(Q38931379)

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:27539547%20AND%20SRC:MED&resulttype=core&format=json

21 March 2020

review article

1 reference

title

Targeted Covalent Inhibitors for Drug Design (English)

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:27539547%20AND%20SRC:MED&resulttype=core&format=json

21 March 2020

1

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:27539547%20AND%20SRC:MED&resulttype=core&format=json

21 March 2020

author name string

Thomas A Baillie

series ordinal

1

1 reference

7 September 2017

language of work or name

English

0 references

publication date

19 August 2016

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:27539547%20AND%20SRC:MED&resulttype=core&format=json

Angewandte Chemie International Edition

21 March 2020

published in

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:27539547%20AND%20SRC:MED&resulttype=core&format=json

21 March 2020

volume

55

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:27539547%20AND%20SRC:MED&resulttype=core&format=json

21 March 2020

issue

43

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:27539547%20AND%20SRC:MED&resulttype=core&format=json

21 March 2020

page(s)

13408-13421

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:27539547%20AND%20SRC:MED&resulttype=core&format=json

The resurgence of covalent drugs

21 March 2020

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How chemoproteomics can enable drug discovery and development

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The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP

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Structure-Based Design of a Potent, Selective, and Irreversible Inhibitor of the Catalytic Domain of the erbB Receptor Subfamily of Protein Tyrosine Kinases

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Keap calm, and carry on covalently

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Drug-protein adducts: an industry perspective on minimizing the potential for drug bioactivation in drug discovery and development

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Future of toxicology-metabolic activation and drug design: challenges and opportunities in chemical toxicology

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Epidermal growth factor receptor irreversible inhibitors: chemical exploration of the cysteine-trap portion.

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Chemistry of covalent inhibition of the gastric (H+, K+)-ATPase by proton pump inhibitors

21 January 2018

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Metabolic oxidative cleavage of thioesters: evidence for the formation of sulfenic acid intermediates in the bioactivation of the antithrombotic prodrugs ticlopidine and clopidogrel

21 January 2018

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Identification of the hepatic protein targets of reactive metabolites of acetaminophen in vivo in mice using two-dimensional gel electrophoresis and mass spectrometry

21 January 2018

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The contributions of Sidney D. Nelson to drug metabolism research

21 January 2018

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Reactive intermediates: molecular and MS-based approaches to assess the functional significance of chemical-protein adducts

21 January 2018

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Acylating drugs: redesigning natural covalent inhibitors

21 January 2018

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Activity-based proteome profiling of potential cellular targets of Orlistat--an FDA-approved drug with anti-tumor activities

21 January 2018

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Protein-reactive natural products

21 January 2018

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Specific, irreversible inactivation of the epidermal growth factor receptor and erbB2, by a new class of tyrosine kinase inhibitor

21 January 2018

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Targeted covalent drugs of the kinase family

21 January 2018

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The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy

21 January 2018

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Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides bearing additional solubilizing functions

21 January 2018

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21 January 2018

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Irreversible inhibitors of serine, cysteine, and threonine proteases

21 January 2018

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Selective irreversible inhibition of a protease by targeting a noncatalytic cysteine

21 January 2018

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Discovery of an irreversible HCV NS5B polymerase inhibitor

21 January 2018

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Identification of covalent active site inhibitors of dengue virus protease

21 January 2018

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Spiroepoxytriazoles Are Fumagillin-like Irreversible Inhibitors of MetAP2 with Potent Cellular Activity

21 January 2018

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Identification of a novel class of covalent modifiers of hemoglobin as potential antisickling agents

21 January 2018

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Rational Design of Fatty Acid Amide Hydrolase Inhibitors That Act by Covalently Bonding to Two Active Site Residues

21 January 2018

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Design, synthesis, and characterization of α-ketoheterocycles that additionally target the cytosolic port Cys269 of fatty acid amide hydrolase

21 January 2018

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Discovery of covalent inhibitors of glyceraldehyde-3-phosphate dehydrogenase, a target for the treatment of malaria

21 January 2018

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Potent activity of carfilzomib, a novel, irreversible inhibitor of the ubiquitin-proteasome pathway, against preclinical models of multiple myeloma

21 January 2018

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Irreversible kinase inhibitors gain traction

21 January 2018

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21 January 2018

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21 January 2018

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21 January 2018

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21 January 2018

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21 January 2018

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21 January 2018

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21 January 2018

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21 January 2018

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21 January 2018

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21 January 2018

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21 January 2018

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21 January 2018

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21 January 2018

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A proposed screening paradigm for discovery of covalent inhibitor drugs

21 January 2018

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21 January 2018

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Developing irreversible inhibitors of the protein kinase cysteinome

21 January 2018

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Irreversible protein kinase inhibitors

21 January 2018

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Proteasome inhibitors - molecular basis and current perspectives in multiple myeloma

21 January 2018

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The pharmacological landscape and therapeutic potential of serine hydrolases

21 January 2018

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21 January 2018

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An overview of recent dipeptidyl peptidase-IV inhibitors: linking their structure and physico-chemical properties with sar, pharmacokinetics and toxicity

21 January 2018

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Covalent EGFR inhibitor analysis reveals importance of reversible interactions to potency and mechanisms of drug resistance

21 January 2018

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Reversible targeting of noncatalytic cysteines with chemically tuned electrophiles

21 January 2018

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Electrophilic Fragment-Based Design of Reversible Covalent Kinase Inhibitors

21 January 2018

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Design of reversible, cysteine-targeted Michael acceptors guided by kinetic and computational analysis.

21 January 2018

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Targeting protein kinases with selective and semipromiscuous covalent inhibitors

21 January 2018

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A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles

21 January 2018

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Structure-based design and synthesis of covalent-reversible inhibitors to overcome drug resistance in EGFR.

21 January 2018

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Drug discovery considerations in the development of covalent inhibitors

21 January 2018

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The role of extrahepatic metabolism in the pharmacokinetics of the targeted covalent inhibitors afatinib, ibrutinib, and neratinib

21 January 2018

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Afatinib pharmacokinetics and metabolism after oral administration to healthy male volunteers.

21 January 2018

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Pharmacokinetics of oral neratinib during co-administration of ketoconazole in healthy subjects

21 January 2018

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Absorption, metabolism, and excretion of oral ¹⁴C radiolabeled ibrutinib: an open-label, phase I, single-dose study in healthy men.

21 January 2018

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Reversible covalent binding of neratinib to human serum albumin in vitro

21 January 2018

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Characterization of HKI-272 covalent binding to human serum albumin

21 January 2018

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Reversibility of covalent electrophile-protein adducts and chemical toxicity

21 January 2018

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Reversible interaction of a reactive intermediate derived from furazolidone with glutathione and protein

21 January 2018

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Benchmarking in vitro covalent binding burden as a tool to assess potential toxicity caused by nonspecific covalent binding of covalent drugs.

21 January 2018

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Kinetic glutathione chemoassay to quantify thiol reactivity of organic electrophiles--application to alpha,beta-unsaturated ketones, acrylates, and propiolates

21 January 2018

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A simple in vitro assay for assessing the reactivity of nitrile containing compounds.

21 January 2018

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A tag-free collisionally induced fragmentation approach to detect drug-adducted proteins by mass spectrometry.

21 January 2018

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A mass spectrometry platform for a streamlined investigation of proteasome integrity, posttranslational modifications, and inhibitor binding

21 January 2018

1 reference

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Label-Free Bottom-Up Proteomic Workflow for Simultaneously Assessing the Target Specificity of Covalent Drug Candidates and Their Off-Target Reactivity to Selected Proteins.

21 January 2018

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Physiochemical drug properties associated with in vivo toxicological outcomes

21 January 2018

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Scientists in the dark after French clinical trial proves fatal.

21 January 2018

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Relationship between daily dose of oral medications and idiosyncratic drug-induced liver injury: search for signals

21 January 2018

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Structural alert/reactive metabolite concept as applied in medicinal chemistry to mitigate the risk of idiosyncratic drug toxicity: a perspective based on the critical examination of trends in the top 200 drugs marketed in the United States

21 January 2018

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Systematic Study of the Glutathione (GSH) Reactivity of N-Arylacrylamides: 1. Effects of Aryl Substitution.

21 January 2018

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Promiscuity and selectivity in covalent enzyme inhibition: a systematic study of electrophilic fragments

21 January 2018

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Predicting the reactivity of nitrile-carrying compounds with cysteine: a combined computational and experimental study

21 January 2018

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Docking-based virtual screening of covalently binding ligands: an orthogonal lead discovery approach

21 January 2018

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A fragment-based method to discover irreversible covalent inhibitors of cysteine proteases

21 January 2018

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The T790M "gatekeeper" mutation in EGFR mediates resistance to low concentrations of an irreversible EGFR inhibitor

21 January 2018

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EGFR Mutations and Resistance to Irreversible Pyrimidine-Based EGFR Inhibitors

21 January 2018

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Covalent modification as a strategy to block protein-protein interactions with small-molecule drugs

21 January 2018

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Targeted inhibition of the Shroom3-Rho kinase protein-protein interaction circumvents Nogo66 to promote axon outgrowth.

21 January 2018

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The design of covalent allosteric drugs

21 January 2018

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Iminoboronates: A New Strategy for Reversible Protein Modification

21 January 2018

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21 January 2018

Identifiers

DOI

10.1002/ANIE.201601091

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:27539547%20AND%20SRC:MED&resulttype=core&format=json

21 March 2020

1 reference