Quantitating drug-target engagement in single cells in vitro and in vivo

Mass Cytometry: Single Cells, Many Features

(2016) Matthew H. Spitzer et al.   CELL

Fluorescent vinblastine probes for live cell imaging

(2016) Labros G. Meimetis et al.   CHEMICAL COMMUNICATIONS

Optimized Near-IR Fluorescent Agents for in Vivo Imaging of Btk Expression

(2015) Eunha Kim et al.   BIOCONJUGATE CHEMISTRY

Fractional killing arises from cell-to-cell variability in overcoming a caspase activity threshold

(2015) J. Roux et al.   Molecular Systems Biology

Selective resistance to the PARP inhibitor olaparib in a mouse model for BRCA1-deficient metaplastic breast cancer

(2015) Linda Henneman et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Highly multiplexed imaging of single cells using a high-throughput cyclic immunofluorescence method

(2015) Jia-Ren Lin et al.   Nature Communications

Tumour-associated macrophages act as a slow-release reservoir of nano-therapeutic Pt(IV) pro-drug

(2015) Miles A. Miller et al.   Nature Communications

Label-Free in Situ Monitoring of Histone Deacetylase Drug Target Engagement by Matrix-Assisted Laser Desorption Ionization-Mass Spectrometry Biotyping and Imaging

(2014) Bogdan Munteanu et al.   ANALYTICAL CHEMISTRY

Single-cell pharmacokinetic imaging reveals a therapeutic strategy to overcome drug resistance to the microtubule inhibitor eribulin

(2014) A. M. Laughney et al.   Science Translational Medicine

In vivo imaging of specific drug–target binding at subcellular resolution

(2014) J. M. Dubach et al.   Nature Communications

Single cell imaging of Bruton's Tyrosine Kinase using an irreversible inhibitor

(2014) Anna Turetsky et al.   Scientific Reports

BMN 673, a Novel and Highly Potent PARP1/2 Inhibitor for the Treatment of Human Cancers with DNA Repair Deficiency

(2013) Y. Shen et al.   CLINICAL CANCER RESEARCH

Determining target engagement in living systems

(2013) Gabriel M Simon et al.   Nature Chemical Biology

Target validation using chemical probes

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

Immunofluorescence and fluorescent-protein tagging show high correlation for protein localization in mammalian cells

(2013) Charlotte Stadler et al.   NATURE METHODS

Quantitative assessment of single-cell RNA-sequencing methods

(2013) Angela R Wu et al.   NATURE METHODS

Appraising iniparib, the PARP inhibitor that never was—what must we learn?

(2013) Joaquin Mateo et al.   Nature Reviews Clinical Oncology

Translational PET imaging research

(2013) Richard J. Hargreaves et al.   NEUROBIOLOGY OF DISEASE

Monitoring Drug Target Engagement in Cells and Tissues Using the Cellular Thermal Shift Assay

(2013) D. M. Molina et al.   SCIENCE

Single-cell and subcellular pharmacokinetic imaging allows insight into drug action in vivo

(2013) Greg M. Thurber et al.   Nature Communications

Family-wide chemical profiling and structural analysis of PARP and tankyrase inhibitors

(2012) Elisabet Wahlberg et al.   NATURE BIOTECHNOLOGY

Positron emission tomography molecular imaging for drug development

(2011) Paul M. Matthews et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

Intravital Imaging

(2011) Mikael J. Pittet et al.   CELL

Can the flow of medicines be improved? Fundamental pharmacokinetic and pharmacological principles toward improving Phase II survival

(2011) Paul Morgan et al.   DRUG DISCOVERY TODAY

Single-cell dissection of transcriptional heterogeneity in human colon tumors

(2011) Piero Dalerba et al.   NATURE BIOTECHNOLOGY

Chemical genetics strategy identifies an HCV NS5A inhibitor with a potent clinical effect

(2010) Min Gao et al.   NATURE

The effect of plasma protein binding on in vivo efficacy: misconceptions in drug discovery

(2010) Dennis A. Smith et al.   NATURE REVIEWS DRUG DISCOVERY

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

Non-genetic cell-to-cell variability and the consequences for pharmacology

(2009) Mario Niepel et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Non-genetic origins of cell-to-cell variability in TRAIL-induced apoptosis

(2009) Sabrina L. Spencer et al.   NATURE

Identification of selective inhibitors of uncharacterized enzymes by high-throughput screening with fluorescent activity-based probes

(2009) Daniel A Bachovchin et al.   NATURE BIOTECHNOLOGY

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

4-[3-(4-Cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: A Novel Bioavailable Inhibitor of Poly(ADP-ribose) Polymerase-1

(2008) Keith A. Menear et al.   JOURNAL OF MEDICINAL CHEMISTRY