PROTAC targeted protein degraders: the past is prologue

The Rise of Molecular Glues

(2021) Stuart L. Schreiber   CELL

Development of Antibody-Based PROTACs for the Degradation of the Cell-Surface Immune Checkpoint Protein PD-L1

(2021) Adam D. Cotton et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Functional Genomics Identify Distinct and Overlapping Genes Mediating Resistance to Different Classes of Heterobifunctional Degraders of Oncoproteins

(2021) Ryosuke Shirasaki et al.   Cell Reports

Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 1: Exploration of Antibody Linker, Payload Loading, and Payload Molecular Properties

(2021) Peter S. Dragovich et al.   JOURNAL OF MEDICINAL CHEMISTRY

Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy

(2021) Peter S. Dragovich et al.   JOURNAL OF MEDICINAL CHEMISTRY

Ubiquitin ligation to F-box protein targets by SCF–RBR E3–E3 super-assembly

(2021) Daniel Horn-Ghetko et al.   NATURE

Cancer therapies based on targeted protein degradation — lessons learned with lenalidomide

(2021) Max Jan et al.   Nature Reviews Clinical Oncology

Tau: Enabler of diverse brain disorders and target of rapidly evolving therapeutic strategies

(2021) Che-Wei Chang et al.   SCIENCE

Targeting oncoproteins with a positive selection assay for protein degraders

(2021) Vidyasagar Koduri et al.   Science Advances

Transforming targeted cancer therapy with PROTACs: A forward-looking perspective

(2021) William Farnaby et al.   CURRENT OPINION IN PHARMACOLOGY

Targeted protein degraders crowd into the clinic

(2021) Asher Mullard   NATURE REVIEWS DRUG DISCOVERY

Nanotechnology advances in pathogen- and host-targeted antiviral delivery: multipronged therapeutic intervention for pandemic control

(2021) Kai-Chieh Yang et al.   Drug Delivery and Translational Research

Persistent repression of tau in the brain using engineered zinc finger protein transcription factors

(2021) Susanne Wegmann et al.   Science Advances

In vitro and in vivo degradation of programmed cell death ligand 1 (PD-L1) by a proteolysis targeting chimera (PROTAC)

(2021) Yubo Wang et al.   BIOORGANIC CHEMISTRY

Strategies toward Discovery of Potent and Orally Bioavailable Proteolysis Targeting Chimera Degraders of Androgen Receptor for the Treatment of Prostate Cancer

(2021) Xin Han et al.   JOURNAL OF MEDICINAL CHEMISTRY

TF-PROTACs Enable Targeted Degradation of Transcription Factors

(2021) Jing Liu et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Harnessing the E3 Ligase KEAP1 for Targeted Protein Degradation

(2021) Jieli Wei et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Highly accurate protein structure prediction for the human proteome

(2021) Kathryn Tunyasuvunakool et al.   NATURE

The PROTACtable genome

(2021) Melanie Schneider et al.   NATURE REVIEWS DRUG DISCOVERY

Accurate prediction of protein structures and interactions using a three-track neural network

(2021) Minkyung Baek et al.   SCIENCE

Degradation of CCNK/CDK12 is a druggable vulnerability of colorectal cancer

(2021) Sebastian M. Dieter et al.   Cell Reports

Unifying Catalysis Framework to Dissect Proteasomal Degradation Paradigms

(2021) Frances P. Rodriguez-Rivera et al.   ACS Central Science

PROTAC cell permeability and oral bioavailability: a journey into uncharted territory

(2021) Vasanthanathan Poongavanam et al.   Future Medicinal Chemistry

Proteolysis-Targeting Chimeras as Therapeutics and Tools for Biological Discovery

(2020) George M. Burslem et al.   CELL

Discovery of CRBN E3 Ligase Modulator CC-92480 for the Treatment of Relapsed and Refractory Multiple Myeloma

(2020) Joshua D. Hansen et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Cancer-Specific Ubiquitin Ligase Drives mRNA Alternative Polyadenylation by Ubiquitinating the mRNA 3′ End Processing Complex

(2020) Seung Wook Yang et al.   MOLECULAR CELL

Harnessing the Power of Proteolysis for Targeted Protein Inactivation

(2020) Rati Verma et al.   MOLECULAR CELL

NEDD8 nucleates a multivalent cullin–RING–UBE2D ubiquitin ligation assembly

(2020) Kheewoong Baek et al.   NATURE

bioPROTACs as versatile modulators of intracellular therapeutic targets including proliferating cell nuclear antigen (PCNA)

