Targeting Cullin–RING E3 ubiquitin ligases for drug discovery: structure, assembly and small-molecule modulation

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

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

Structural and biochemical characterization of the KLHL3–WNK kinase interaction important in blood pressure regulation

(2014) Frances-Rose Schumacher et al.   BIOCHEMICAL JOURNAL

RBR E3 ubiquitin ligases: new structures, new insights, new questions

(2014) Donald E. Spratt et al.   BIOCHEMICAL JOURNAL

New strategies to inhibit KEAP1 and the Cul3-based E3 ubiquitin ligases

(2014) Peter Canning et al.   BIOCHEMICAL SOCIETY TRANSACTIONS

Structure of a RING E3 Trapped in Action Reveals Ligation Mechanism for the Ubiquitin-like Protein NEDD8

(2014) Daniel C. Scott et al.   CELL

Small-Molecule Inhibitors of Protein-Protein Interactions: Progressing toward the Reality

(2014) Michelle R. Arkin et al.   CHEMISTRY & BIOLOGY

Binding Mode and Structure-Activity Relationships around Direct Inhibitors of the Nrf2-Keap1 Complex

(2014) Eric Jnoff et al.   ChemMedChem

Biophysical Studies on Interactions and Assembly of Full-size E3 Ubiquitin Ligase

(2014) Emil Bulatov et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Structure-Guided Design and Optimization of Small Molecules Targeting the Protein–Protein Interaction between the von Hippel–Lindau (VHL) E3 Ubiquitin Ligase and the Hypoxia Inducible Factor (HIF) Alpha Subunit with in Vitro Nanomolar Affinities

(2014) Carles Galdeano et al.   JOURNAL OF MEDICINAL CHEMISTRY

Crystal structure of the human COP9 signalosome

(2014) Gondichatnahalli M. Lingaraju et al.   NATURE

Structural basis for hijacking CBF-β and CUL5 E3 ligase complex by HIV-1 Vif

(2014) Yingying Guo et al.   NATURE

Structure of the human Cereblon–DDB1–lenalidomide complex reveals basis for responsiveness to thalidomide analogs

(2014) Philip P Chamberlain et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

NMR approaches in structure-based lead discovery: Recent developments and new frontiers for targeting multi-protein complexes

(2014) David M. Dias et al.   PROGRESS IN BIOPHYSICS & MOLECULAR BIOLOGY

Structural insights for HIV-1 therapeutic strategies targeting Vif

(2014) Jason D. Salter et al.   TRENDS IN BIOCHEMICAL SCIENCES

Small molecules that inhibit Vif-induced degradation of APOBEC3G

(2014) Masashi Matsui et al.   Virology Journal

Structural basis of high-order oligomerization of the cullin-3 adaptor SPOP

(2013) Laura K. van Geersdaele et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Structural basis of intersubunit recognition in elongin BC–cullin 5–SOCS box ubiquitin–protein ligase complexes

(2013) Young Kwan Kim et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Multimeric Complexes among Ankyrin-Repeat and SOCS-box Protein 9 (ASB9), ElonginBC, and Cullin 5: Insights into the Structure and Assembly of ECS-type Cullin-RING E3 Ubiquitin Ligases

(2013) Jemima C. Thomas et al.   BIOCHEMISTRY

Small molecules inhibit the interaction of Nrf2 and the Keap1 Kelch domain through a non-covalent mechanism

(2013) Douglas Marcotte et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Discovery of a small-molecule inhibitor and cellular probe of Keap1–Nrf2 protein–protein interaction

(2013) Longqin Hu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Cand1 Promotes Assembly of New SCF Complexes through Dynamic Exchange of F Box Proteins

(2013) Nathan W. Pierce 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

The emerging family of CULLIN3-RING ubiquitin ligases (CRL3s): cellular functions and disease implications

(2013) Pascal Genschik et al.   EMBO JOURNAL

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

Substrate Binding Promotes Formation of the Skp1-Cul1-Fbxl3 (SCFFbxl3) Protein Complex

(2013) Kanae Yumimoto et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Structural Basis for Cul3 Protein Assembly with the BTB-Kelch Family of E3 Ubiquitin Ligases

(2013) Peter Canning 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

Molecular Architecture of the Ankyrin SOCS Box Family of Cul5-Dependent E3 Ubiquitin Ligases

(2013) João R.C. Muniz et al.   JOURNAL OF MOLECULAR 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

Crystal Structure of KLHL3 in Complex with Cullin3

(2013) Alan X. Ji et al.   PLoS One

Is NMR Fragment Screening Fine-Tuned to Assess Druggability of Protein–Protein Interactions?

