SCF ubiquitin ligase-targeted therapies

Macrocerebellum, epilepsy, intellectual disability, and gut malrotation in a child with a 16q24.1-q24.2 contiguous gene deletion

(2014) Andrea H. Seeley et al.   AMERICAN JOURNAL OF MEDICAL GENETICS PART A

Small-Molecule Control of Intracellular Protein Levels through Modulation of the Ubiquitin Proteasome System

(2014) Dennis L. Buckley et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

MLN4924, an NAE inhibitor, suppresses AKT and mTOR signaling via upregulation of REDD1 in human myeloma cells

(2014) Y. Gu et al.   BLOOD

Role of Fbxw7 in the maintenance of normal stem cells and cancer-initiating cells

(2014) S Takeishi et al.   BRITISH JOURNAL OF CANCER

New Hepatitis C Therapies: The Toolbox, Strategies, and Challenges

(2014) Jean–Michel Pawlotsky   GASTROENTEROLOGY

Truncation of the E3 ubiquitin ligase component FBXO31 causes non-syndromic autosomal recessive intellectual disability in a Pakistani family

(2014) Asif Mir et al.   HUMAN GENETICS

Proteasome inhibitors - molecular basis and current perspectives in multiple myeloma

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

Inactivation of SAG/RBX2 E3 ubiquitin ligase suppresses KrasG12D-driven lung tumorigenesis

(2014) Hua Li et al.   JOURNAL OF CLINICAL INVESTIGATION

Overactivated Neddylation Pathway as a Therapeutic Target in Lung Cancer

(2014) Lihui Li et al.   JNCI-Journal of the National Cancer Institute

Discovery and saturation analysis of cancer genes across 21 tumour types

(2014) Michael S. Lawrence et al.   NATURE

Nature Biotechnology's academic spinouts of 2013

(2014) Aaron Bouchie et al.   NATURE BIOTECHNOLOGY

New insights into ubiquitin E3 ligase mechanism

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

Mutations in UBA3 Confer Resistance to the NEDD8-Activating Enzyme Inhibitor MLN4924 in Human Leukemic Cells

(2014) G. Wei Xu et al.   PLoS One

Antiviral treatment of hepatitis C

(2014) E. R. Feeney et al.   BMJ-British Medical Journal

Mutations in FBXL4 Cause Mitochondrial Encephalopathy and a Disorder of Mitochondrial DNA Maintenance

(2013) Penelope E. Bonnen et al.   AMERICAN JOURNAL OF HUMAN GENETICS

Mutations in FBXL4, Encoding a Mitochondrial Protein, Cause Early-Onset Mitochondrial Encephalomyopathy

(2013) Xiaowu Gai et al.   AMERICAN JOURNAL OF HUMAN GENETICS

Regulation of proteasome activity in health and disease

(2013) Marion Schmidt et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

A novel small molecule inhibitor of deubiquitylating enzyme USP14 and UCHL5 induces apoptosis in multiple myeloma and overcomes bortezomib resistance

(2013) Z. Tian et al.   BLOOD

Regulation of c-Myc Ubiquitination Controls Chronic Myelogenous Leukemia Initiation and Progression

(2013) Linsey Reavie et al.   CANCER CELL

Ablation of Fbxw7 Eliminates Leukemia-Initiating Cells by Preventing Quiescence

(2013) Shoichiro Takeishi et al.   CANCER CELL

P97/CDC-48: Proteostasis control in tumor cell biology

(2013) Delphine Fessart et al.   CANCER LETTERS

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

(2013) Tom Van Maerken et al.   CANCER LETTERS

The Ubiquitin Ligase FBXW7 Modulates Leukemia-Initiating Cell Activity by Regulating MYC Stability

(2013) Bryan King et al.   CELL

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

(2013) Chia-Hsin Chan et al.   CELL

Crystal structure of mammalian cryptochrome in complex with a small molecule competitor of its ubiquitin ligase

(2013) Shannon Nangle et al.   CELL RESEARCH

Structure-Activity Relationship Study Reveals ML240 and ML241 as Potent and Selective Inhibitors of p97 ATPase

(2013) Tsui-Fen Chou et al.   ChemMedChem

Building and remodelling Cullin-RING E3 ubiquitin ligases

(2013) John R Lydeard et al.   EMBO REPORTS

Inhibitors of SCF-Skp2/Cks1 E3 Ligase Block Estrogen-Induced Growth Stimulation and Degradation of Nuclear p27kip1: Therapeutic Potential for Endometrial Cancer

