Targeting ubiquitination for cancer therapies

Targeting deubiquitinase activity with a novel small-molecule inhibitor as therapy for B-cell malignancies

(2015) L. F. Peterson et al.   BLOOD

Characterization and identification of ubiquitin conjugation sites with E3 ligase recognition specificities

(2015) Van-Nui Nguyen et al.   BMC BIOINFORMATICS

Lenalidomide in multiple myeloma

(2015) Young Kim et al.   Expert Review of Anticancer Therapy

E3 ubiquitin ligases as drug targets and prognostic biomarkers in melanoma

(2015) Kristina Bielskienė et al.   Medicina-Lithuania

Skp2-Dependent Ubiquitination and Activation of LKB1 Is Essential for Cancer Cell Survival under Energy Stress

(2015) Szu-Wei Lee et al.   MOLECULAR CELL

Deubiquitinase inhibition as a cancer therapeutic strategy

(2015) Padraig D'Arcy et al.   PHARMACOLOGY & THERAPEUTICS

E3 ubiquitin ligases as drug targets and prognostic biomarkers in melanoma

(2015) Kristina Bielskienė et al.   Medicina-Lithuania

Modulation of Immune Cell Functions by the E3 Ligase Cbl-b

(2015) Christina Lutz-Nicoladoni et al.   Frontiers in Oncology

Proteotoxic crisis, the ubiquitin-proteasome system, and cancer therapy

(2014) Raymond J Deshaies   BMC BIOLOGY

Emerging Potential of Therapeutic Targeting of Ubiquitin-Specific Proteases in the Treatment of Cancer

(2014) A. Pal et al.   CANCER RESEARCH

Skp2: A dream target in the coming age of cancer therapy

(2014) Chia-Hsin Chan et al.   CELL CYCLE

E3 ubiquitin ligase Cbl-b in innate and adaptive immunity

(2014) Liu Qingjun et al.   CELL CYCLE

Proteasome inhibitors - molecular basis and current perspectives in multiple myeloma

(2014) Lenka Kubiczkova et al.   JOURNAL OF CELLULAR AND MOLECULAR MEDICINE

Safety and tolerability of ixazomib, an oral proteasome inhibitor, in combination with lenalidomide and dexamethasone in patients with previously untreated multiple myeloma: an open-label phase 1/2 study

(2014) Shaji K Kumar et al.   LANCET ONCOLOGY

USP15 stabilizes MDM2 to mediate cancer-cell survival and inhibit antitumor T cell responses

(2014) Qiang Zou et al.   NATURE IMMUNOLOGY

Ubiquitination in disease pathogenesis and treatment

(2014) Doris Popovic et al.   NATURE MEDICINE

SCF ubiquitin ligase-targeted therapies

(2014) Jeffrey R. Skaar et al.   NATURE REVIEWS DRUG DISCOVERY

New insights into ubiquitin E3 ligase mechanism

(2014) Christopher E Berndsen et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

The E3 ubiquitin ligase NEDD4 negatively regulates HER3/ErbB3 level and signaling

(2014) Z Huang et al.   ONCOGENE

Pharmacologic activation of wild-type p53 by nutlin therapy in childhood cancer

(2013) Tom Van Maerken et al.   CANCER LETTERS

Pharmacological Inactivation of Skp2 SCF Ubiquitin Ligase Restricts Cancer Stem Cell Traits and Cancer Progression

(2013) Chia-Hsin Chan et al.   CELL

Inhibition of Protein Deubiquitination by PR-619 Activates the Autophagic Pathway in OLN-t40 Oligodendroglial Cells

(2013) Veronika Seiberlich et al.   CELL BIOCHEMISTRY AND BIOPHYSICS

Over-Expression of Deubiquitinating Enzyme USP14 in Lung Adenocarcinoma Promotes Proliferation through the Accumulation of β-Catenin

(2013) Ning Wu et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Role of Ubiquitin Ligases and the Proteasome in Oncogenesis: Novel Targets for Anticancer Therapies

(2013) Lindsey N. Micel et al.   JOURNAL OF CLINICAL ONCOLOGY

Exploring a New Frontier in Cancer Treatment: Targeting the Ubiquitin and Ubiquitin-like Activating Enzymes

(2013) Sara R. da Silva et al.   JOURNAL OF MEDICINAL CHEMISTRY

A combinatorial F box protein directed pathway controls TRAF adaptor stability to regulate inflammation

(2013) Bill B Chen et al.   NATURE IMMUNOLOGY

Mechanisms and function of substrate recruitment by F-box proteins

(2013) Jeffrey R. Skaar et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Structure of a ubiquitin-loaded HECT ligase reveals the molecular basis for catalytic priming

(2013) Elena Maspero et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Alterations of the Intracellular Peptidome in Response to the Proteasome Inhibitor Bortezomib

(2013) Julia S. Gelman et al.   PLoS One

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

A Strategy for Modulation of Enzymes in the Ubiquitin System

(2013) A. Ernst et al.   SCIENCE

The Myeloma Drug Lenalidomide Promotes the Cereblon-Dependent Destruction of Ikaros Proteins

(2013) G. Lu et al.   SCIENCE

Linear ubiquitination: a newly discovered regulator of cell signalling

(2013) Eva Rieser et al.   TRENDS IN BIOCHEMICAL SCIENCES

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

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

The Ubiquitin Code

(2012) David Komander et al.   Annual Review of Biochemistry

The small molecule inhibitor PR-619 of deubiquitinating enzymes affects the microtubule network and causes protein aggregate formation in neural cells: Implications for neurodegenerative diseases

(2012) Veronika Seiberlich et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

Ubiquitin-based anticancer therapy: Carpet bombing with proteasome inhibitors vs surgical strikes with E1, E2, E3, or DUB inhibitors

(2012) Michael R. Mattern et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

An open-label, single-arm, phase 2 (PX-171-004) study of single-agent carfilzomib in bortezomib-naive patients with relapsed and/or refractory multiple myeloma

(2012) R. Vij et al.   BLOOD

An open-label, single-arm, phase 2 study of single-agent carfilzomib in patients with relapsed and/or refractory multiple myeloma who have been previously treated with bortezomib

(2012) Ravi Vij et al.   BRITISH JOURNAL OF HAEMATOLOGY

The Skp2-SCF E3 Ligase Regulates Akt Ubiquitination, Glycolysis, Herceptin Sensitivity, and Tumorigenesis

(2012) Chia-Hsin Chan et al.   CELL

Specific Small Molecule Inhibitors of Skp2-Mediated p27 Degradation

(2012) Lily Wu et al.   CHEMISTRY & BIOLOGY

P53 Mdm2 Inhibitors

(2012) Kareem Khoury et al.   CURRENT PHARMACEUTICAL DESIGN

Computational Prediction of Protein Hot Spot Residues

(2012) John Kenneth Morrow et al.   CURRENT PHARMACEUTICAL DESIGN

MLN4924: a novel first-in-class inhibitor of NEDD8-activating enzyme for cancer therapy

(2012) Steffan T Nawrocki et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

HECT and RING finger families of E3 ubiquitin ligases at a glance

(2012) M. B. Metzger et al.   JOURNAL OF CELL SCIENCE

Manadosterols A and B, Sulfonated Sterol Dimers Inhibiting the Ubc13–Uev1A Interaction, Isolated from the Marine Sponge Lissodendryx fibrosa

(2012) Shuntaro Ushiyama et al.   JOURNAL OF NATURAL PRODUCTS

Cereblon is a direct protein target for immunomodulatory and antiproliferative activities of lenalidomide and pomalidomide

(2012) A Lopez-Girona et al.   LEUKEMIA

Refined Preparation and Use of Anti-diglycine Remnant (K-ε-GG) Antibody Enables Routine Quantification of 10,000s of Ubiquitination Sites in Single Proteomics Experiments

(2012) Namrata D. Udeshi et al.   MOLECULAR & CELLULAR PROTEOMICS

MDM4 is a key therapeutic target in cutaneous melanoma

(2012) Agnieszka Gembarska et al.   NATURE MEDICINE

USP15 stabilizes TGF-β receptor I and promotes oncogenesis through the activation of TGF-β signaling in glioblastoma

(2012) Pieter J A Eichhorn et al.   NATURE MEDICINE

Erioflorin Stabilizes the Tumor Suppressor Pdcd4 by Inhibiting Its Interaction with the E3-ligase β-TrCP1

(2012) Johanna S. Blees et al.   PLoS One

Cereblon expression is required for the antimyeloma activity of lenalidomide and pomalidomide

(2011) Y. X. Zhu et al.   BLOOD

Preclinical assessment of JNJ-26854165 (Serdemetan), a novel tryptamine compound with radiosensitizing activity in vitro and in tumor xenografts

(2011) Cyrus Chargari et al.   CANCER LETTERS

An Allosteric Inhibitor of the Human Cdc34 Ubiquitin-Conjugating Enzyme

(2011) Derek F. Ceccarelli et al.   CELL

Activity-Based Chemical Proteomics Accelerates Inhibitor Development for Deubiquitylating Enzymes

(2011) Mikael Altun et al.   CHEMISTRY & BIOLOGY

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

Marizomib, a Proteasome Inhibitor for All Seasons: Preclinical Profile and a Framework for Clinical Trials

(2011) B. C. Potts et al.   CURRENT CANCER DRUG TARGETS

Nedd4-1 binds and ubiquitylates activated FGFR1 to control its endocytosis and function

(2011) Avinash Persaud et al.   EMBO JOURNAL

Structure of the HECT:ubiquitin complex and its role in ubiquitin chain elongation

(2011) Elena Maspero et al.   EMBO REPORTS

Phase 1 clinical trial of the novel proteasome inhibitor marizomib with the histone deacetylase inhibitor vorinostat in patients with melanoma, pancreatic and lung cancer based on in vitro assessments of the combination

(2011) Michael Millward et al.   INVESTIGATIONAL NEW DRUGS

Mechanism of Action of Proteasome Inhibitors and Deacetylase Inhibitors and the Biological Basis of Synergy in Multiple Myeloma

