Cysteine-reactive chemical probes based on a modular 4-aminopiperidine scaffold

GABAA receptor modulation by piperine and a non-TRPV1 activating derivative

(2013) Sophia Khom et al.   BIOCHEMICAL PHARMACOLOGY

Targeting caspases in cancer therapeutics

(2013) Patrick Hensley et al.   BIOLOGICAL CHEMISTRY

Synthesis and evaluation of novel azetidine analogs as potent inhibitors of vesicular [3H]dopamine uptake

(2013) Derong Ding et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Stereoselective Potencies and Relative Toxicities of γ-Coniceine and N-Methylconiine Enantiomers

(2013) Stephen T. Lee et al.   CHEMICAL RESEARCH IN TOXICOLOGY

Developing Irreversible Inhibitors of the Protein Kinase Cysteinome

(2013) Qingsong Liu et al.   CHEMISTRY & BIOLOGY

Discovery of 4-Amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (AZD5363), an Orally Bioavailable, Potent Inhibitor of Akt Kinases

(2013) Matt Addie et al.   JOURNAL OF MEDICINAL CHEMISTRY

Casuarinines A–J, Lycodine-Type Alkaloids from Lycopodiastrum casuarinoides

(2013) Yu Tang et al.   JOURNAL OF NATURAL PRODUCTS

1,3,5-Triazine as a Modular Scaffold for Covalent Inhibitors with Streamlined Target Identification

(2013) Ranjan Banerjee et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Diverse Functional Roles of Reactive Cysteines

(2012) Nicholas J. Pace et al.   ACS Chemical Biology

An Inhibitor of Glutathione S-Transferase Omega 1 that Selectively Targets Apoptotic Cells

(2012) Nicholas J. Pace et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Cellular Redox Pathways as a Therapeutic Target in the Treatment of Cancer

(2011) Alberto J. Montero et al.   DRUGS

Cysteine Mapping in Conformationally Distinct Kinase Nucleotide Binding Sites: Application to the Design of Selective Covalent Inhibitors

(2011) Emeline Leproult et al.   JOURNAL OF MEDICINAL CHEMISTRY

Potent and Selective Inhibitors of GlutathioneS-Transferase Omega 1 That Impair Cancer Drug Resistance

(2011) Katsunori Tsuboi et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Isoform-specific regulation of Akt by PDGF-induced reactive oxygen species

(2011) R. Wani et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Inhibition of Pyruvate Kinase M2 by Reactive Oxygen Species Contributes to Cellular Antioxidant Responses

(2011) D. Anastasiou et al.   SCIENCE

Glutathione transferase omega 1-1 (GSTO1-1) plays an anti-apoptotic role in cell resistance to cisplatin toxicity

(2010) S. Piaggi et al.   CARCINOGENESIS

Azetidine derivatives as novel γ-aminobutyric acid uptake inhibitors: Synthesis, biological evaluation, and structure–activity relationship

(2010) Mark R. Faust et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Strategies for discovering and derisking covalent, irreversible enzyme inhibitors

(2010) Douglas S Johnson et al.   Future Medicinal Chemistry

Akt Cys-310-targeted Inhibition by Hydroxylated Benzene Derivatives Is Tightly Linked to Their Immunosuppressive Effects

(2010) Ji Yeon Lee et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Quantitative reactivity profiling predicts functional cysteines in proteomes

(2010) Eranthie Weerapana et al.   NATURE

Crystal Structure of Human AKT1 with an Allosteric Inhibitor Reveals a New Mode of Kinase Inhibition

(2010) Wen-I Wu et al.   PLoS One

The two faces of PTP1B in cancer

(2009) Laurent Lessard et al.   BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS

Erratum: Identification of selective inhibitors of uncharacterized enzymes by high-throughput screening with fluorescent activity-based probes

(2009) Daniel A Bachovchin et al.   NATURE BIOTECHNOLOGY

Role of a Novel PH-Kinase Domain Interface in PKB/Akt Regulation: Structural Mechanism for Allosteric Inhibition

(2009) Véronique Calleja et al.   PLOS BIOLOGY

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

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

Disparate proteome reactivity profiles of carbon electrophiles

(2008) Eranthie Weerapana et al.   Nature Chemical Biology

Synthesis of pharmaceutically active compounds containing a disubstituted piperidine framework

(2007) Sara Källström et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Cysteine cathepsin proteases as pharmacological targets in cancer

(2007) Carmela Palermo et al.   TRENDS IN PHARMACOLOGICAL SCIENCES