Prediction of intracellular exposure bridges the gap between target- and cell-based drug discovery

Intracellular drug bioavailability: a new predictor of system dependent drug disposition

(2017) André Mateus et al.   Scientific Reports

A Modular Probe Strategy for Drug Localization, Target Identification and Target Occupancy Measurement on Single Cell Level

(2016) Anna Rutkowska et al.   ACS Chemical Biology

SEPT8 modulates β-amyloidogenic processing of APP by affecting the sorting and accumulation of BACE1

(2016) Kaisa M. A. Kurkinen et al.   JOURNAL OF CELL SCIENCE

Proteome-wide covalent ligand discovery in native biological systems

(2016) Keriann M. Backus et al.   NATURE

Thermal profiling reveals phenylalanine hydroxylase as an off-target of panobinostat

(2016) Isabelle Becher et al.   Nature Chemical Biology

Chemoproteomic profiling and discovery of protein electrophiles in human cells

(2016) Megan L. Matthews et al.   Nature Chemistry

CETSA screening identifies known and novel thymidylate synthase inhibitors and slow intracellular activation of 5-fluorouracil

(2016) Helena Almqvist et al.   Nature Communications

Extending kinome coverage by analysis of kinase inhibitor broad profiling data

(2015) Edgar Jacoby et al.   DRUG DISCOVERY TODAY

Cell permeable affinity- and activity-based probes

(2015) Lyn H Jones   Future Medicinal Chemistry

Comprehensive characterization of the Published Kinase Inhibitor Set

(2015) Jonathan M Elkins et al.   NATURE BIOTECHNOLOGY

Prolonged and tunable residence time using reversible covalent kinase inhibitors

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

Proteome-wide drug and metabolite interaction mapping by thermal-stability profiling

(2015) Kilian V M Huber et al.   NATURE METHODS

Visualizing APP and BACE-1 approximation in neurons yields insight into the amyloidogenic pathway

(2015) Utpal Das et al.   NATURE NEUROSCIENCE

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

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

Target engagement and drug residence time can be observed in living cells with BRET

(2015) Matthew B. Robers et al.   Nature Communications

Modifications of the endosomal compartment in peripheral blood mononuclear cells and fibroblasts from Alzheimer’s disease patients

(2015) F Corlier et al.   Translational Psychiatry

ATP-Mediated Kinome Selectivity: The Missing Link in Understanding the Contribution of Individual JAK Kinase Isoforms to Cellular Signaling

(2014) Atli Thorarensen et al.   ACS Chemical Biology

A High-Throughput Cell-Based Method to Predict the Unbound Drug Fraction in the Brain

(2014) André Mateus et al.   JOURNAL OF MEDICINAL CHEMISTRY

Amine-Containing Molecules and the Induction of an Expanded Lysosomal Volume Phenotype: A Structure–Activity Relationship Study

(2014) Randall Logan et al.   JOURNAL OF PHARMACEUTICAL SCIENCES

Targeting the β secretase BACE1 for Alzheimer's disease therapy

(2014) Riqiang Yan et al.   LANCET NEUROLOGY

Intracellular drug concentration and disposition – The missing link?

(2014) Michael M. Hann et al.   METHODS

Imaging the intracellular distribution of tyrosine kinase inhibitors in living cells with quantitative hyperspectral stimulated Raman scattering

(2014) Dan Fu et al.   Nature Chemistry

The cellular thermal shift assay for evaluating drug target interactions in cells

(2014) Rozbeh Jafari et al.   Nature Protocols

Lessons learned from the fate of AstraZeneca's drug pipeline: a five-dimensional framework

(2014) David Cook et al.   NATURE REVIEWS DRUG DISCOVERY

Tracking cancer drugs in living cells by thermal profiling of the proteome

(2014) M. M. Savitski et al.   SCIENCE

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

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

The Alzheimer’s β-secretase BACE1 localizes to normal presynaptic terminals and to dystrophic presynaptic terminals surrounding amyloid plaques

(2013) Patty C. Kandalepas et al.   ACTA NEUROPATHOLOGICA

Identification of Malate Dehydrogenase 2 as a Target Protein of the HIF-1 Inhibitor LW6 using Chemical Probes

(2013) Kyeong Lee et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

p38 MAPK/PP2Acα/TTP pathway on the connection of TNF-α and caspases activation on hydroquinone-induced apoptosis

(2013) Wen-Hsin Liu et al.   CARCINOGENESIS

Differential selectivity of JAK2 inhibitors in enzymatic and cellular settings

(2013) Violeta Yu et al.   EXPERIMENTAL HEMATOLOGY

Rapid Measurement of Intracellular Unbound Drug Concentrations

(2013) André Mateus et al.   MOLECULAR PHARMACEUTICS

Target identification and mechanism of action in chemical biology and drug discovery

(2013) Monica Schenone et al.   Nature Chemical Biology

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

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

(2013) D. M. Molina et al.   SCIENCE

BACE1 Protein Endocytosis and Trafficking Are Differentially Regulated by Ubiquitination at Lysine 501 and the Di-leucine Motif in the Carboxyl Terminus

(2012) Eugene L. Kang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Classification of Inhibitors of Hepatic Organic Anion Transporting Polypeptides (OATPs): Influence of Protein Expression on Drug–Drug Interactions

(2012) Maria Karlgren et al.   JOURNAL OF MEDICINAL CHEMISTRY

A public-private partnership to unlock the untargeted kinome

(2012) Stefan Knapp et al.   Nature Chemical Biology

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

Molecular obesity, potency and other addictions in drug discovery

(2011) Michael M. Hann   MedChemComm

Measurement of Unbound Drug Exposure in Brain: Modeling of pH Partitioning Explains Diverging Results between the Brain Slice and Brain Homogenate Methods

(2010) M. Friden et al.   DRUG METABOLISM AND DISPOSITION

Mechanisms of amine accumulation in, and egress from, lysosomes

(2010) Stephen DB Goldman et al.   Bioanalysis

Development of a High-Throughput Brain Slice Method for Studying Drug Distribution in the Central Nervous System

(2009) M. Friden et al.   DRUG METABOLISM AND DISPOSITION

The  -Secretase Enzyme BACE in Health and Alzheimer's Disease: Regulation, Cell Biology, Function, and Therapeutic Potential

(2009) R. Vassar et al.   JOURNAL OF NEUROSCIENCE

Subcellular targeting strategies for drug design and delivery

(2009) Lawrence Rajendran et al.   NATURE REVIEWS DRUG DISCOVERY

Sensors and regulators of intracellular pH

(2009) Joseph R. Casey et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Identification of Novel Specific and General Inhibitors of the Three Major Human ATP-Binding Cassette Transporters P-gp, BCRP and MRP2 Among Registered Drugs

(2009) Pär Matsson et al.   PHARMACEUTICAL RESEARCH

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

Tristetraprolin regulates TNF TNF-α mRNA stability via a proteasome dependent mechanism involving the combined action of the ERK and p38 pathways

(2007) Kristen M. Deleault et al.   MOLECULAR IMMUNOLOGY