CETSA quantitatively verifies in vivo target engagement of novel RIPK1 inhibitors in various biospecimens

Complex Pathologic Roles of RIPK1 and RIPK3: Moving Beyond Necroptosis

(2017) Kelby W. Wegner et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

The Cellular Thermal Shift Assay: A Novel Biophysical Assay for In Situ Drug Target Engagement and Mechanistic Biomarker Studies

(2016) Daniel Martinez Molina et al.   Annual Review of Pharmacology and Toxicology

RIPK3 deficiency or catalytically inactive RIPK1 provides greater benefit than MLKL deficiency in mouse models of inflammation and tissue injury

(2016) K Newton et al.   CELL DEATH AND DIFFERENTIATION

Generation of small molecules to interfere with regulated necrosis

(2016) Alexei Degterev et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors

(2016) Philip A. Harris et al.   JOURNAL OF MEDICINAL CHEMISTRY

RIPK1 mediates axonal degeneration by promoting inflammation and necroptosis in ALS

(2016) Yasushi Ito et al.   SCIENCE

CETSA screening identifies known and novel thymidylate synthase inhibitors and slow intracellular activation of 5-fluorouracil

(2016) Helena Almqvist et al.   Nature Communications

Target Engagement in Lead Generation

(2015) Timothy B. Durham et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Characterization of RIPK3-mediated phosphorylation of the activation loop of MLKL during necroptosis

(2015) D A Rodriguez et al.   CELL DEATH AND DIFFERENTIATION

Necrostatin-1 alleviates reperfusion injury following acute myocardial infarction in pigs

(2015) Stefan Koudstaal et al.   EUROPEAN JOURNAL OF CLINICAL INVESTIGATION

An analysis of the attrition of drug candidates from four major pharmaceutical companies

(2015) Michael J. Waring et al.   NATURE REVIEWS DRUG DISCOVERY

Structure Guided Design of Potent and Selective Ponatinib-Based Hybrid Inhibitors for RIPK1

(2015) Malek Najjar et al.   Cell Reports

Activation of Necroptosis in Multiple Sclerosis

(2015) Dimitry Ofengeim et al.   Cell Reports

Cutting Edge: RIPK1 Kinase Inactive Mice Are Viable and Protected from TNF-Induced Necroptosis In Vivo

(2014) Apostolos Polykratis et al.   JOURNAL OF IMMUNOLOGY

Cutting Edge: RIP1 Kinase Activity Is Dispensable for Normal Development but Is a Key Regulator of Inflammation in SHARPIN-Deficient Mice

(2014) S. B. Berger et al.   JOURNAL OF IMMUNOLOGY

NQO2 Is a Reactive Oxygen Species Generating Off-Target for Acetaminophen

(2014) Teemu P. Miettinen et al.   MOLECULAR PHARMACEUTICS

The cellular thermal shift assay for evaluating drug target interactions in cells

(2014) Rozbeh Jafari et al.   Nature Protocols

The Pseudokinase MLKL Mediates Necroptosis via a Molecular Switch Mechanism

(2013) James M. Murphy et al.   IMMUNITY

Target validation using chemical probes

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

Translational PET imaging research

(2013) Richard J. Hargreaves et al.   NEUROBIOLOGY OF DISEASE

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

(2013) D. M. Molina et al.   SCIENCE

Discovery of Small Molecule RIP1 Kinase Inhibitors for the Treatment of Pathologies Associated with Necroptosis

(2013) Philip A. Harris 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

Experimental autoimmune encephalomyelitis (EAE) as a model for multiple sclerosis (MS)

(2011) Cris S Constantinescu et al.   BRITISH JOURNAL OF PHARMACOLOGY

Can the flow of medicines be improved? Fundamental pharmacokinetic and pharmacological principles toward improving Phase II survival

(2011) Paul Morgan et al.   DRUG DISCOVERY TODAY

RIP Kinase-Dependent Necrosis Drives Lethal Systemic Inflammatory Response Syndrome

(2011) Linde Duprez et al.   IMMUNITY

The resurgence of covalent drugs

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

Physiological levels of ATP negatively regulate proteasome function

(2010) Hongbiao Huang et al.   CELL RESEARCH

Receptor Interacting Protein Kinase-3 Determines Cellular Necrotic Response to TNF-α

(2009) Sudan He et al.   CELL

Identification of RIP1 kinase as a specific cellular target of necrostatins

(2008) Alexei Degterev et al.   Nature Chemical Biology