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

The Cellular Thermal Shift Assay: A Novel Biophysical Assay for In Situ Drug Target Engagement and Mechanistic Biomarker Studies

(2016) Daniel Martinez Molina et al.   Annual Review of Pharmacology and Toxicology

The Amino Acid Specificity for Activation of Phenylalanine Hydroxylase Matches the Specificity for Stabilization of Regulatory Domain Dimers

(2015) Shengnan Zhang et al.   BIOCHEMISTRY

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

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

Thermal proteome profiling monitors ligand interactions with cellular membrane proteins

(2015) Friedrich B M Reinhard et al.   NATURE METHODS

Thermal proteome profiling for unbiased identification of direct and indirect drug targets using multiplexed quantitative mass spectrometry

(2015) Holger Franken et al.   Nature Protocols

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

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

Activation of Phenylalanine Hydroxylase by Phenylalanine Does Not Require Binding in the Active Site

(2014) Kenneth M. Roberts et al.   BIOCHEMISTRY

Integrated genomic and functional analyses reveal glyoxalase I as a novel metabolic oncogene in human gastric cancer

(2014) F Hosoda et al.   ONCOGENE

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

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

Target Identification for Small Bioactive Molecules: Finding the Needle in the Haystack

(2013) Slava Ziegler et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Measuring and Managing Ratio Compression for Accurate iTRAQ/TMT Quantification

(2013) Mikhail M. Savitski et al.   JOURNAL OF PROTEOME RESEARCH

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

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

(2013) D. M. Molina et al.   SCIENCE

Affinity Profiling of the Cellular Kinome for the Nucleotide Cofactors ATP, ADP, and GTP

(2012) Isabelle Becher et al.   ACS Chemical Biology

High-Resolution Enabled TMT 8-plexing

(2012) Thilo Werner et al.   ANALYTICAL CHEMISTRY

Panobinostat in Patients With Relapsed/Refractory Hodgkin's Lymphoma After Autologous Stem-Cell Transplantation: Results of a Phase II Study

(2012) Anas Younes et al.   JOURNAL OF CLINICAL ONCOLOGY

Chemoproteomic approaches to drug target identification and drug profiling

(2011) Marcus Bantscheff et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Chemoproteomics profiling of HDAC inhibitors reveals selective targeting of HDAC complexes

(2011) Marcus Bantscheff et al.   NATURE BIOTECHNOLOGY

Targeted data acquisition for improved reproducibility and robustness of proteomic mass spectrometry assays

(2010) Mikhail M. Savitski et al.   JOURNAL OF THE AMERICAN SOCIETY FOR MASS SPECTROMETRY

Development of the pan-DAC inhibitor panobinostat (LBH589): Successes and challenges

(2009) Peter Atadja   CANCER LETTERS