Pharmacological reactivation of p53 as a strategy to treat cancer

Small molecule MIRA-1 induces in vitro and in vivo anti-myeloma activity and synergizes with current anti-myeloma agents

(2014) M N Saha et al.   BRITISH JOURNAL OF CANCER

Mutant p53 in Cancer: New Functions and Therapeutic Opportunities

(2014) Patricia A.J. Muller et al.   CANCER CELL

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

(2014) Karita Peltonen et al.   CANCER CELL

Drugging the p53 pathway: understanding the route to clinical efficacy

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

Rescue of embryonic stem cells from cellular transformation by proteomic stabilization of mutant p53 and conversion into WT conformation

(2014) N. Rivlin et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

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

PRIMA-1Met/APR-246 Displays High Antitumor Activity in Multiple Myeloma By Induction of p73 and Noxa

(2013) Manujendra N. Saha et al.   MOLECULAR CANCER THERAPEUTICS

Interaction of p53 with the CCT Complex Promotes Protein Folding and Wild-Type p53 Activity

(2013) Antonio Garcia Trinidad et al.   MOLECULAR CELL

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

(2013) Michael S. Lawrence et al.   NATURE

Small molecule induced reactivation of mutant p53 in cancer cells

(2013) Xiangrui Liu et al.   NUCLEIC ACIDS RESEARCH

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

Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development

(2013) Binh Vu et al.   ACS Medicinal Chemistry Letters

Computational identification of a transiently open L1/S3 pocket for reactivation of mutant p53

(2013) Christopher D. Wassman et al.   Nature Communications

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

Allele-Specific p53 Mutant Reactivation

(2012) Xin Yu et al.   CANCER CELL

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

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

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

The substitutions G245C and G245D in the Zn2+-binding pocket of the p53 protein result in differences of conformational flexibility of the DNA-binding domain

(2012) S.S. Pintus et al.   JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS

Targeting p53 in Vivo: A First-in-Human Study With p53-Targeting Compound APR-246 in Refractory Hematologic Malignancies and Prostate Cancer

(2012) Sören Lehmann et al.   JOURNAL OF CLINICAL ONCOLOGY

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

MDM4 is a key therapeutic target in cutaneous melanoma

(2012) Agnieszka Gembarska et al.   NATURE MEDICINE

The TP53 website: an integrative resource centre for the TP53 mutation database and TP53 mutant analysis

(2012) Bernard Leroy et al.   NUCLEIC ACIDS RESEARCH

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

p73 tumor suppressor protein: A close relative of p53 not only in structure but also in anti-cancer approach?

(2011) Joanna Zawacka-Pankau 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

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

SAHA shows preferential cytotoxicity in mutant p53 cancer cells by destabilizing mutant p53 through inhibition of the HDAC6-Hsp90 chaperone axis

(2011) D Li et al.   CELL DEATH AND DIFFERENTIATION

PRIMA-1Met/APR-246 Induces Apoptosis and Tumor Growth Delay in Small Cell Lung Cancer Expressing Mutant p53

(2011) R. Zandi et al.   CLINICAL CANCER RESEARCH

Functional Inactivation of Endogenous MDM2 and CHIP by HSP90 Causes Aberrant Stabilization of Mutant p53 in Human Cancer Cells

(2011) D. Li et al.   MOLECULAR CANCER RESEARCH

The oncogenic phosphatase PPM1D confers cisplatin resistance in ovarian carcinoma cells by attenuating checkpoint kinase 1 and p53 activation

(2011) A Y Ali et al.   ONCOGENE

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

(2011) M H Aziz et al.   ONCOGENE

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

Non-genotoxic anti-neoplastic effects of ellipticine derivative NSC176327 in p53-deficient human colon carcinoma cells involve stimulation of p73

(2010) Chao Lu et al.   CANCER BIOLOGY & THERAPY

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

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

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

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 missing Zinc: p53 misfolding and cancer

(2010) Stewart N. Loh   Metallomics

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

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

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

Drug discovery and mutant p53

(2010) Magda M. Maslon et al.   TRENDS IN CELL BIOLOGY

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

PRIMA-1 Reactivates Mutant p53 by Covalent Binding to the Core Domain

(2009) Jeremy M.R. Lambert et al.   CANCER CELL

Blinded by the Light: The Growing Complexity of p53

(2009) Karen H. Vousden et al.   CELL

A comparison between p53 accumulation determined by immunohistochemistry andTP53mutations as prognostic variables in tumours from breast cancer patients

(2008) Jan Alsner et al.   ACTA ONCOLOGICA

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

(2008) Sonia Lain et al.   CANCER CELL

Restoring wtp53 activity in HIPK2 depleted MCF7 cells by modulating metallothionein and zinc

(2008) Rosa Puca et al.   EXPERIMENTAL CELL RESEARCH

The inherent instability of mutant p53 is alleviated by Mdm2 or p16INK4a loss

(2008) T. Terzian et al.   GENES & DEVELOPMENT

Small-molecule RETRA suppresses mutant p53-bearing cancer cells through a p73-dependent salvage pathway

(2008) J. E. Kravchenko et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Targeted rescue of a destabilized mutant of p53 by an in silico screened drug

(2008) F. M. Boeckler et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA