Wild type p53 reactivation: From lab bench to clinic

A Targeting Modality for Destruction of RNA Polymerase I that Possesses Anticancer Activity

(2014) Karita Peltonen et al.   CANCER CELL

ROS-dependent activation of JNK converts p53 into an efficient inhibitor of oncogenes leading to robust apoptosis

(2014) Y Shi et al.   CELL DEATH AND DIFFERENTIATION

Targeting MDM2-p53 Interaction for Cancer Therapy: Are We There Yet?

(2014) S. Nag et al.   CURRENT MEDICINAL CHEMISTRY

Activation of a promyelocytic leukemia–tumor protein 53 axis underlies acute promyelocytic leukemia cure

(2014) Julien Ablain et al.   NATURE MEDICINE

Drugging the p53 pathway: understanding the route to clinical efficacy

(2014) Kian Hoe Khoo et al.   NATURE REVIEWS DRUG DISCOVERY

Non-Cell-Autonomous Tumor Suppression by p53

(2013) Amaia Lujambio et al.   CELL

Dual Targeting of Wild-Type and Mutant p53 by Small Molecule RITA Results in the Inhibition of N-Myc and Key Survival Oncogenes and Kills Neuroblastoma Cells In Vivo and In Vitro

(2013) M. Burmakin et al.   CLINICAL CANCER RESEARCH

Global genomic profiling reveals an extensive p53-regulated autophagy program contributing to key p53 responses

(2013) D. Kenzelmann Broz et al.   GENES & DEVELOPMENT

Autophagy suppresses progression of K-ras-induced lung tumors to oncocytomas and maintains lipid homeostasis

(2013) J. Y. Guo et al.   GENES & DEVELOPMENT

Discovery of RG7388, a Potent and Selective p53–MDM2 Inhibitor in Clinical Development

(2013) Qingjie Ding et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Potent Small-Molecule Inhibitor of the MDM2–p53 Interaction (MI-888) Achieved Complete and Durable Tumor Regression in Mice

(2013) Yujun Zhao et al.   JOURNAL OF MEDICINAL CHEMISTRY

p53 status determines the role of autophagy in pancreatic tumour development

(2013) Mathias T. Rosenfeldt et al.   NATURE

Mutational heterogeneity in cancer and the search for new cancer-associated genes

(2013) Michael S. Lawrence et al.   NATURE

Stapled α−helical peptide drug development: A potent dual inhibitor of MDM2 and MDMX for p53-dependent cancer therapy

(2013) Yong S. Chang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Identification of a second Nutlin-3 responsive interaction site in the N-terminal domain of MDM2 using hydrogen/deuterium exchange mass spectrometry

(2013) Lenka Hernychova et al.   PROTEOMICS

p53 increases MHC class I expression by upregulating the endoplasmic reticulum aminopeptidase ERAP1

(2013) Bei Wang et al.   Nature Communications

Autophagy Opposes p53-Mediated Tumor Barrier to Facilitate Tumorigenesis in a Model of PALB2-Associated Hereditary Breast Cancer

(2013) Y. Huo et al.   Cancer Discovery

p53 DNA Binding Cooperativity Is Essential for Apoptosis and Tumor Suppression In Vivo

(2013) Oleg Timofeev et al.   Cell Reports

Facilitates Chromatin Transcription Complex Is an “Accelerator” of Tumor Transformation and Potential Marker and Target of Aggressive Cancers

(2013) Henry Garcia et al.   Cell Reports

p53 Efficiently Suppresses Tumor Development in the Complete Absence of Its Cell-Cycle Inhibitory and Proapoptotic Effectors p21, Puma, and Noxa

(2013) Liz J. Valente et al.   Cell Reports

Inhibition of RNA Polymerase I as a Therapeutic Strategy to Promote Cancer-Specific Activation of p53

(2012) Megan J. Bywater et al.   CANCER CELL

p53-Mediated Senescence Impairs the Apoptotic Response to Chemotherapy and Clinical Outcome in Breast Cancer

(2012) James G. Jackson et al.   CANCER CELL

Loss of p53 in Enterocytes Generates an Inflammatory Microenvironment Enabling Invasion and Lymph Node Metastasis of Carcinogen-Induced Colorectal Tumors

(2012) Sarah Schwitalla et al.   CANCER CELL

Tumor Suppression in the Absence of p53-Mediated Cell-Cycle Arrest, Apoptosis, and Senescence

(2012) Tongyuan Li et al.   CELL

Insights into p53 transcriptional function via genome-wide chromatin occupancy and gene expression analysis

(2012) F Nikulenkov et al.   CELL DEATH AND DIFFERENTIATION

Molecular Pathways: Targeting Mdm2 and Mdm4 in Cancer Therapy

(2012) Q. Li et al.   CLINICAL CANCER RESEARCH

A small molecule Inauhzin inhibits SIRT1 activity and suppresses tumour growth through activation of p53