(2013) Savvas C. Pavlides et al.   ENDOCRINOLOGY

Palbociclib (PD 0332991): targeting the cell cycle machinery in breast cancer

(2013) Andrea Rocca et al.   EXPERT OPINION ON PHARMACOTHERAPY

Ubiquitin E3 Ligase CRL4CDT2/DCAF2as a Potential Chemotherapeutic Target for Ovarian Surface Epithelial Cancer

(2013) Wei-Wei Pan et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Targeting F Box Protein Fbxo3 To Control Cytokine-Driven Inflammation

(2013) R. K. Mallampalli et al.   JOURNAL OF IMMUNOLOGY

Regulation of the CRL4Cdt2 Ubiquitin Ligase and Cell-Cycle Exit by the SCFFbxo11 Ubiquitin Ligase

(2013) Mario Rossi et al.   MOLECULAR CELL

CRL1-FBXO11 Promotes Cdt2 Ubiquitylation and Degradation and Regulates Pr-Set7/Set8-Mediated Cellular Migration

(2013) Tarek Abbas et al.   MOLECULAR CELL

SCFFBXL3 ubiquitin ligase targets cryptochromes at their cofactor pocket

(2013) Weiman Xing et al.   NATURE

FBXL2- and PTPL1-mediated degradation of p110-free p85β regulatory subunit controls the PI(3)K signalling cascade

(2013) Shafi Kuchay et al.   NATURE CELL BIOLOGY

Covalent and allosteric inhibitors of the ATPase VCP/p97 induce cancer cell death

(2013) Paola Magnaghi et al.   Nature Chemical Biology

E2 enzyme inhibition by stabilization of a low-affinity interface with ubiquitin

(2013) Hao Huang et al.   Nature Chemical Biology

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

Targeting nuclear kinases in cancer: Development of cell cycle kinase inhibitors

(2013) Todd M. Pitts et al.   PHARMACOLOGY & THERAPEUTICS

Lenalidomide Causes Selective Degradation of IKZF1 and IKZF3 in Multiple Myeloma Cells

(2013) J. Kronke 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

Skp-cullin-F box E3 ligase component FBXL2 ubiquitinates Aurora B to inhibit tumorigenesis

(2013) B B Chen et al.   Cell Death & Disease

The Ubiquitin Code

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

Serine Phosphorylation Is Critical for the Activation of Ubiquitin-Specific Protease 1 and Its Interaction with WD40-Repeat Protein UAF1

(2012) Mark A. Villamil et al.   BIOCHEMISTRY

A Noncanonical Cysteine Protease USP1 Is Activated through Active Site Modulation by USP1-Associated Factor 1

(2012) Mark A. Villamil et al.   BIOCHEMISTRY

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

F-box protein FBXL2 targets cyclin D2 for ubiquitination and degradation to inhibit leukemic cell proliferation

(2012) B. B. Chen et al.   BLOOD

A Small Molecule Inhibitor of Ubiquitin-Specific Protease-7 Induces Apoptosis in Multiple Myeloma Cells and Overcomes Bortezomib Resistance

(2012) Dharminder Chauhan et al.   CANCER CELL

Treatment-Emergent Mutations in NAEβ Confer Resistance to the NEDD8-Activating Enzyme Inhibitor MLN4924

(2012) Michael A. Milhollen et al.   CANCER CELL

Novel DNA Damage Checkpoints Mediating Cell Death Induced by the NEDD8-Activating Enzyme Inhibitor MLN4924

(2012) J. L. Blank et al.   CANCER RESEARCH

MiR-30a-5p suppresses tumor growth in colon carcinoma by targeting DTL

(2012) Alexander Baraniskin et al.   CARCINOGENESIS

Specific Small Molecule Inhibitors of Skp2-Mediated p27 Degradation

(2012) Lily Wu et al.   CHEMISTRY & BIOLOGY

HIV-1 Vpu Interference with Innate Cell-mediated Immune Mechanisms

(2012) Johan K. Sandberg et al.   CURRENT HIV RESEARCH

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

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

Signal-Induced Disassembly of the SCF Ubiquitin Ligase Complex by Cdc48/p97

(2012) James L. Yen et al.   MOLECULAR CELL

Fbxw7α- and GSK3-mediated degradation of p100 is a pro-survival mechanism in multiple myeloma

(2012) Luca Busino et al.   NATURE CELL BIOLOGY

Recurrent mutation of the ID3 gene in Burkitt lymphoma identified by integrated genome, exome and transcriptome sequencing

