Advances in identification and validation of protein targets of natural products without chemical modification

Identifying compound efficacy targets in phenotypic drug discovery

(2016) Markus Schirle et al.   DRUG DISCOVERY TODAY

Target deconvolution of bioactive small molecules: the heart of chemical biology and drug discovery

(2015) Hye Jin Jung et al.   ARCHIVES OF PHARMACAL RESEARCH

CCR 20th Anniversary Commentary: Determining a Pharmacokinetic/Pharmacodynamic Relationship for Sunitinib--A Look Back

(2015) D. B. Mendel et al.   CLINICAL CANCER RESEARCH

The impact of CRISPR–Cas9 on target identification and validation

(2015) Jonathan D. Moore   DRUG DISCOVERY TODAY

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

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

Network pharmacology applications to map the unexplored target space and therapeutic potential of natural products

(2015) Milla Kibble et al.   NATURAL PRODUCT REPORTS

A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models

(2015) Elayne Chan-Penebre et al.   Nature Chemical Biology

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

(2015) Holger Franken et al.   Nature Protocols

The Cyclic Peptide Ecumicin Targeting ClpC1 Is Active against Mycobacterium tuberculosis In Vivo

(2014) Wei Gao et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Probabilistic drug connectivity mapping

(2014) Juuso A Parkkinen et al.   BMC BIOINFORMATICS

Stable Isotope Labeling with Amino Acids in Cell Culture (SILAC)-Based Strategy for Proteome-Wide Thermodynamic Analysis of Protein-Ligand Binding Interactions

(2014) Duc T. Tran et al.   MOLECULAR & CELLULAR PROTEOMICS

NQO2 Is a Reactive Oxygen Species Generating Off-Target for Acetaminophen

(2014) Teemu P. Miettinen et al.   MOLECULAR PHARMACEUTICS

Mass spectrometry imaging of plant metabolites – principles and possibilities

(2014) Nanna Bjarnholt et al.   NATURAL PRODUCT REPORTS

DNA sequencing and CRISPR-Cas9 gene editing for target validation in mammalian cells

(2014) Yegor Smurnyy et al.   Nature Chemical Biology

DrugTargetSeqR: a genomics- and CRISPR-Cas9–based method to analyze drug targets

(2014) Corynn Kasap et al.   Nature Chemical Biology

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

(2014) Rozbeh Jafari et al.   Nature Protocols

Queries of MALDI-imaging global datasets identifying ion mass signatures associated with tissue compartments

(2014) Thomas E. Fehniger et al.   PROTEOMICS

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

A Systematic Mammalian Genetic Interaction Map Reveals Pathways Underlying Ricin Susceptibility

(2013) Michael C. Bassik et al.   CELL

Methods for the Elucidation of Protein-Small Molecule Interactions

(2013) Amanda McFedries et al.   CHEMISTRY & BIOLOGY

Experimental Models to Study Drug Distributions in Tissue Using MALDI Mass Spectrometry Imaging

(2013) Ákos Végvári et al.   JOURNAL OF PROTEOME RESEARCH

Target identification of small molecules based on chemical biology approaches

(2013) Yushi Futamura et al.   Molecular BioSystems

High-frequency off-target mutagenesis induced by CRISPR-Cas nucleases in human cells

(2013) Yanfang Fu et al.   NATURE BIOTECHNOLOGY

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

(2013) Monica Schenone et al.   Nature Chemical Biology

Genome engineering using the CRISPR-Cas9 system

(2013) F Ann Ran et al.   Nature Protocols

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

(2013) D. M. Molina et al.   SCIENCE

RNA-Guided Human Genome Engineering via Cas9

(2013) P. Mali et al.   SCIENCE

Genome-Scale CRISPR-Cas9 Knockout Screening in Human Cells

(2013) Ophir Shalem et al.   SCIENCE

Genetic Screens in Human Cells Using the CRISPR-Cas9 System

(2013) Tim Wang et al.   SCIENCE

Multiplex Genome Engineering Using CRISPR/Cas Systems

(2013) L. Cong et al.   SCIENCE

In situ label-free imaging for visualizing the biotransformation of a bioactive polyphenol

(2013) Yoon Hee Kim et al.   Scientific Reports

Mass Spectrometry-Based Proteomics in Preclinical Drug Discovery

(2012) Markus Schirle et al.   CHEMISTRY & BIOLOGY

Applications of Connectivity Map in drug discovery and development

(2012) Xiaoyan A. Qu et al.   DRUG DISCOVERY TODAY

Cancer drug's survivin suppression called into question

(2012) David Holmes   NATURE MEDICINE

Thermodynamic analysis of protein-ligand binding interactions in complex biological mixtures using the stability of proteins from rates of oxidation

