Design of reversible, cysteine-targeted Michael acceptors guided by kinetic and computational analysis. (Q34160457)

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:25153195%20AND%20SRC:MED&resulttype=core&format=json

13 March 2020

title

Design of reversible, cysteine-targeted Michael acceptors guided by kinetic and computational analysis (English)

1 reference

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13 March 2020

author name string

Shyam Krishnan

1

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13 March 2020

Rand M Miller

2

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13 March 2020

Boxue Tian

3

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13 March 2020

Jack Taunton

6

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13 March 2020

language of work or name

English

0 references

publication date

2 September 2014

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Journal of the American Chemical Society

13 March 2020

published in

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13 March 2020

volume

136

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13 March 2020

issue

36

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13 March 2020

page(s)

12624-12630

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

13 March 2020

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1 reference

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

5 July 2018

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5 July 2018

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Targeting BTK with ibrutinib in relapsed chronic lymphocytic leukemia

5 July 2018

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Electrophilic Fragment-Based Design of Reversible Covalent Kinase Inhibitors

5 July 2018

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Developing irreversible inhibitors of the protein kinase cysteinome

5 July 2018

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Reversible Michael additions: covalent inhibitors and prodrugs

5 July 2018

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Reversible targeting of noncatalytic cysteines with chemically tuned electrophiles

5 July 2018

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The resurgence of covalent drugs

5 July 2018

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Managing the challenge of chemically reactive metabolites in drug development.

5 July 2018

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Identification of diaryl ether-based ligands for estrogen-related receptor α as potential antidiabetic agents

5 July 2018

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Nitrile-containing pharmaceuticals: efficacious roles of the nitrile pharmacophore

5 July 2018

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Development of nitrile-based peptidic inhibitors of cysteine cathepsins

5 July 2018

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Reversibility of covalent electrophile-protein adducts and chemical toxicity

5 July 2018

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Covalent modifiers: an orthogonal approach to drug design

5 July 2018

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Beyond picomolar affinities: quantitative aspects of noncovalent and covalent binding of drugs to proteins

5 July 2018

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

5 July 2018

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

5 July 2018

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Protein damage by reactive electrophiles: targets and consequences

5 July 2018

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Idiosyncratic drug reactions: past, present, and future

5 July 2018

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Applying mechanisms of chemical toxicity to predict drug safety

5 July 2018

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Drug-target residence time and its implications for lead optimization

5 July 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

5 July 2018

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

5 July 2018

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A proton-pump inhibitor expedition: the case histories of omeprazole and esomeprazole

5 July 2018

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Structure and stereochemistry of the active metabolite of clopidogrel

5 July 2018

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SAR and mode of action of novel non-nucleoside inhibitors of hepatitis C NS5b RNA polymerase

5 July 2018

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Studies on the reactivity of CDDO, a promising new chemopreventive and chemotherapeutic agent: implications for a molecular mechanism of action

28 October 2018

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First-principle predictions of absolute pKa's of organic acids in dimethyl sulfoxide solution

28 October 2018

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The pKa Value and Accessibility of Cysteine Residues Are Key Determinants for Protein Substrate Discrimination by Glutaredoxin

28 October 2018

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28 October 2018

Identifiers

DOI

10.1021/JA505194W

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:25153195%20AND%20SRC:MED&resulttype=core&format=json

13 March 2020

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:25153195%20AND%20SRC:MED&resulttype=core&format=json

13 March 2020

PubMed publication ID

25153195

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:25153195%20AND%20SRC:MED&resulttype=core&format=json