(2012)   NATURE GENETICS

NEDD8 links cullin-RING ubiquitin ligase function to the p97 pathway

(2012) Willem den Besten et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

WEE1 accumulation and deregulation of S-phase proteins mediate MLN4924 potent inhibitory effect on Ewing sarcoma cells

(2012) C Mackintosh et al.   ONCOGENE

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

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

Discovery and prioritization of somatic mutations in diffuse large B-cell lymphoma (DLBCL) by whole-exome sequencing

(2012) J. G. Lohr et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Identification of Small Molecule Activators of Cryptochrome

(2012) T. Hirota et al.   SCIENCE

Selective Dual Inhibitors of the Cancer-Related Deubiquitylating Proteases USP7 and USP47

(2012) Joseph Weinstock et al.   ACS Medicinal Chemistry Letters

A Gatekeeper Residue for NEDD8-Activating Enzyme Inhibition by MLN4924

(2012) Julia I. Toth et al.   Cell Reports

GS-1101: A Delta-Specific PI3K Inhibitor in Chronic Lymphocytic Leukemia

(2012) Ines M. Macias-Perez et al.   Current Hematologic Malignancy Reports

Chemical genetics approach to restoring p27Kip1 reveals novel compounds with antiproliferative activity in prostate cancer cells

(2011) Elizabeth Rico-Bautista et al.   BMC BIOLOGY

Phase I study of PD 0332991, a cyclin-dependent kinase inhibitor, administered in 3-week cycles (Schedule 2/1)

(2011) G K Schwartz et al.   BRITISH JOURNAL OF CANCER

NEDD8 Pathways in Cancer, Sine Quibus Non

(2011) Ian R. Watson et al.   CANCER CELL

Radiosensitization of Human Pancreatic Cancer Cells by MLN4924, an Investigational NEDD8-Activating Enzyme Inhibitor

(2011) D. Wei et al.   CANCER RESEARCH

An Allosteric Inhibitor of the Human Cdc34 Ubiquitin-Conjugating Enzyme

(2011) Derek F. Ceccarelli et al.   CELL

The Multifaceted Roles of USP7: New Therapeutic Opportunities

(2011) Benjamin Nicholson et al.   CELL BIOCHEMISTRY AND BIOPHYSICS

Teratogenic effects of thalidomide: molecular mechanisms

(2011) Takumi Ito et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

Selective and Cell-Active Inhibitors of the USP1/ UAF1 Deubiquitinase Complex Reverse Cisplatin Resistance in Non-small Cell Lung Cancer Cells

(2011) Junjun Chen et al.   CHEMISTRY & BIOLOGY

Mechanistic Studies of Substrate-assisted Inhibition of Ubiquitin-activating Enzyme by Adenosine Sulfamate Analogues

(2011) Jesse J. Chen et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Novel Proteasome Inhibitors to Overcome Bortezomib Resistance

(2011) Amy M. Ruschak et al.   JNCI-Journal of the National Cancer Institute

Calmodulin Antagonizes a Calcium-Activated SCF Ubiquitin E3 Ligase Subunit, FBXL2, To Regulate Surfactant Homeostasis

(2011) B. B. Chen et al.   MOLECULAR AND CELLULAR BIOLOGY

Mechanism of USP7/HAUSP Activation by Its C-Terminal Ubiquitin-like Domain and Allosteric Regulation by GMP-Synthetase

(2011) Alex C. Faesen et al.   MOLECULAR CELL

Frequent pathway mutations of splicing machinery in myelodysplasia

(2011) Kenichi Yoshida et al.   NATURE

FBXO11 targets BCL6 for degradation and is inactivated in diffuse large B-cell lymphomas

(2011) Shanshan Duan et al.   NATURE

F-box protein FBXL2 exerts human lung tumor suppressor-like activity by ubiquitin-mediated degradation of cyclin D3 resulting in cell cycle arrest

(2011) B B Chen et al.   ONCOGENE

1q gain and CDT2 overexpression underlie an aggressive and highly proliferative form of Ewing sarcoma

(2011) C Mackintosh et al.   ONCOGENE

Initial testing of the investigational NEDD8-activating enzyme inhibitor MLN4924 by the pediatric preclinical testing program

(2011) Malcolm A. Smith et al.   PEDIATRIC BLOOD & CANCER

Molecular Mechanisms of Bortezomib Resistant Adenocarcinoma Cells

(2011) Erika Suzuki et al.   PLoS One

The Mutational Landscape of Head and Neck Squamous Cell Carcinoma

(2011) N. Stransky et al.   SCIENCE

PI3K  Inhibitors in Cancer: Rationale and Serendipity Merge in the Clinic

(2011) D. A. Fruman et al.   Cancer Discovery

MLN4924, a NEDD8-activating enzyme inhibitor, is active in diffuse large B-cell lymphoma models: rationale for treatment of NF- B-dependent lymphoma

(2010) M. A. Milhollen et al.   BLOOD

NEDD8-Targeting Drug MLN4924 Elicits DNA Rereplication by Stabilizing Cdt1 in S Phase, Triggering Checkpoint Activation, Apoptosis, and Senescence in Cancer Cells

(2010) J. J. Lin et al.   CANCER RESEARCH

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

(2010) V. Kapuria et al.   CANCER RESEARCH

Will the Ubiquitin System Furnish as Many Drug Targets as Protein Kinases?

(2010) Philip Cohen et al.   CELL

Toward the Rational Design of p53-Stabilizing Drugs: Probing the Surface of the Oncogenic Y220C Mutant

(2010) Nicolas Basse et al.   CHEMISTRY & BIOLOGY

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

(2010) Byung-Hoon Lee et al.   NATURE

Diverse somatic mutation patterns and pathway alterations in human cancers

(2010) Zhengyan Kan 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

New genetic loci implicated in fasting glucose homeostasis and their impact on type 2 diabetes risk

(2010) Josée Dupuis et al.   NATURE GENETICS

Cryptochrome mediates circadian regulation of cAMP signaling and hepatic gluconeogenesis

(2010) Eric E Zhang et al.   NATURE MEDICINE

The ubiquitous nature of cancer: the role of the SCFFbw7 complex in development and transformation

(2010) K M Crusio et al.   ONCOGENE

Identification of a Primary Target of Thalidomide Teratogenicity

(2010) T. Ito et al.   SCIENCE

Oncogenic Activation of NF- B

(2010) L. M. Staudt   Cold Spring Harbor Perspectives in Biology

RING Domain E3 Ubiquitin Ligases

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

Identification of retinoic acid-regulated nuclear matrix-associated protein as a novel regulator of gastric cancer

(2009) J Li et al.   BRITISH JOURNAL OF CANCER

SnapShot: F Box Proteins II

(2009) Jeffrey R. Skaar et al.   CELL

Interplay between poxviruses and the cellular ubiquitin/ubiquitin-like pathways

(2009) Leiliang Zhang et al.   FEBS LETTERS

The 26 S Proteasome: From Basic Mechanisms to Drug Targeting

(2009) Ami Navon et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Small-molecule inhibitor of USP7/HAUSP ubiquitin protease stabilizes and activates p53 in cells

(2009) F. Colland et al.   MOLECULAR CANCER THERAPEUTICS

βTrCP- and Rsk1/2-Mediated Degradation of BimEL Inhibits Apoptosis

(2009) Elinor Dehan et al.   MOLECULAR CELL

An inhibitor of NEDD8-activating enzyme as a new approach to treat cancer

(2009) Teresa A. Soucy et al.   NATURE

An auxin-based degron system for the rapid depletion of proteins in nonplant cells

(2009) Kohei Nishimura et al.   NATURE METHODS

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

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

Molecular Mimicry by an F-Box Effector of Legionella pneumophila Hijacks a Conserved Polyubiquitination Machinery within Macrophages and Protozoa

(2009) Christopher T. Price et al.   PLoS Pathogens

A novel small-molecule inhibitor of NF-κB signaling

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

Targeted intracellular protein degradation induced by a small molecule: En route to chemical proteomics

(2008) Ashley R. Schneekloth 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

Fbxw7 acts as a critical fail-safe against premature loss of hematopoietic stem cells and development of T-ALL

(2008) S. Matsuoka et al.   GENES & DEVELOPMENT

Control of hematopoietic stem cell quiescence by the E3 ubiquitin ligase Fbw7

(2008) Benjamin J. Thompson et al.   JOURNAL OF EXPERIMENTAL MEDICINE

FBXO7 mutations cause autosomal recessive, early-onset parkinsonian-pyramidal syndrome

(2008) A. D. Fonzo et al.   NEUROLOGY

Involvement of elevated expression of multiple cell-cycle regulator, DTL/RAMP (denticleless/RA-regulated nuclear matrix associated protein), in the growth of breast cancer cells

(2008) T Ueki et al.   ONCOGENE

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

The COP9 signalosome: more than a protease

(2008) N WEI et al.   TRENDS IN BIOCHEMICAL SCIENCES

Activating the ubiquitin family: UBA6 challenges the field

(2008) Marcus Groettrup et al.   TRENDS IN BIOCHEMICAL SCIENCES