(2012) Erin C Strickland et al.   Nature Protocols

Identification of Small Molecule Activators of Cryptochrome

(2012) T. Hirota et al.   SCIENCE

A Programmable Dual-RNA-Guided DNA Endonuclease in Adaptive Bacterial Immunity

(2012) M. Jinek et al.   SCIENCE

Direct Demonstration of Tissue Uptake of an Inhaled Drug: Proof-of-Principle Study Using Matrix-Assisted Laser Desorption Ionization Mass Spectrometry Imaging

(2011) Thomas E. Fehniger et al.   ANALYTICAL CHEMISTRY

Identification and validation of protein targets of bioactive small molecules

(2011) Denis V. Titov et al.   BIOORGANIC & MEDICINAL CHEMISTRY

A Novel Method of Transcriptional Response Analysis to Facilitate Drug Repositioning for Cancer Therapy

(2011) G. Jin et al.   CANCER RESEARCH

Thermodynamic Analysis of Protein–Ligand Interactions in Complex Biological Mixtures using a Shotgun Proteomics Approach

(2011) Patrick D. DeArmond et al.   JOURNAL OF PROTEOME RESEARCH

Systematic exploration of essential yeast gene function with temperature-sensitive mutants

(2011) Zhijian Li et al.   NATURE BIOTECHNOLOGY

Natural product–inspired cascade synthesis yields modulators of centrosome integrity

(2011) Heiko Dückert et al.   Nature Chemical Biology

Bugs, drugs and chemical genomics

(2011) Terry Roemer et al.   Nature Chemical Biology

An Integrated Bioinformatics Approach Identifies Elevated Cyclin E2 Expression and E2F Activity as Distinct Features of Tamoxifen Resistant Breast Tumors

(2011) Lei Huang et al.   PLoS One

Identification of Genes Affecting the Toxicity of Anti-Cancer Drug Bortezomib by Genome-Wide Screening in S. pombe

(2011) Kojiro Takeda et al.   PLoS One

Pyrazinamide Inhibits Trans-Translation in Mycobacterium tuberculosis

(2011) W. Shi et al.   SCIENCE

MALDI imaging mass spectrometry of human tissue: method challenges and clinical perspectives

(2011) Erin H. Seeley et al.   TRENDS IN BIOTECHNOLOGY

Identification of Direct Protein Targets of Small Molecules

(2010) Brett Lomenick et al.   ACS Chemical Biology

Analysis of a genome-wide set of gene deletions in the fission yeast Schizosaccharomyces pombe

(2010) Dong-Uk Kim et al.   NATURE BIOTECHNOLOGY

Marine antifungal theonellamides target 3β-hydroxysterol to activate Rho1 signaling

(2010) Shinichi Nishimura et al.   Nature Chemical Biology

Quantitative proteomics approach for identifying protein-drug interactions in complex mixtures using protein stability measurements

(2010) G. M. West et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The Ras Pathway Modulator Melophlin A Targets Dynamins

(2009) Tanja Knoth et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Screening a genome-wide S. pombe deletion library identifies novel genes and pathways involved in genome stability maintenance

(2009) Gaurang P. Deshpande et al.   DNA REPAIR

Identification of novel hair-growth inducers by means of connectivity mapping

(2009) Yumiko Ishimatsu-Tsuji et al.   FASEB JOURNAL

Coordinated posttranscriptional mRNA population dynamics during T-cell activation

(2009) Neelanjan Mukherjee et al.   Molecular Systems Biology

Imaging mass spectrometry of natural products

(2009) Eduardo Esquenazi et al.   NATURAL PRODUCT REPORTS

A molecular barcoded yeast ORF library enables mode-of-action analysis of bioactive compounds

(2009) Cheuk Hei Ho et al.   NATURE BIOTECHNOLOGY

Target profiling of small molecules by chemical proteomics

(2009) Uwe Rix et al.   Nature Chemical Biology

Small molecule–mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer

(2009) Baozhi Chen 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

Thermodynamic Analysis of Protein Stability and Ligand Binding Using a Chemical Modification- and Mass Spectrometry-Based Strategy

(2008) Graham M. West et al.   ANALYTICAL CHEMISTRY

Identification of a potent natural triterpenoid inhibitor of proteosome chymotrypsin-like activity and NF- B with antimyeloma activity in vitro and in vivo

(2008) R. E. Tiedemann et al.   BLOOD

New insights into chemical biology from ORFeome libraries

(2008) Yoko Yashiroda et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Proteomic methods for drug target discovery

(2008) Lekha Sleno et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Identifying targets for drug discovery using bioinformatics

(2008) Yi-Ping Phoebe Chen et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

An integrated platform of genomic assays reveals small-molecule bioactivities

(2008) Shawn Hoon et al.   Nature Chemical Biology

Drug Target Identification Using Side-Effect Similarity

(2008) M. Campillos et al.   SCIENCE

Imaging mass spectrometry of proteins and peptides: 3D volume reconstruction

(2007) Malin Andersson et al.   NATURE METHODS