(2020) Shuhui Lim et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Small-molecule MDM2/X inhibitors and PROTAC degraders for cancer therapy: advances and perspectives

(2020) Yuan Fang et al.   Acta Pharmaceutica Sinica B

Prey for the Proteasome: Targeted Protein Degradation – A Medicinal Chemist´s Perspective

(2020) Laura M. Luh et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Drug Development and Medicinal Chemistry Efforts toward SARS‐Coronavirus and Covid‐19 Therapeutics

(2020) Arun K. Ghosh et al.   ChemMedChem

Discovery of PROTAC BCL-XL degraders as potent anticancer agents with low on-target platelet toxicity

(2020) Xuan Zhang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Investigational IRAK-4 inhibitors for the treatment of rheumatoid arthritis

(2020) Michael D. Wiese et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

First-in-human phase I study of ARV-110, an androgen receptor (AR) PROTAC degrader in patients (pts) with metastatic castrate-resistant prostate cancer (mCRPC) following enzalutamide (ENZ) and/or abiraterone (ABI).

(2020) Daniel Peter Petrylak et al.   JOURNAL OF CLINICAL ONCOLOGY

Multispecific drugs herald a new era of biopharmaceutical innovation

(2020) Raymond J. Deshaies   NATURE

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing

(2020) David E. Gordon et al.   NATURE

PROteolysis TArgeting Chimeras (PROTACs) as emerging anticancer therapeutics

(2020) Sajid Khan et al.   ONCOGENE

Structural basis for inhibition of the RNA-dependent RNA polymerase from SARS-CoV-2 by remdesivir

(2020) Wanchao Yin et al.   SCIENCE

Targeting the E3 ubiquitin ligases DCAF15 and cereblon for cancer therapy

(2020) Khai M. Nguyen et al.   SEMINARS IN CANCER BIOLOGY

Emerging New Concepts of Degrader Technologies

(2020) Yu Ding et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Viral gene delivery vectors: the next generation medicines for immune-related diseases

(2020) Peter De Haan et al.   Human Vaccines & Immunotherapeutics

A Nimbolide-Based Kinase Degrader Preferentially Degrades Oncogenic BCR-ABL

(2020) Bingqi Tong et al.   ACS Chemical Biology

Multiple Cereblon genetic changes associate with acquired resistance to Lenalidomide or Pomalidomide in Multiple Myeloma

(2020) Sarah Gooding et al.   BLOOD

Targeted protein degradation: current and future challenges

(2020) Alexander Hanzl et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Proteolysis targeting chimeras (PROTACs) are emerging therapeutics for hematologic malignancies

(2020) Yonghan He et al.   Journal of Hematology & Oncology

DT2216—a Bcl-xL-specific degrader is highly active against Bcl-xL-dependent T cell lymphomas

(2020) Yonghan He et al.   Journal of Hematology & Oncology

Lysosome-targeting chimaeras for degradation of extracellular proteins

(2020) Steven M. Banik et al.   NATURE

The CDK inhibitor CR8 acts as a molecular glue degrader that depletes cyclin K

(2020) Mikołaj Słabicki et al.   NATURE

Rational discovery of molecular glue degraders via scalable chemical profiling

(2020) Cristina Mayor-Ruiz et al.   Nature Chemical Biology

RAS-targeted therapies: is the undruggable drugged?

(2020) Amanda R. Moore et al.   NATURE REVIEWS DRUG DISCOVERY

Targeted protein degradation as a powerful research tool in basic biology and drug target discovery

(2020) Tao Wu et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Opportunities for Small Molecules in Cancer Immunotherapy

(2020) Sabina Y. van der Zanden et al.   TRENDS IN IMMUNOLOGY

Targeted Degradation of Oncogenic KRASG12C by VHL-Recruiting PROTACs

(2020) Michael J. Bond et al.   ACS Central Science

Strategies to Investigate Ubiquitination in Huntington's Disease

(2020) Karen A. Sap et al.   Frontiers in Chemistry

Hematopoietic Progenitor Kinase1 (HPK1) Mediates T Cell Dysfunction and Is a Druggable Target for T Cell-Based Immunotherapies

(2020) Jingwen Si et al.   CANCER CELL

Could PROTACs Protect Us From COVID-19?

