Benzimidazole-2-one: a novel anchoring principle for antagonizing p53-Mdm2 (Q37026970)

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7 February 2020

title

Benzimidazole-2-one: a novel anchoring principle for antagonizing p53-Mdm2 (English)

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7 February 2020

1

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7 February 2020

Alex Domling

6

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7 February 2020

author name string

Haiping Cao

2

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7 February 2020

Siglinde Wolf

3

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7 February 2020

Miguel S Camacho-Horvitz

4

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7 February 2020

Tad A Holak

5

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7 February 2020

language of work or name

English

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publication date

20 June 2012

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Bioorganic & Medicinal Chemistry

7 February 2020

published in

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7 February 2020

volume

21

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7 February 2020

issue

14

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7 February 2020

page(s)

3982-3995

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The p53-MDM2/MDMX axis - A chemotype perspective

7 February 2020

cites work

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Enabling large-scale design, synthesis and validation of small molecule protein-protein antagonists

29 September 2017

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Rational approaches to improving selectivity in drug design

29 September 2017

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Exhaustive Fluorine Scanning toward Potent p53-Mdm2 Antagonists

29 September 2017

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The Structure‐Based Design of Mdm2/Mdmx–p53 Inhibitors Gets Serious

29 September 2017

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Systematic analysis of helical protein interfaces reveals targets for synthetic inhibitors

29 September 2017

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29 September 2017

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29 September 2017

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New substructure filters for removal of pan assay interference compounds (PAINS) from screening libraries and for their exclusion in bioassays

29 September 2017

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Targeting the cancer kinome through polypharmacology

29 September 2017

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Discovery and optimization of chromenotriazolopyrimidines as potent inhibitors of the mouse double minute 2-tumor protein 53 protein-protein interaction

29 September 2017

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Rapid and efficient hydrophilicity tuning of p53/mdm2 antagonists

29 September 2017

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Synthesis, molecular docking and biological evaluation as HDAC inhibitors of cyclopeptide mimetics by a tandem three-component reaction and intramolecular [3 2] cycloaddition.

29 September 2017

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Structure of the human Mdmx protein bound to the p53 tumor suppressor transactivation domain

29 September 2017

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Small molecular weight protein-protein interaction antagonists: an insurmountable challenge?

29 September 2017

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Amino acid derivatives as histone deacetylase inhibitors

29 September 2017

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Molecular basis for the inhibition of p53 by Mdmx

29 September 2017

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Protein-protein interactions as targets for small molecule drug discovery

29 September 2017

1 reference

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Structure-based design of spiro-oxindoles as potent, specific small-molecule inhibitors of the MDM2-p53 interaction.

29 September 2017

1 reference

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Monitoring the effects of antagonists on protein-protein interactions with NMR spectroscopy

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3716288

Discovery and cocrystal structure of benzodiazepinedione HDM2 antagonists that activate p53 in cells.

29 September 2017

1 reference

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In vivo activation of the p53 pathway by small-molecule antagonists of MDM2

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3716288

Chalcone derivatives antagonize interactions between the human oncoprotein MDM2 and p53.

29 September 2017

1 reference

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Discovering high-affinity ligands for proteins: SAR by NMR

29 September 2017

1 reference

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Structure of the MDM2 oncoprotein bound to the p53 tumor suppressor transactivation domain

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3716288

Improved sensitivity of HSQC spectra of exchanging protons at short interscan delays using a new fast HSQC (FHSQC) detection scheme that avoids water saturation

29 September 2017

1 reference

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Robust generation of lead compounds for protein-protein interactions by computational and MCR chemistry: p53/Hdm2 antagonists.

29 September 2017

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1,4-Thienodiazepine-2,5-diones via MCR (I): synthesis, virtual space and p53-Mdm2 activity.

27 June 2018

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Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pa

27 June 2018

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Fragment-guided approach to incorporating structural information into a CoMFA study: BACE-1 as an example

4 September 2018

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Structures of low molecular weight inhibitors bound to MDMX and MDM2 reveal new approaches for p53-MDMX/MDM2 antagonist drug discovery.

4 September 2018

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QSAR study of Akt/protein kinase B (PKB) inhibitors using support vector machine

4 September 2018

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Robust NMR screening for lead compounds using tryptophan-containing proteins.

4 September 2018

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High affinity interaction of the p53 peptide-analogue with human Mdm2 and Mdmx

4 September 2018

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NMR screening for lead compounds using tryptophan-mutated proteins

4 September 2018

1 reference

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Acid-free, aminoborane-mediated Ugi-type reaction leading to general utilization of secondary amines

4 September 2018

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NMR indicates that the small molecule RITA does not block p53-MDM2 binding in vitro

4 September 2018

1 reference

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Adamantane 11-beta-HSD-1 inhibitors: Application of an isocyanide multicomponent reaction

4 September 2018

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12 December 2020

Catalytic three-component Ugi reaction

1 reference

12 December 2020

Charge distribution from a simple molecular orbital type calculation and non-bonding interaction terms in the force field MAB

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12 December 2020

NMR structure of a complex between MDM2 and a small molecule inhibitor

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12 December 2020

Cascade coupling/cyclization process to N-substituted 1,3-dihydrobenzimidazol-2-ones

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12 December 2020

Application of NMR in structural proteomics: screening for proteins amenable to structural analysis

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12 December 2020

Discovery of potent antagonists of the interaction between human double minute 2 and tumor suppressor p53

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12 December 2020

An NMR-based antagonist induced dissociation assay for targeting the ligand-protein and protein-protein interactions in competition binding experiments

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12 December 2020

10.1016/J.BMC.2012.06.020

Identifiers

DOI

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:22789708 AND SRC:MED&resulttype=core&format=json

7 February 2020

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7 February 2020

PubMed publication ID

22789708

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:22789708 AND SRC:MED&resulttype=core&format=json