Identification of protein binding partners of small molecules using label-free methods

Identifying compound efficacy targets in phenotypic drug discovery

(2016) Markus Schirle et al.   DRUG DISCOVERY TODAY

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

(2016) J. Chang et al.   NATURAL PRODUCT REPORTS

Chemical proteomics approaches for identifying the cellular targets of natural products

(2016) M. H. Wright et al.   NATURAL PRODUCT REPORTS

Synthesis of novel 5-arylidenethiazolidinones with apoptotic properties via a three component reaction using piperidine as a bifunctional reagent

(2016) Chandramohan Bathula et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Target identification of natural and traditional medicines with quantitative chemical proteomics approaches

(2016) Jigang Wang et al.   PHARMACOLOGY & THERAPEUTICS

Photoaffinity labeling in target- and binding-site identification

(2015) Ewan Smith et al.   Future Medicinal Chemistry

Recent developments and applications of clickable photoprobes in medicinal chemistry and chemical biology

(2015) David J Lapinsky et al.   Future Medicinal Chemistry

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

Back to the Future with Phenotypic Screening

(2014) Marguerite Prior et al.   ACS Chemical Neuroscience

Proteasome Activation is a Mechanism for Pyrazolone Small Molecules Displaying Therapeutic Potential in Amyotrophic Lateral Sclerosis

(2014) Paul C. Trippier et al.   ACS Chemical Neuroscience

Synthesis and evaluation of effective photoaffinity probe molecule of furospinosulin-1, a hypoxia-selective growth inhibitor

(2014) Naoyuki Kotoku et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Target Identification of Grape Seed Extract in Colorectal Cancer Using Drug Affinity Responsive Target Stability (DARTS) Technique: Role of Endoplasmic Reticulum Stress Response Proteins

(2014) Molly Derry et al.   CURRENT CANCER DRUG TARGETS

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

The metabolite α-ketoglutarate extends lifespan by inhibiting ATP synthase and TOR

(2014) Randall M. Chin et al.   NATURE

The discovery of first-in-class drugs: origins and evolution

(2014) Jörg Eder et al.   NATURE REVIEWS DRUG DISCOVERY

Phenotypic screening in cancer drug discovery — past, present and future

(2014) John G. Moffat et al.   NATURE REVIEWS DRUG DISCOVERY

Fulleropyrrolidine interlayers: Tailoring electrodes to raise organic solar cell efficiency

(2014) Zachariah A. Page et al.   SCIENCE

Quantitative phenotypic and pathway profiling guides rational drug combination strategies

(2014) John C. Dawson et al.   Frontiers in Pharmacology

High-throughput screen identifies disulfiram as a potential therapeutic for triple-negative breast cancer cells: Interaction with IQ motif-containing factors

(2013) Tyler Robinson et al.   CELL CYCLE

Target deconvolution techniques in modern phenotypic profiling

(2013) Jiyoun Lee et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Drug Discovery for Neglected Diseases: Molecular Target-Based and Phenotypic Approaches

(2013) Ian H. Gilbert   JOURNAL OF MEDICINAL CHEMISTRY

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

(2013) Monica Schenone et al.   Nature Chemical Biology

Identification of a Mitochondrial Target of Thiazolidinedione Insulin Sensitizers (mTOT)—Relationship to Newly Identified Mitochondrial Pyruvate Carrier Proteins

(2013) Jerry R. Colca et al.   PLoS One

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

(2013) D. M. Molina et al.   SCIENCE

Dichloroacetate induces protective autophagy in LoVo cells: involvement of cathepsin D/thioredoxin-like protein 1 and Akt-mTOR-mediated signaling

(2013) F Gong et al.   Cell Death & Disease

High-Resolution Enabled TMT 8-plexing

(2012) Thilo Werner et al.   ANALYTICAL CHEMISTRY

Development of clickable active site-directed photoaffinity probes for γ-secretase

(2012) Christina J. Crump et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Functional genomic and high-content screening for target discovery and deconvolution

(2012) Susanne Heynen-Genel et al.   Expert Opinion on Drug Discovery

Chemoproteomic approaches to drug target identification and drug profiling

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

Design and synthesis of novel photoaffinity probes for study of the target proteins of oleanolic acid

(2011) Liying Zhang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

How were new medicines discovered?

(2011) David C. Swinney et al.   NATURE REVIEWS DRUG DISCOVERY

Identification of Direct Protein Targets of Small Molecules

(2010) Brett Lomenick et al.   ACS Chemical Biology

Activity-based Proteomics of Enzyme Superfamilies: Serine Hydrolases as a Case Study

(2010) Gabriel M. Simon et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

A Small Molecule Primes Embryonic Stem Cells for Differentiation

(2009) Shoutian Zhu et al.   Cell Stem Cell

Small-molecule affinity chromatography coupled mass spectrometry for drug target deconvolution

(2009) Chaitanya Saxena et al.   Expert Opinion on Drug Discovery

Capture of Drug Targets from Live Cells Using a Multipurpose Immuno-Chemo-Proteomics Tool

(2009) Chaitanya Saxena et al.   JOURNAL OF PROTEOME RESEARCH

Identifying the proteins to which small-molecule probes and drugs bind in cells

(2009) S.-E. Ong et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

An Immuno-Chemo-Proteomics Method for Drug Target Deconvolution

(2008) Chaitanya Saxena et al.   JOURNAL OF PROTEOME RESEARCH