Rational Design of Resorcylic Acid Lactone Analogues as Covalent MNK1/2 Kinase Inhibitors by Tuning the Reactivity of an Enamide Michael Acceptor

Targeting of the MNK-eIF4E axis in blast crisis chronic myeloid leukemia inhibits leukemia stem cell function

(2013) S. Lim et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Selective affinity-based probe for oncogenic kinases suitable for live cell imaging

(2013) Claudio Zambaldo et al.   Chemical Science

Mechanism and In Vitro Pharmacology of TAK1 Inhibition by (5Z)-7-Oxozeaenol

(2012) Jiaquan Wu et al.   ACS Chemical Biology

Reversible Covalent Inhibition of a Protein Target

(2012) Chang-Uk Lee et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Reversible targeting of noncatalytic cysteines with chemically tuned electrophiles

(2012) Iana M Serafimova et al.   Nature Chemical Biology

Polyubiquitination of Transforming Growth Factor β (TGFβ)-associated Kinase 1 Mediates Nuclear Factor-κB Activation in Response to Different Inflammatory Stimuli

(2011) Anahita Hamidi et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

Resorcylic Acid Lactones with Cytotoxic and NF-κB Inhibitory Activities and Their Structure–Activity Relationships

(2011) Sloan Ayers et al.   JOURNAL OF NATURAL PRODUCTS

The resurgence of covalent drugs

(2011) Juswinder Singh et al.   NATURE REVIEWS DRUG DISCOVERY

Exploring Aigialomycin D and Its Analogues as Protein Kinase Inhibitors for Cancer Targets

(2011) Jin Xu et al.   ACS Medicinal Chemistry Letters

An NMR Spectroscopic Method to Identify and Classify Thiol-Trapping Agents: Revival of Michael Acceptors for Drug Discovery?

(2010) Cristina Avonto et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Discovery of anti-inflammatory clinical candidate E6201, inspired from resorcylic lactone LL-Z1640-2, III

(2010) Yongchun Shen et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

In Vivo Efficacy of Natural Product-Inspired Irreversible Kinase Inhibitors

(2010) Sofia Barluenga et al.   CHEMBIOCHEM

A Structure-Guided Approach to Creating Covalent FGFR Inhibitors

(2010) Wenjun Zhou et al.   CHEMISTRY & BIOLOGY

Molecular Editing of Kinase-Targeting Resorcylic Acid Lactones (RAL): Fluoroenone RAL

(2010) Rajamalleswaramma Jogireddy et al.   ChemMedChem

Strategies for discovering and derisking covalent, irreversible enzyme inhibitors

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

Autoactivation of Transforming Growth Factor β-activated Kinase 1 Is a Sequential Bimolecular Process

(2010) Roland Scholz et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Discovery of Mitogen-Activated Protein Kinase-Interacting Kinase 1 Inhibitors by a Comprehensive Fragment-Oriented Virtual Screening Approach

(2010) Julen Oyarzabal et al.   JOURNAL OF MEDICINAL CHEMISTRY

Access to Resorcylic Acid LactonesviaPhosphonate Based Intramolecular Olefination

(2010) Carmela Napolitano et al.   JOURNAL OF ORGANIC CHEMISTRY

Selective irreversible inhibition of a protease by targeting a noncatalytic cysteine

(2010) Margit Hagel et al.   Nature Chemical Biology

Combined deficiency for MAP kinase-interacting kinase 1 and 2 (Mnk1 and Mnk2) delays tumor development

(2010) T. Ueda et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Mnk earmarks eIF4E for cancer therapy

(2010) N. Hay   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Kinase Inhibition by Deoxy Analogues of the Resorcylic Lactone L-783277

(2010) Marc Liniger et al.   ACS Medicinal Chemistry Letters

Synthesis of a Resorcylic Acid Lactone (RAL) Library Using Fluorous-Mixture Synthesis and Profile of its Selectivity Against a Panel of Kinases

(2009) Rajamalleswaramma Jogireddy et al.   CHEMISTRY-A EUROPEAN JOURNAL

Divergent Syntheses of Resorcylic Acid Lactones: L-783277, LL-Z1640-2, and Hypothemycin

(2009) Pierre-Yves Dakas et al.   CHEMISTRY-A EUROPEAN JOURNAL

Covalent Modifiers: An Orthogonal Approach to Drug Design

(2009) Michele H. Potashman et al.   JOURNAL OF MEDICINAL CHEMISTRY

E6201 [(3S,4R,5Z,8S,9S,11E)-14-(Ethylamino)-8, 9,16-trihydroxy-3,4-dimethyl-3,4,9,19-tetrahydro-1H-2-benzoxacyclotetradecine-1,7(8H)-dione], a Novel Kinase Inhibitor of Mitogen-Activated Protein Kinase/Extracellular Signal-Regulated Kinase Kinase (MEK)-1 and MEK Kinase-1: In Vitro Characterization of Its Anti-Inflammatory and Antihyperproliferative Activities

(2009) M. Goto et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Resorcylic acid lactones: A pluripotent scaffold with therapeutic potential

(2008) Sofia Barluenga et al.   COMPTES RENDUS CHIMIE

Molecular modeling and crystal structure of ERK2–hypothemycin complexes

(2008) Giulio Rastelli et al.   JOURNAL OF STRUCTURAL BIOLOGY

A novel palladium-catalyzed hydroalkoxylation of alkenes with a migration of double bond

(2008) Jiajing Tan et al.   ORGANIC & BIOMOLECULAR CHEMISTRY