(2012) Qi Zhang et al.   EMBO Molecular Medicine

An iTRAQ Proteomics Screen Reveals the Effects of the MDM2 Binding Ligand Nutlin-3 on Cellular Proteostasis

(2012) Judith Nicholson et al.   JOURNAL OF PROTEOME RESEARCH

Effect of the MDM2 antagonist RG7112 on the P53 pathway in patients with MDM2-amplified, well-differentiated or dedifferentiated liposarcoma: an exploratory proof-of-mechanism study

(2012) Isabelle Ray-Coquard et al.   LANCET ONCOLOGY

ATM and MET kinases are synthetic lethal with nongenotoxic activation of p53

(2012) Kelly D Sullivan et al.   Nature Chemical Biology

MDM4 is a key therapeutic target in cutaneous melanoma

(2012) Agnieszka Gembarska et al.   NATURE MEDICINE

Protein–protein interaction inhibitors get into the groove

(2012) Asher Mullard   NATURE REVIEWS DRUG DISCOVERY

Activation of the p53 pathway by small-molecule-induced MDM2 and MDMX dimerization

(2012) B. Graves et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Lithocholic acid is an endogenous inhibitor of MDM4 and MDM2

(2012) S. M. Vogel et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Human NK Cells Are Alerted to Induction of p53 in Cancer Cells by Upregulation of the NKG2D Ligands ULBP1 and ULBP2

(2011) S. Textor et al.   CANCER RESEARCH

Distinct p53 Transcriptional Programs Dictate Acute DNA-Damage Responses and Tumor Suppression

(2011) Colleen A. Brady et al.   CELL

Elevated MDM2 boosts the apoptotic activity of p53-MDM2 binding inhibitors by facilitating MDMX degradation

(2011) Mingxuan Xia et al.   CELL CYCLE

p53-dependent inhibition of TrxR1 contributes to the tumor-specific induction of apoptosis by RITA

(2011) Elisabeth Hedström et al.   CELL CYCLE

PRIMA-1Met/APR-246 induces wild-type p53-dependent suppression of malignant melanoma tumor growth in 3D culture and in vivo

(2011) Wenjie Bao et al.   CELL CYCLE

Pharmacological activation of p53 triggers anticancer innate immune response through induction of ULBP2

(2011) Hai Li et al.   CELL CYCLE

Mechanism-specific signatures for small-molecule p53 activators

(2011) Ingeborg M.M. van Leeuwen et al.   CELL CYCLE

Abrogation of Wip1 expression by RITA-activated p53 potentiates apoptosis induction via activation of ATM and inhibition of HdmX

(2011) C Spinnler et al.   CELL DEATH AND DIFFERENTIATION

A Phase I First-in-Human Pharmacokinetic and Pharmacodynamic Study of Serdemetan in Patients with Advanced Solid Tumors

(2011) J. Tabernero et al.   CLINICAL CANCER RESEARCH

The stress kinase MKK7 couples oncogenic stress to p53 stability and tumor suppression

(2011) Daniel Schramek et al.   NATURE GENETICS

Acquisition of p53 mutations in response to the non-genotoxic p53 activator Nutlin-3

(2011) M H Aziz et al.   ONCOGENE

Full p53 transcriptional activation potential is dispensable for tumor suppression in diverse lineages

(2011) D. Jiang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Curaxins: Anticancer Compounds That Simultaneously Suppress NF- B and Activate p53 by Targeting FACT

(2011) A. V. Gasparian et al.   Science Translational Medicine

Adaptation of cancer cells from different entities to the MDM2 inhibitor nutlin-3 results in the emergence of p53-mutated multi-drug-resistant cancer cells

(2011) M Michaelis et al.   Cell Death & Disease

Discovery of Mdm2-MdmX E3 Ligase Inhibitors Using a Cell-Based Ubiquitination Assay

(2011) A. G. Herman et al.   Cancer Discovery

Rescue of p53 Function by Small-Molecule RITA in Cervical Carcinoma by Blocking E6-Mediated Degradation

(2010) C. Y. Zhao et al.   CANCER RESEARCH

A Large Intergenic Noncoding RNA Induced by p53 Mediates Global Gene Repression in the p53 Response

(2010) Maite Huarte et al.   CELL

Activation of a unique p53-dependent DNA damage response

(2010) Jun Yang et al.   CELL CYCLE

Specific activation of the p53 pathway by low dose actinomycin D: A new route to p53 based cyclotherapy

(2010) Meng Ling Choong et al.   CELL CYCLE

Rescue of the apoptotic-inducing function of mutant p53 by small molecule RITA

(2010) Carolyn Y. Zhao et al.   CELL CYCLE

Combination of nutlin-3 and VX-680 selectively targets p53 mutant cells with reversible effects on cells expressing wild-type p53

(2010) C F Cheok et al.   CELL DEATH AND DIFFERENTIATION

Identification and Characterization of the First Small Molecule Inhibitor of MDMX

(2010) Damon Reed et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

SCH529074, a Small Molecule Activator of Mutant p53, Which Binds p53 DNA Binding Domain (DBD), Restores Growth-suppressive Function to Mutant p53 and Interrupts HDM2-mediated Ubiquitination of Wild Type p53

(2010) Mark Demma et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Novel Pyrrolopyrimidine-Based α-Helix Mimetics: Cell-Permeable Inhibitors of Protein−Protein Interactions

(2010) Ji Hoon Lee et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

The Novel Tryptamine Derivative JNJ-26854165 Induces Wild-Type p53- and E2F1-Mediated Apoptosis in Acute Myeloid and Lymphoid Leukemias

(2010) K. Kojima et al.   MOLECULAR CANCER THERAPEUTICS

A Small-Molecule Inhibitor of MDMX Activates p53 and Induces Apoptosis

(2010) H. Wang et al.   MOLECULAR CANCER THERAPEUTICS

Cellular Metabolic Stress: Considering How Cells Respond to Nutrient Excess

(2010) Kathryn E. Wellen et al.   MOLECULAR CELL

Selective activation of p53-mediated tumour suppression in high-grade tumours

(2010) Melissa R. Junttila et al.   NATURE

Stage-specific sensitivity to p53 restoration during lung cancer progression

(2010) David M. Feldser et al.   NATURE

Role of Mdm4 in drug sensitivity of breast cancer cells

(2010) S Lam et al.   ONCOGENE

Identification of Novel p53 Pathway Activating Small-Molecule Compounds Reveals Unexpected Similarities with Known Therapeutic Agents

(2010) Karita Peltonen et al.   PLoS One

Mitochondrial metabolism and ROS generation are essential for Kras-mediated tumorigenicity

(2010) F. Weinberg et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The Control of the Metabolic Switch in Cancers by Oncogenes and Tumor Suppressor Genes

(2010) A. J. Levine et al.   SCIENCE

p53 post-translational modification: deregulated in tumorigenesis

(2010) Chao Dai et al.   TRENDS IN MOLECULAR MEDICINE

Ablation of Key Oncogenic Pathways by RITA-Reactivated p53 Is Required for Efficient Apoptosis

(2009) Vera V. Grinkevich et al.   CANCER CELL

MDM2-Dependent Downregulation of p21 and hnRNP K Provides a Switch between Apoptosis and Growth Arrest Induced by Pharmacologically Activated p53

(2009) Martin Enge et al.   CANCER CELL

HIPK2 Regulation by MDM2 Determines Tumor Cell Response to the p53-Reactivating Drugs Nutlin-3 and RITA

(2009) C. Rinaldo et al.   CANCER RESEARCH

Identification of Nuclear Export Inhibitors with Potent Anticancer Activity In vivo

(2009) S. C. Mutka et al.   CANCER RESEARCH

Blinded by the Light: The Growing Complexity of p53

(2009) Karen H. Vousden et al.   CELL

Principles of Cancer Therapy: Oncogene and Non-oncogene Addiction

(2009) Ji Luo et al.   CELL

Modes of p53 Regulation

(2009) Jan-Philipp Kruse et al.   CELL

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

(2009) S. Sur et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Discovery, In Vivo Activity, and Mechanism of Action of a Small-Molecule p53 Activator

(2008) Sonia Lain et al.   CANCER CELL

SnapShot: p53 Posttranslational Modifications

(2008) Jan-Philipp Kruse et al.   CELL

A novel p53 rescue compound induces p53-dependent growth arrest and sensitises glioma cells to Apo2L/TRAIL-induced apoptosis

(2008) L Weinmann et al.   CELL DEATH AND DIFFERENTIATION

p53 Regulates Toll-Like Receptor 3 Expression and Function in Human Epithelial Cell Lines

(2008) M. Taura et al.   MOLECULAR AND CELLULAR BIOLOGY

Targeting tumor cells expressing p53 with a water-soluble inhibitor of Hdm2

(2008) J. Kitagaki et al.   MOLECULAR CANCER THERAPEUTICS

Mdm2 Regulates p53 mRNA Translation through Inhibitory Interactions with Ribosomal Protein L26

(2008) Yaara Ofir-Rosenfeld et al.   MOLECULAR CELL

Transcriptional control of human p53-regulated genes

(2008) Todd Riley et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Temporal activation of p53 by a specific MDM2 inhibitor is selectively toxic to tumors and leads to complete tumor growth inhibition

(2008) S. Shangary et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA