Determining target engagement in living systems

Modelling vemurafenib resistance in melanoma reveals a strategy to forestall drug resistance

(2013) Meghna Das Thakur et al.   NATURE

Activity-Based Probes for Studying the Activity of Flavin-Dependent Oxidases and for the Protein Target Profiling of Monoamine Oxidase Inhibitors

(2012) Joanna M. Krysiak et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Clinical perspectives for irreversible tyrosine kinase inhibitors in cancer

(2012) Caterina Carmi et al.   BIOCHEMICAL PHARMACOLOGY

Interrogating Signaling Nodes Involved in Cellular Transformations Using Kinase Activity Probes

(2012) Cliff I. Stains et al.   CHEMISTRY & BIOLOGY

A Nonpeptidic Cathepsin S Activity-Based Probe for Noninvasive Optical Imaging of Tumor-Associated Macrophages

(2012) Martijn Verdoes et al.   CHEMISTRY & BIOLOGY

Bruton Tyrosine Kinase Inhibitor Ibrutinib (PCI-32765) Has Significant Activity in Patients With Relapsed/Refractory B-Cell Malignancies

(2012) Ranjana H. Advani et al.   JOURNAL OF CLINICAL ONCOLOGY

Confirming Target Engagement for Reversible Inhibitors in Vivo by Kinetically Tuned Activity-Based Probes

(2012) Alexander Adibekian et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Functional Imaging of Legumain in Cancer Using a New Quenched Activity-Based Probe

(2012) Laura E. Edgington et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Drug candidates derailed in case of mistaken identity

(2012) Heidi Ledford   NATURE

Using transcriptome sequencing to identify mechanisms of drug action and resistance

(2012) Sarah A Wacker et al.   Nature Chemical Biology

DAGLβ inhibition perturbs a lipid network involved in macrophage inflammatory responses

(2012) Ku-Lung Hsu et al.   Nature Chemical Biology

The synthesis and in vivo evaluation of [18F]PF-9811: a novel PET ligand for imaging brain fatty acid amide hydrolase (FAAH)

(2012) Marc B. Skaddan et al.   NUCLEAR MEDICINE AND BIOLOGY

Brain Penetrant LRRK2 Inhibitor

(2012) Hwan Geun Choi et al.   ACS Medicinal Chemistry Letters

Positron emission tomography molecular imaging for drug development

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

In Situ Kinase Profiling Reveals Functionally Relevant Properties of Native Kinases

(2011) Matthew P. Patricelli et al.   CHEMISTRY & BIOLOGY

Lipidomics at the Interface of Structure and Function in Systems Biology

(2011) Richard W. Gross et al.   CHEMISTRY & BIOLOGY

Nonproteasomal Targets of the Proteasome Inhibitors Bortezomib and Carfilzomib: a Link to Clinical Adverse Events

(2011) S. Arastu-Kapur et al.   CLINICAL CANCER RESEARCH

Functional imaging of proteases: recent advances in the design and application of substrate-based and activity-based probes

(2011) Laura E Edgington et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Chemoproteomics profiling of HDAC inhibitors reveals selective targeting of HDAC complexes

(2011) Marcus Bantscheff et al.   NATURE BIOTECHNOLOGY

Identification of Direct Target Engagement Biomarkers for Kinase-Targeted Therapeutics

(2011) Cloud P. Paweletz et al.   PLoS One

Academic cross-fertilization by public screening yields a remarkable class of protein phosphatase methylesterase-1 inhibitors

(2011) D. A. Bachovchin et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

A HIF-Regulated VHL-PTP1B-Src Signaling Axis Identifies a Therapeutic Target in Renal Cell Carcinoma

(2011) N. Suwaki et al.   Science Translational Medicine

Evaluation of 11C-GSK189254 as a Novel Radioligand for the H3 Receptor in Humans Using PET

(2010) S. Ashworth et al.   JOURNAL OF NUCLEAR MEDICINE

Chemical phylogenetics of histone deacetylases

(2010) James E Bradner et al.   Nature Chemical Biology

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

Small-animal positron emission tomography as a tool for neuropharmacology

(2010) Sophie Lancelot et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Discovery and Characterization of a Highly Selective FAAH Inhibitor that Reduces Inflammatory Pain

(2009) Kay Ahn et al.   CHEMISTRY & BIOLOGY

Sensitive multiplexed analysis of kinase activities and activity-based kinase identification

(2009) Kazuishi Kubota et al.   NATURE BIOTECHNOLOGY

Noninvasive optical imaging of apoptosis by caspase-targeted activity-based probes

(2009) Laura E Edgington et al.   NATURE MEDICINE

Target site occupancy: Emerging generalizations from clinical and preclinical studies

(2009) Sarah Grimwood et al.   PHARMACOLOGY & THERAPEUTICS

Accelerating Drug Development Using Biomarkers: A Case Study with Sitagliptin, A Novel DPP4 Inhibitor for Type 2 Diabetes

(2008) Rajesh Krishna et al.   AAPS Journal

Activity-Based Protein Profiling: From Enzyme Chemistry to Proteomic Chemistry

(2008) Benjamin F. Cravatt et al.   Annual Review of Biochemistry

Peptidase substrates via global peptide profiling

(2008) Debarati M Tagore et al.   Nature Chemical Biology

Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases

(2008) Beth Apsel et al.   Nature Chemical Biology

Selective blockade of 2-arachidonoylglycerol hydrolysis produces cannabinoid behavioral effects

(2008) Jonathan Z Long et al.   Nature Chemical Biology

The Role of Imaging in Proof of Concept for CNS Drug Discovery and Development

(2008) Dean F Wong et al.   NEUROPSYCHOPHARMACOLOGY

Strategic Approach to Fit-for-Purpose Biomarkers in Drug Development

(2007) John A. Wagner   Annual Review of Pharmacology and Toxicology