(2013) David M. Dias et al.   ACS Medicinal Chemistry Letters

CSN- and CAND1-dependent remodelling of the budding yeast SCF complex

(2013) Aleksandra Zemla et al.   Nature Communications

CAND1 controls in vivo dynamics of the cullin 1-RING ubiquitin ligase repertoire

(2013) Shuangding Wu et al.   Nature Communications

Cullin 3 as a novel target in diverse pathologies

(2013) Ana Cristina Andérica-Romero et al.   Redox Biology

Small-Molecule Inhibitors of the Interaction between the E3 Ligase VHL and HIF1α

(2012) Dennis L. Buckley et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Small-Molecule Stabilization of Protein-Protein Interactions: An Underestimated Concept in Drug Discovery?

(2012) Philipp Thiel et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Dissecting Fragment-Based Lead Discovery at the von Hippel-Lindau Protein:Hypoxia Inducible Factor 1α Protein-Protein Interface

(2012) Inge Van Molle et al.   CHEMISTRY & BIOLOGY

Specific Small Molecule Inhibitors of Skp2-Mediated p27 Degradation

(2012) Lily Wu et al.   CHEMISTRY & BIOLOGY

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

The SOCS box-Adapting proteins for ubiquitination and proteasomal degradation

(2012) Edmond M. Linossi et al.   IUBMB LIFE

Targeting the von Hippel–Lindau E3 Ubiquitin Ligase Using Small Molecules To Disrupt the VHL/HIF-1α Interaction

(2012) Dennis L. Buckley et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

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

(2012) A Lopez-Girona et al.   LEUKEMIA

Small Molecule Modulators of Keap1-Nrf2-ARE Pathway as Potential Preventive and Therapeutic Agents

(2012) Sadagopan Magesh et al.   MEDICINAL RESEARCH REVIEWS

Structure of an E3:E2∼Ub Complex Reveals an Allosteric Mechanism Shared among RING/U-box Ligases

(2012) Jonathan N. Pruneda et al.   MOLECULAR CELL

Adaptor Protein Self-Assembly Drives the Control of a Cullin-RING Ubiquitin Ligase

(2012) Wesley J. Errington et al.   STRUCTURE

The Cullin-RING E3 Ubiquitin Ligase CRL4−DCAF1 Complex Dimerizes via a Short Helical Region in DCAF1

(2011) Jinwoo Ahn et al.   BIOCHEMISTRY

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

(2011) Y. X. Zhu et al.   BLOOD

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

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

NEDD8 Pathways in Cancer, Sine Quibus Non

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

The Molecular Basis of CRL4DDB2/CSA Ubiquitin Ligase Architecture, Targeting, and Activation

(2011) Eric S. Fischer et al.   CELL

An Allosteric Inhibitor of the Human Cdc34 Ubiquitin-Conjugating Enzyme

(2011) Derek F. Ceccarelli et al.   CELL

The Cullin7 E3 ubiquitin ligase: A novel player in growth control

(2011) Antonio Sarikas et al.   CELL CYCLE

Roles of COP9 signalosome in cancer

(2011) Mong-Hong Lee et al.   CELL CYCLE

Structural regulation of cullin-RING ubiquitin ligase complexes

(2011) David M Duda et al.   CURRENT OPINION IN STRUCTURAL 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

Vif hijacks CBF-β to degrade APOBEC3G and promote HIV-1 infection

(2011) Stefanie Jäger et al.   NATURE

An OBSL1-Cul7Fbxw8 Ubiquitin Ligase Signaling Mechanism Regulates Golgi Morphology and Dendrite Patterning

(2011) Nadia Litterman et al.   PLOS BIOLOGY

The cullin protein family

(2011) Antonio Sarikas et al.   GENOME BIOLOGY

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

(2010) Philip Cohen et al.   CELL

Dynamics of Cullin-RING Ubiquitin Ligase Network Revealed by Systematic Quantitative Proteomics