(2011) T. Hideshima et al.   MOLECULAR CANCER THERAPEUTICS

USP15 is a deubiquitylating enzyme for receptor-activated SMADs

(2011) Masafumi Inui et al.   NATURE CELL BIOLOGY

Molecular Mechanisms of Bortezomib Resistant Adenocarcinoma Cells

(2011) Erika Suzuki et al.   PLoS One

Inhibition of NEDD8-activating enzyme: a novel approach for the treatment of acute myeloid leukemia

(2010) R. T. Swords et al.   BLOOD

Deubiquitinase Inhibition by Small-Molecule WP1130 Triggers Aggresome Formation and Tumor Cell Apoptosis

(2010) V. Kapuria et al.   CANCER RESEARCH

Evaluation of the Proteasome Inhibitor MLN9708 in Preclinical Models of Human Cancer

(2010) E. Kupperman et al.   CANCER RESEARCH

Differential binding of p53 and nutlin to MDM2 and MDMX: Computational studies

(2010) Thomas Leonard Joseph et al.   CELL CYCLE

Ubiquitin networks in cancer

(2010) Vladimir Kirkin et al.   CURRENT OPINION IN GENETICS & DEVELOPMENT

Building on bortezomib: second-generation proteasome inhibitors as anti-cancer therapy

(2010) Lawrence R. Dick et al.   DRUG DISCOVERY TODAY

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

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

Enhancement of proteasome activity by a small-molecule inhibitor of USP14

(2010) Byung-Hoon Lee et al.   NATURE

An allosteric inhibitor of substrate recognition by the SCFCdc4 ubiquitin ligase

(2010) Stephen Orlicky et al.   NATURE BIOTECHNOLOGY

Chemical genetics screen for enhancers of rapamycin identifies a specific inhibitor of an SCF family E3 ubiquitin ligase

(2010) Mariam Aghajan et al.   NATURE BIOTECHNOLOGY

Deciphering the transcriptional complex critical for RhoA gene expression and cancer metastasis

(2010) Chia-Hsin Chan et al.   NATURE CELL BIOLOGY

Emerging role of Lys-63 ubiquitination in protein kinase and phosphatase activation and cancer development

(2010) W-L Yang et al.   ONCOGENE

Identification of a Primary Target of Thalidomide Teratogenicity

(2010) T. Ito et al.   SCIENCE

Pomalidomide: A new IMiD with remarkable activity in both multiple myeloma and myelofibrosis

(2009) Martha Q. Lacy et al.   AMERICAN JOURNAL OF HEMATOLOGY

RING Domain E3 Ubiquitin Ligases

(2009) Raymond J. Deshaies et al.   Annual Review of Biochemistry

The multiple levels of regulation by p53 ubiquitination

(2009) J T Lee et al.   CELL DEATH AND DIFFERENTIATION

Nedd4 mediates ErbB4 JM-a/CYT-1 ICD ubiquitination and degradation in MDCK II cells

(2009) Fenghua Zeng et al.   FASEB JOURNAL

Absolute Configuration of the α,ω-Bifunctionalized Sphingolipid Leucettamol A fromLeucetta microrhaphisby Deconvoluted Exciton Coupled CD⊥

(2009) Doralyn S. Dalisay et al.   JOURNAL OF NATURAL PRODUCTS

Nonproteolytic Functions of Ubiquitin in Cell Signaling

(2009) Zhijian J. Chen et al.   MOLECULAR CELL

Targeting the ubiquitin system in cancer therapy

(2009) Daniela Hoeller et al.   NATURE

Phosphorylation-dependent regulation of cytosolic localization and oncogenic function of Skp2 by Akt/PKB

(2009) Hui-Kuan Lin et al.   NATURE CELL BIOLOGY

Ubiquitin-like protein activation by E1 enzymes: the apex for downstream signalling pathways

(2009) Brenda A. Schulman et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Physiological functions of the HECT family of ubiquitin ligases

(2009) Daniela Rotin et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Breaking the chains: structure and function of the deubiquitinases

(2009) David Komander et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

A novel small-molecule inhibitor of NF-κB signaling

(2008) Hiroto Nakajima et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Leucettamol A: A new inhibitor of Ubc13-Uev1A interaction isolated from a marine sponge, Leucetta aff. microrhaphis

(2008) Sachiko Tsukamoto et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Targeting the p27 E3 ligase SCFSkp2 results in p27- and Skp2-mediated cell-cycle arrest and activation of autophagy

(2008) Q. Chen et al.   BLOOD

Oncogenic properties and prognostic implications of the ubiquitin ligase Skp2 in cancer

(2008) Dan D. Hershko   CANCER

Targeting the ubiquitin-proteasome system for cancer therapy

(2008) Yili Yang et al.   CANCER SCIENCE

Identification of SCF Ubiquitin Ligase Substrates by Global Protein Stability Profiling

(2008) H.-C. S. Yen et al.   SCIENCE

Global Protein Stability Profiling in Mammalian Cells

(2008) H.-C. S. Yen et al.   SCIENCE

Targeting ubiquitin specific proteases for drug discovery

(2007) Laurent Daviet et al.   BIOCHIMIE