TAK1 selective inhibition: state of the art and future opportunities

Insights into the Biosynthesis of 12-Membered Resorcylic Acid Lactones from Heterologous Production in Saccharomyces cerevisiae

(2014) Yuquan Xu et al.   ACS Chemical Biology

TAK1 kinase switches cell fate from apoptosis to necrosis following TNF stimulation

(2014) Sho Morioka et al.   JOURNAL OF CELL BIOLOGY

Synthetic Phosphorylation of p38α Recapitulates Protein Kinase Activity

(2014) K. Phin Chooi et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Positive Feedback Within a Kinase Signaling Complex Functions as a Switch Mechanism for NF- B Activation

(2014) H. Shinohara et al.   SCIENCE

Activation of TAK1 by MYD88 L265P drives malignant B-cell Growth in non-Hodgkin lymphoma

(2014) S M Ansell et al.   Blood Cancer Journal

TAK1 inhibitor 5Z-7-oxozeaenol sensitizes neuroblastoma to chemotherapy

(2013) Yihui Fan et al.   APOPTOSIS

Discovery and optimization of 7-aminofuro[2,3-c]pyridine inhibitors of TAK1

(2013) Keith R. Hornberger et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of 7-aminofuro[2,3-c]pyridine inhibitors of TAK1: Optimization of kinase selectivity and pharmacokinetics

(2013) Keith R. Hornberger et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

RIPK3 contributes to TNFR1-mediated RIPK1 kinase-dependent apoptosis in conditions of cIAP1/2 depletion or TAK1 kinase inhibition

(2013) Y Dondelinger et al.   CELL DEATH AND DIFFERENTIATION

TAK1 Inhibition in the DFG-Out Conformation

(2013) Iain Kilty et al.   Chemical Biology & Drug Design

Developing Irreversible Inhibitors of the Protein Kinase Cysteinome

(2013) Qingsong Liu et al.   CHEMISTRY & BIOLOGY

Target validation using chemical probes

(2013) Mark E Bunnage et al.   Nature Chemical Biology

Mechanism and consequence of the autoactivation of p38α mitogen-activated protein kinase promoted by TAB1

(2013) Gian Felice De Nicola et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

In Vivo Knockdown of TAK1 Accelerates Bone Marrow Proliferation/Differentiation and Induces Systemic Inflammation

(2013) Paul M. Vink et al.   PLoS One

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

(2012) Jiaquan Wu et al.   ACS Chemical Biology

Essential role of TAK1 in regulating mantle cell lymphoma survival

(2012) D. Buglio et al.   BLOOD

TAK1 Inhibition Promotes Apoptosis in KRAS-Dependent Colon Cancers

(2012) Anurag Singh et al.   CELL

Identification of Type-II Inhibitors Using Kinase Structures

(2012) Frank Lovering et al.   Chemical Biology & Drug Design

How Chemoproteomics Can Enable Drug Discovery and Development

(2012) Raymond E. Moellering et al.   CHEMISTRY & BIOLOGY

Cis-enone Resorcylic Acid Lactones (RALs) as Irreversible Protein Kinase Inhibitors

(2012) Linyi Wei et al.   CURRENT PHARMACEUTICAL DESIGN

TAK1 Negatively Regulates NF-κB and p38 MAP Kinase Activation in Gr-1+CD11b+ Neutrophils

(2012) Adebusola Alagbala Ajibade et al.   IMMUNITY

Essential Role for IKKβ in Production of Type 1 Interferons by Plasmacytoid Dendritic Cells

(2012) Eduardo Pauls et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Fully Functionalized Small-Molecule Probes for Integrated Phenotypic Screening and Target Identification

(2012) Justin S. Cisar et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

The IkappaB Kinase Family Phosphorylates the Parkinson’s Disease Kinase LRRK2 at Ser935 and Ser910 during Toll-Like Receptor Signaling

(2012) Nicolas Dzamko et al.   PLoS One

Transforming growth factor beta-activated kinase 1 (TAK1)-dependent checkpoint in the survival of dendritic cells promotes immune homeostasis and function

(2012) Y. Wang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Oxindole derivatives as inhibitors of TAK1 kinase

(2011) Jeffrey W. Lockman et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design and Synthesis of Inhaled p38 Inhibitors for the Treatment of Chronic Obstructive Pulmonary Disease

(2011) David S. Millan 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

Modulation of Pancreatic Cancer Chemoresistance by Inhibition of TAK1

(2011) Davide Melisi et al.   JNCI-Journal of the National Cancer Institute

The Prevalence of TNFα-Induced Necrosis over Apoptosis Is Determined by TAK1-RIP1 Interplay

(2011) Seda Çöl Arslan et al.   PLoS One

In vivo RNAi-mediated silencing of TAK1 decreases inflammatory Th1 and Th17 cells through targeting of myeloid cells

(2010) G. Courties et al.   BLOOD

In Vivo Efficacy of Natural Product-Inspired Irreversible Kinase Inhibitors

(2010) Sofia Barluenga et al.   CHEMBIOCHEM

A comprehensive overview on genomically directed assembly of aromatic polyketides and macrolide lactones using fungal megasynthases

(2010) Takayoshi Saruwatari et al.   JOURNAL OF ANTIBIOTICS

Rapid assessment of a novel series of selective CB2 agonists using parallel synthesis protocols: A Lipophilic Efficiency (LipE) analysis

(2009) Thomas Ryckmans et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

A critical role of TAK1 in B-cell receptor–mediated nuclear factor κB activation

(2009) James Schuman et al.   BLOOD

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

Transforming Growth Factor β-activated Kinase 1 (TAK1) Kinase Adaptor, TAK1-binding Protein 2, Plays Dual Roles in TAK1 Signaling by Recruiting Both an Activator and an Inhibitor of TAK1 Kinase in Tumor Necrosis Factor Signaling Pathway

(2009) Peter Broglie et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Epoxyquinol B, a Naturally Occurring Pentaketide Dimer, Inhibits NF-κB Signaling by Crosslinking TAK1

(2008) Hiroshi KAMIYAMA et al.   BIOSCIENCE BIOTECHNOLOGY AND BIOCHEMISTRY