Awakening guardian angels: drugging the p53 pathway (Q35014385)

5 August 2017

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title

Awakening guardian angels: drugging the p53 pathway (English)

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5 August 2017

4

Alan R Fersht

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5 August 2017

Christopher J Brown

1

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5 August 2017

Sonia Lain

series ordinal

2

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5 August 2017

Chandra S Verma

series ordinal

3

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5 August 2017

David P Lane

series ordinal

5

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5 August 2017

language of work or name

English

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publication date

1 December 2009

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5 August 2017

Nature Reviews Cancer

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5 August 2017

9

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5 August 2017

12

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5 August 2017

862-873

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https://scigraph.springernature.com/pub.10.1038/nrc2763

5 August 2017

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Small molecule RITA binds to p53, blocks p53-HDM-2 interaction and activates p53 function in tumors.

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A panel of isogenic human cancer cells suggests a therapeutic approach for cancers with inactivated p53

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31 March 2020

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31 March 2020

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Flexibility: the key to p53 function?

31 March 2020

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31 March 2020

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Dissecting cellular processes using small molecules: identification of colchicine-like, taxol-like and other small molecules that perturb mitosis

31 March 2020

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PRIMA-1 reactivates mutant p53 by covalent binding to the core domain

31 March 2020

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Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue in the central conserved region

31 March 2020

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Targeting the DNA repair defect in BRCA mutant cells as a therapeutic strategy

31 March 2020

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Amplification of a gene encoding a p53-associated protein in human sarcomas

31 March 2020

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The MDM2 gene amplification database

31 March 2020

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Tumor suppression and normal aging in mice with constitutively high p53 activity

31 March 2020

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Small-molecule MDM2 antagonists reveal aberrant p53 signaling in cancer: implications for therapy

31 March 2020

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

31 March 2020

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Structure-based design of potent non-peptide MDM2 inhibitors

31 March 2020

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

31 March 2020

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Benzodiazepinedione inhibitors of the Hdm2:p53 complex suppress human tumor cell proliferation in vitro and sensitize tumors to doxorubicin in vivo

31 March 2020

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31 March 2020

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Enhanced pharmacokinetic properties of 1,4-benzodiazepine-2,5-dione antagonists of the HDM2-p53 protein-protein interaction through structure-based drug design

31 March 2020

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Small-molecule inhibitors of the MDM2-p53 protein-protein interaction to reactivate p53 function: a novel approach for cancer therapy

31 March 2020

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Rescue of embryonic lethality in Mdm4-null mice by loss of Trp53 suggests a nonoverlapping pathway with MDM2 to regulate p53

31 March 2020

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Rescue of early embryonic lethality in mdm2-deficient mice by deletion of p53

31 March 2020

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31 March 2020

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Mdmx stabilizes p53 and Mdm2 via two distinct mechanisms

31 March 2020

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Structure of the MDM2/MDMX RING domain heterodimer reveals dimerization is required for their ubiquitylation in trans

31 March 2020

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MDM2 interacts with MDMX through their RING finger domains

31 March 2020

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Stabilization of the MDM2 oncoprotein by interaction with the structurally related MDMX protein

31 March 2020

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HdmX stimulates Hdm2-mediated ubiquitination and degradation of p53.

31 March 2020

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Mutual dependence of MDM2 and MDMX in their functional inactivation of p53

31 March 2020

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MDM2 promotes ubiquitination and degradation of MDMX

31 March 2020

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DNA damage-induced MDMX degradation is mediated by MDM2.

31 March 2020

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Hdmx protein stability is regulated by the ubiquitin ligase activity of Mdm2.

31 March 2020

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Targeting Mdm2 and Mdmx in cancer therapy: better living through medicinal chemistry?

31 March 2020

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Significance of HDMX-S (or MDM4) mRNA splice variant overexpression and HDMX gene amplification on primary soft tissue sarcoma prognosis.

31 March 2020

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Comparative study of the p53-mdm2 and p53-MDMX interfaces

31 March 2020

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Structural basis for high-affinity peptide inhibition of p53 interactions with MDM2 and MDMX

31 March 2020

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Reactivation of the p53 tumor suppressor pathway by a stapled p53 peptide

31 March 2020

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Activation of p53 by scaffold-stabilised expression of Mdm2-binding peptides: visualisation of reporter gene induction at the single-cell level

31 March 2020

1 reference

Small molecule inhibitors of HDM2 ubiquitin ligase activity stabilize and activate p53 in cells

31 March 2020

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An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors

31 March 2020

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Suppression of the deubiquitinating enzyme USP5 causes the accumulation of unanchored polyubiquitin and the activation of p53

31 March 2020

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Cancer. p53, guardian of the genome

31 March 2020

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High-throughput measurement of the Tp53 response to anticancer drugs and random compounds using a stably integrated Tp53-responsive luciferase reporter

31 March 2020

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Pilot screening programme for small molecule activators of p53.

