Drug discovery for a new generation of covalent drugs (Q38011256)

26 August 2017

title

Drug discovery for a new generation of covalent drugs (English)

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26 August 2017

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Amit S Kalgutkar

1

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26 August 2017

Deepak K Dalvie

series ordinal

2

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26 August 2017

language of work or name

English

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publication date

19 May 2012

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Expert Opinion on Drug Discovery

26 August 2017

published in

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26 August 2017

volume

7

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26 August 2017

issue

7

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26 August 2017

page(s)

561-581

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Covalent modifiers: an orthogonal approach to drug design

26 August 2017

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Application of the Hard and Soft, Acids and Bases (HSAB) theory to toxicant--target interactions

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Application of structure-activity relationships to investigate the molecular mechanisms of hepatocyte toxicity and electrophilic reactivity of alpha,beta-unsaturated aldehydes

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Prediction of Michael-Type Acceptor Reactivity toward Glutathione

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Structural bioinformatics-based design of selective, irreversible kinase inhibitors

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Targeted covalent drugs of the kinase family

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beta-Lactam allergenic determinants: fine structural recognition of a cross-reacting determinant on benzylpenicillin and cephalothin

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Immune-mediated adverse drug reactions

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Kinetic and structural studies on the interaction of cholinesterases with the anti-Alzheimer drug rivastigmine

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Discovery and Characterization of a Highly Selective FAAH Inhibitor that Reduces Inflammatory Pain

21 January 2018

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Benzothiophene piperazine and piperidine urea inhibitors of fatty acid amide hydrolase (FAAH)

21 January 2018

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Structure-guided inhibitor design for human FAAH by interspecies active site conversion

21 January 2018

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Quantitative reactivity profiling predicts functional cysteines in proteomes

21 January 2018

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Discovery and development of VX-950, a novel, covalent, and reversible inhibitor of hepatitis C virus NS3.4A serine protease

21 January 2018

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Efficacy of boceprevir, an NS3 protease inhibitor, in combination with peginterferon alfa-2b and ribavirin in treatment-naive patients with genotype 1 hepatitis C infection (SPRINT-1): an open-label, randomised, multicentre phase 2 trial

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Development of nitrile-based peptidic inhibitors of cysteine cathepsins

21 January 2018

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The pH dependencies of individual rate constants in papain-catalyzed reactions.

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Novel and potent cyclic cyanamide-based cathepsin K inhibitors

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Novel purine nitrile derived inhibitors of the cysteine protease cathepsin K.

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The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.

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The consequences of lysosomotropism on the design of selective cathepsin K inhibitors

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Nitrile-containing pharmaceuticals: efficacious roles of the nitrile pharmacophore

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Vildagliptin: a new oral treatment for type 2 diabetes mellitus

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Identification of a potent and selective non-basic cathepsin K inhibitor

21 January 2018

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Involvement of DPP-IV catalytic residues in enzyme-saxagliptin complex formation

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Reversible targeting of noncatalytic cysteines with chemically tuned electrophiles

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Structure-activity relationships for thiol reactivity and rat or human hepatocyte toxicity induced by substituted p-benzoquinone compounds

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Chemical reactivity of methoxy 4-o-aryl quinolines: identification of glutathione displacement products in vitro and in vivo

21 January 2018

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Intrinsic electrophilicity of the 4-methylsulfonyl-2-pyridone scaffold in glucokinase activators: Role of glutathione-S-transferases and in vivo quantitation of a glutathione conjugate in rats

21 January 2018

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Non-enzymatic glutathione reactivity and in vitro toxicity: a non-animal approach to skin sensitization

21 January 2018

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Structure-activity relationships for reactivity of carbonyl-containing compounds with glutathione

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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ALARM NMR: a rapid and robust experimental method to detect reactive false positives in biochemical screens

21 January 2018

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Toxicological evaluation of thiol-reactive compounds identified using a la assay to detect reactive molecules by nuclear magnetic resonance

21 January 2018

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Structure of the C-terminal domain of human La protein reveals a novel RNA recognition motif coupled to a helical nuclear retention element

21 January 2018

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A novel class of highly potent irreversible hepatitis C virus NS5B polymerase inhibitors

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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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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Activity-based protein profiling: from enzyme chemistry to proteomic chemistry

21 January 2018

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Tandem orthogonal proteolysis-activity-based protein profiling (TOP-ABPP)--a general method for mapping sites of probe modification in proteomes

21 January 2018

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Discovering potent and selective reversible inhibitors of enzymes in complex proteomes

21 January 2018

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Novel mechanistic class of fatty acid amide hydrolase inhibitors with remarkable selectivity

21 January 2018

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Click chemistry and bioorthogonal reactions: unprecedented selectivity in the labeling of biological molecules.

21 January 2018

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Profiling enzyme activities in vivo using click chemistry methods

21 January 2018

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Mechanism of carbamate inactivation of FAAH: implications for the design of covalent inhibitors and in vivo functional probes for enzymes

21 January 2018

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https://api.crossref.org/works/10.1517%2F17460441.2012.688744

Examination of Michael addition reactivity towards glutathione by transition-state calculations

21 January 2018

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https://api.crossref.org/works/10.1517%2F17460441.2012.688744

Redox ranking of inducers of a cancer-protective enzyme via the energy of their highest occupied molecular orbital

21 January 2018

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https://api.crossref.org/works/10.1517%2F17460441.2012.688744

The role of metabolic activation in drug-induced hepatotoxicity

21 January 2018

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https://api.crossref.org/works/10.1517%2F17460441.2012.688744

Concordance of the toxicity of pharmaceuticals in humans and in animals

21 January 2018

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https://api.crossref.org/works/10.1517%2F17460441.2012.688744

Structure and stereochemistry of the active metabolite of clopidogrel

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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Metabolism and disposition of the thienopyridine antiplatelet drugs ticlopidine, clopidogrel, and prasugrel in humans

21 January 2018

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Mechanism-based inactivation of cytochrome P450 3A4 by lapatinib

21 January 2018

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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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Multicenter, randomized, phase II trial of CI-1033, an irreversible pan-ERBB inhibitor, for previously treated advanced non small-cell lung cancer

21 January 2018

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Antitumor activity and pharmacokinetic properties of PF-00299804, a second-generation irreversible pan-erbB receptor tyrosine kinase inhibitor

21 January 2018

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Cutaneous lesions in the rat following administration of an irreversible inhibitor of erbB receptors, including the epidermal growth factor receptor

21 January 2018

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10.1517/17460441.2012.688744

21 January 2018

Identifiers

DOI

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26 August 2017

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