(2010) Eric J. Bennett et al.   CELL

Structural assembly of cullin-RING ubiquitin ligase complexes

(2010) Erik S Zimmerman et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

Substrate-Assisted Inhibition of Ubiquitin-like Protein-Activating Enzymes: The NEDD8 E1 Inhibitor MLN4924 Forms a NEDD8-AMP Mimetic In Situ

(2010) James E. Brownell et al.   MOLECULAR CELL

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

Ubiquitin-like protein conjugation and the ubiquitin–proteasome system as drug targets

(2010) Lynn Bedford et al.   NATURE REVIEWS DRUG DISCOVERY

Identification of a Primary Target of Thalidomide Teratogenicity

(2010) T. Ito et al.   SCIENCE

RING Domain E3 Ubiquitin Ligases

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

The emerging complexity of protein ubiquitination

(2009) David Komander   BIOCHEMICAL SOCIETY TRANSACTIONS

Rapid E2-E3 Assembly and Disassembly Enable Processive Ubiquitylation of Cullin-RING Ubiquitin Ligase Substrates

(2009) Gary Kleiger et al.   CELL

Ubiquitination, Ubiquitin-like Modifiers, and Deubiquitination in Viral Infection

(2009) Marisa K. Isaacson et al.   Cell Host & Microbe

REDD1, an inhibitor of mTOR signalling, is regulated by the CUL4A–DDB1 ubiquitin ligase

(2009) Samiksha Katiyar et al.   EMBO REPORTS

Structures of SPOP-Substrate Complexes: Insights into Molecular Architectures of BTB-Cul3 Ubiquitin Ligases

(2009) Min Zhuang et al.   MOLECULAR CELL

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

(2009) Teresa A. Soucy et al.   NATURE

Viral avoidance and exploitation of the ubiquitin system

(2009) Felix Randow et al.   NATURE CELL BIOLOGY

Building ubiquitin chains: E2 enzymes at work

(2009) Yihong Ye et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

A promiscuous α-helical motif anchors viral hijackers and substrate receptors to the CUL4–DDB1 ubiquitin ligase machinery

(2009) Ti Li et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Trapping Moving Targets with Small Molecules

(2009) G. M. Lee et al.   SCIENCE

CRL4s: the CUL4-RING E3 ubiquitin ligases

(2009) Sarah Jackson et al.   TRENDS IN BIOCHEMICAL SCIENCES

A novel small-molecule inhibitor of NF-κB signaling

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

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

The ubiquitin system, disease, and drug discovery

(2008) Matthew D Petroski   BMC BIOCHEMISTRY

Structural Insights into NEDD8 Activation of Cullin-RING Ligases: Conformational Control of Conjugation

(2008) David M. Duda et al.   CELL

WD40 protein FBW5 promotes ubiquitination of tumor suppressor TSC2 by DDB1-CUL4-ROC1 ligase

(2008) J. Hu et al.   GENES & DEVELOPMENT

Characterization of Cullin-box Sequences That Direct Recruitment of Cul2-Rbx1 and Cul5-Rbx2 Modules to Elongin BC-based Ubiquitin Ligases

(2008) Nawel Mahrour et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The SOCS Box Domain of SOCS3: Structure and Interaction with the ElonginBC-Cullin5 Ubiquitin Ligase

(2008) Jeffrey J. Babon et al.   JOURNAL OF MOLECULAR BIOLOGY

A Targeted Proteomic Analysis of the Ubiquitin-Like Modifier Nedd8 and Associated Proteins

(2008) Jeffrey Jones et al.   JOURNAL OF PROTEOME RESEARCH

The CUL7 E3 Ubiquitin Ligase Targets Insulin Receptor Substrate 1 for Ubiquitin-Dependent Degradation

(2008) Xinsong Xu et al.   MOLECULAR CELL

Multimodal Activation of the Ubiquitin Ligase SCF by Nedd8 Conjugation

(2008) Anjanabha Saha et al.   MOLECULAR CELL

Small-molecule inhibition of HIV-1 Vif

(2008) Robin Nathans et al.   NATURE BIOTECHNOLOGY

Diversity of degradation signals in the ubiquitin–proteasome system

(2008) Tommer Ravid et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Small-molecule agonists and antagonists of F-box protein-substrate interactions in auxin perception and signaling

(2008) K.-i. Hayashi et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA