for Selective Profiling and Imaging of Monoamine Oxidase B Activities in Models of Parkinson’s Disease

(2015) Lin Li et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Connectivity of mouse somatosensory and prefrontal cortex examined with trans-synaptic tracing

(2015) Laura A DeNardo et al.   NATURE NEUROSCIENCE

Enzyme Inhibitor Discovery by Activity-Based Protein Profiling

(2014) Micah J. Niphakis et al.   Annual Review of Biochemistry

iDISCO: A Simple, Rapid Method to Immunolabel Large Tissue Samples for Volume Imaging

(2014) Nicolas Renier et al.   CELL

Proteome-Wide Reactivity Profiling Identifies Diverse Carbamate Chemotypes Tuned for Serine Hydrolase Inhibition

(2013) Jae Won Chang et al.   ACS Chemical Biology

Evaluation of NHS Carbamates as a Potent and Selective Class of Endocannabinoid Hydrolase Inhibitors

(2013) Micah J. Niphakis et al.   ACS Chemical Neuroscience

Structural and molecular interrogation of intact biological systems

(2013) Kwanghun Chung et al.   NATURE

Targeting BTK with Ibrutinib in Relapsed Chronic Lymphocytic Leukemia

(2013) John C. Byrd et al.   NEW ENGLAND JOURNAL OF MEDICINE

Activity-Based Probes for Studying the Activity of Flavin-Dependent Oxidases and for the Protein Target Profiling of Monoamine Oxidase Inhibitors

(2012) Joanna M. Krysiak et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

A review of imaging methods for measuring drug release at nanometre scale: a case for drug delivery systems

(2012) Ketan Pancholi   Expert Opinion on Drug Delivery

Afatinib versus placebo for patients with advanced, metastatic non-small-cell lung cancer after failure of erlotinib, gefitinib, or both, and one or two lines of chemotherapy (LUX-Lung 1): a phase 2b/3 randomised trial

(2012) Vincent A Miller et al.   LANCET ONCOLOGY

Three-dimensional imaging of solvent-cleared organs using 3DISCO

(2012) Ali Ertürk et al.   Nature Protocols

O-Hydroxyacetamide Carbamates as a Highly Potent and Selective Class of Endocannabinoid Hydrolase Inhibitors

(2011) Micah J. Niphakis et al.   ACS Chemical Neuroscience

Increasing the Efficacy of Bioorthogonal Click Reactions for Bioconjugation: A Comparative Study

(2011) Christen Besanceney-Webler et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Sulfated Ligands for the Copper(I)-Catalyzed Azide-Alkyne Cycloaddition

(2011) Wei Wang et al.   Chemistry-An Asian Journal

The resurgence of covalent drugs

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

Chronic monoacylglycerol lipase blockade causes functional antagonism of the endocannabinoid system

(2010) Joel E Schlosburg et al.   NATURE NEUROSCIENCE

Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor

(2010) Douglas S. Johnson et al.   ACS Medicinal Chemistry Letters