31 March 2020

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Small molecules that reactivate p53 in renal cell carcinoma reveal a NF-kappaB-dependent mechanism of p53 suppression in tumors

31 March 2020

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Targeting lysosomal degradation induces p53-dependent cell death and prevents cancer in mouse models of lymphomagenesis

31 March 2020

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Mycophenolic acid activation of p53 requires ribosomal proteins L5 and L11

31 March 2020

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A reversible, p53-dependent G0/G1 cell cycle arrest induced by ribonucleotide depletion in the absence of detectable DNA damage.

31 March 2020

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RNA synthesis block by 5, 6-dichloro-1-beta-D-ribofuranosylbenzimidazole (DRB) triggers p53-dependent apoptosis in human colon carcinoma cells.

31 March 2020

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Inhibition of RNA polymerase II as a trigger for the p53 response

31 March 2020

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Regulation of HDM2 activity by the ribosomal protein L11

31 March 2020

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Cancer-associated mutations in the MDM2 zinc finger domain disrupt ribosomal protein interaction and attenuate MDM2-induced p53 degradation

31 March 2020

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Disruption of the nucleolus mediates stabilization of p53 in response to DNA damage and other stresses

31 March 2020

1 reference

Comparison between single-dose and divided-dose administration of dactinomycin and doxorubicin for patients with Wilms' tumor: a report from the National Wilms' Tumor Study Group

31 March 2020

1 reference

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

31 March 2020

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Small-molecule activation of p53 blocks hypoxia-inducible factor 1alpha and vascular endothelial growth factor expression in vivo and leads to tumor cell apoptosis in normoxia and hypoxia

31 March 2020

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Selective toxicity of the tricyclic thiophene NSC 652287 in renal carcinoma cell lines: differential accumulation and metabolism

31 March 2020

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DNA protein cross-links produced by NSC 652287, a novel thiophene derivative active against human renal cancer cells.

31 March 2020

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MDM2-dependent downregulation of p21 and hnRNP K provides a switch between apoptosis and growth arrest induced by pharmacologically activated p53

31 March 2020

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Ablation of key oncogenic pathways by RITA-reactivated p53 is required for efficient apoptosis

31 March 2020

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Negative control of p53 by Sir2alpha promotes cell survival under stress

31 March 2020

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hSIR2(SIRT1) functions as an NAD-dependent p53 deacetylase

31 March 2020

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Human SIR2 deacetylates p53 and antagonizes PML/p53-induced cellular senescence

31 March 2020

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Identification of nuclear export inhibitors with potent anticancer activity in vivo

31 March 2020

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Activation of p53 by MDM2 antagonists can protect proliferating cells from mitotic inhibitors

31 March 2020

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Modelling Myc inhibition as a cancer therapy

31 March 2020

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Structure-based design of molecular cancer therapeutics

31 March 2020

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Discovering novel ligands for macromolecules using X-ray crystallographic screening

31 March 2020

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Increased radioresistance and accelerated B cell lymphomas in mice with Mdmx mutations that prevent modifications by DNA-damage-activated kinases

31 March 2020

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MDM2 inhibitors for cancer therapy

31 March 2020

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Activity of MDM2, a ubiquitin ligase, toward p53 or itself is dependent on the RING finger domain of the ligase

31 March 2020

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Mdm2 is a RING finger-dependent ubiquitin protein ligase for itself and p53

31 March 2020

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p53 and human cancer: the first ten thousand mutations.

31 March 2020

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12 December 2020

Oncogenic mutations of the p53 tumor suppressor: the demons of the guardian of the genome.

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12 December 2020

Family feud in chemosensitvity: p73 and mutant p53.

1 reference

12 December 2020

Control of p53 ubiquitination and nuclear export by MDM2 and ARF.

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12 December 2020

p53 accumulates but is functionally impaired when DNA synthesis is blocked

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12 December 2020

Recombinant adenovirus expressing wild-type p53 is antiangiogenic: a proposed mechanism for bystander effect

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12 December 2020

p14ARF silencing by promoter hypermethylation mediates abnormal intracellular localization of MDM2.

1 reference

12 December 2020

Tumor-suppressing gene therapy

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12 December 2020

The ability of human papillomavirus E6 proteins to target p53 for degradation in vivo correlates with their ability to abrogate actinomycin D-induced growth arrest.

1 reference

12 December 2020

Cancer-specific viruses and the development of ONYX-015

1 reference

12 December 2020

A new anti-p53 monoclonal antibody, previously reported to be directed against the large T antigen of simian virus 40.

1 reference

12 December 2020

Aberrant expression of HDMX proteins in tumor cells correlates with wild-type p53.

1 reference

12 December 2020

Amplification and overexpression of the MDM4 (MDMX) gene from 1q32 in a subset of malignant gliomas without TP53 mutation or MDM2 amplification.

1 reference

12 December 2020

Identifiers

DOI

10.1038/NRC2763

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5 August 2017

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