A fragment-based method to discover irreversible covalent inhibitors of cysteine proteases (Q35175346)

6 August 2017

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

1 reference

6 August 2017

Stefan G Kathman

1

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6 August 2017

Ziyang Xu

series ordinal

2

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6 August 2017

Alexander V Statsyuk

series ordinal

3

1 reference

6 August 2017

language of work or name

English

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publication date

28 May 2014

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Journal of Medicinal Chemistry

6 August 2017

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6 August 2017

57

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6 August 2017

11

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6 August 2017

4969-4974

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USP8 is a novel target for overcoming gefitinib resistance in lung cancer

6 August 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4113264

Electrophilic Fragment-Based Design of Reversible Covalent Kinase Inhibitors

28 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4113264

Approaches for enhancing oral bioavailability of peptides and proteins

28 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4113264

Identification of Cys255 in HIF-1α as a novel site for development of covalent inhibitors of HIF-1α/ARNT PasB domain protein-protein interaction

28 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4113264

Fragment-based approaches in drug discovery and chemical biology

28 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4113264

Falcipains and other cysteine proteases of malaria parasites

28 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4113264

The resurgence of covalent drugs

28 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4113264

Novel peptidomimetics containing a vinyl ester moiety as highly potent and selective falcipain-2 inhibitors.

28 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4113264

Novel control of S phase of the cell cycle by ubiquitin-conjugating enzyme H7

28 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4113264

In vitro antiviral activity and single-dose pharmacokinetics in humans of a novel, orally bioavailable inhibitor of human rhinovirus 3C protease

28 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4113264

Tethering: fragment-based drug discovery

28 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4113264

A ‘Rule of Three’ for fragment-based lead discovery?

28 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4113264

Esters of methanesulfonic acid as irreversible inhibitors of acetylcholinesterase

28 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4113264

Irreversible inhibitors of serine, cysteine, and threonine proteases

28 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4113264

Site-directed ligand discovery

28 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4113264

Vinylogous amino acid esters: a new class of inactivators for thiol proteases

28 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4113264

Quantitative reactivity profiling predicts functional cysteines in proteomes

28 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4113264

Reactivity of functional groups on the protein surface: development of epoxide probes for protein labeling.

27 September 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4113264

Structure-activity relationships for inhibition of papain by peptide Michael acceptors

27 September 2018

1 reference

12 December 2020

Mechanism-based inhibition: deriving K(I) and k(inact) directly from time-dependent IC(50) values

1 reference

12 December 2020

Kinetic template-guided tethering of fragments

1 reference

12 December 2020

Relative rates of Michael reactions of 2'-(phenethyl)thiol with vinyl sulfones, vinyl sulfonate esters, and vinyl sulfonamides relevant to vinyl sulfonyl cysteine protease inhibitors

1 reference

12 December 2020

Identifiers

DOI

10.1021/JM500345Q

1 reference

6 August 2017

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6 August 2017

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