(2020) Wilnelly Martinez-Ortiz et al.   DRUG DISCOVERY TODAY

Kinase inhibition in autoimmunity and inflammation

(2020) Ali A. Zarrin et al.   NATURE REVIEWS DRUG DISCOVERY

PROTAC-DB: an online database of PROTACs

(2020) Gaoqi Weng et al.   NUCLEIC ACIDS RESEARCH

Rapid and direct control of target protein levels with VHL-recruiting dTAG molecules

(2020) Behnam Nabet et al.   Nature Communications

RNA‐PROTACs: Degraders of RNA‐Binding Proteins

(2020) Alice Ghidini et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Tailored Bioorthogonal and Bioconjugate Chemistry: A Source of Inspiration for Developing Kinetic Target-Guided Synthesis Strategies

(2020) Alexis Lossouarn et al.   BIOCONJUGATE CHEMISTRY

CC-90009, a novel cereblon E3 ligase modulator targets acute myeloid leukemia blasts and leukemia stem cells

(2020) Christine Surka et al.   BLOOD

Mapping the Degradable Kinome Provides a Resource for Expedited Degrader Development

(2020) Katherine A. Donovan et al.   CELL

The TRIM9/TRIM67 neuronal interactome reveals novel activators of morphogenesis

(2020) Shalini Menon et al.   MOLECULAR BIOLOGY OF THE CELL

Snapshots and ensembles of BTK and cIAP1 protein degrader ternary complexes

(2020) James Schiemer et al.   Nature Chemical Biology

Solution Conformations Shed Light on PROTAC Cell Permeability

(2020) Yoseph Atilaw et al.   ACS Medicinal Chemistry Letters

Design, Synthesis, and Biological Evaluation of IRAK4-Targeting PROTACs

(2020) Yun Chen et al.   ACS Medicinal Chemistry Letters

Exquisitely Specific anti-KRAS Biodegraders Inform on the Cellular Prevalence of Nucleotide-Loaded States

(2020) Shuhui Lim et al.   ACS Central Science

Small-Molecule Approaches to Targeted Protein Degradation

(2020) Tyler B. Faust et al.   Annual Review of Cancer Biology-Series

Building ubiquitination machineries: E3 ligase multi-subunit assembly and substrate targeting by PROTACs and molecular glues

(2020) Sarath Ramachandran et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

NEDD8 and ubiquitin ligation by cullin-RING E3 ligases

(2020) Kheewoong Baek et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

Mechanisms of substrate recognition by the 26S proteasome

(2020) Caroline Davis et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

Prospective discovery of small molecule enhancers of an E3 ligase-substrate interaction

(2019) Kyle R. Simonetta et al.   Nature Communications

Matrix Mediated Viral Gene Delivery: A Review

(2019) Douglas Steinhauff et al.   BIOCONJUGATE CHEMISTRY

PROTAC-Mediated Degradation of Bruton’s Tyrosine Kinase Is Inhibited by Covalent Binding

(2019) Christopher P. Tinworth et al.   ACS Chemical Biology

Covalent Ligand Screening Uncovers a RNF4 E3 Ligase Recruiter for Targeted Protein Degradation Applications

(2019) Carl C. Ward et al.   ACS Chemical Biology

New Electrophiles and Strategies for Mechanism-Based and Targeted Covalent Inhibitor Design

(2019) Sneha Ray et al.   BIOCHEMISTRY

Targeting Nuclear Receptors with PROTAC degraders

(2019) John J. Flanagan et al.   MOLECULAR AND CELLULAR ENDOCRINOLOGY

Acquired Resistance to BET-PROTACs(Proteolysis Targeting Chimeras) Caused by Genomic Alterations in Core Components of E3 ligase Complexes

(2019) Lu Zhang et al.   MOLECULAR CANCER THERAPEUTICS

Targeted degradation of aberrant tau in frontotemporal dementia patient-derived neuronal cell models

(2019) M Catarina Silva et al.   eLife

Advances in targeted degradation of endogenous proteins

(2019) Sascha Röth et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

Harnessing the anti-cancer natural product nimbolide for targeted protein degradation

(2019) Jessica N. Spradlin et al.   Nature Chemical Biology

BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design

(2019) William Farnaby et al.   Nature Chemical Biology

Electrophilic PROTACs that degrade nuclear proteins by engaging DCAF16

(2019) Xiaoyu Zhang et al.   Nature Chemical Biology

Molecular mechanisms of cereblon-based drugs

(2019) Tomoko Asatsuma-Okumura et al.   PHARMACOLOGY & THERAPEUTICS

Targeting IRAK4 for Degradation with PROTACs

(2019) Joao Nunes et al.   ACS Medicinal Chemistry Letters

Small molecule degraders of the hepatitis C virus protease reduce susceptibility to resistance mutations

(2019) Mélissanne de Wispelaere et al.   Nature Communications

IKZF1/3 and CRL4-CRBN E3 ubiquitin ligase mutations and IMiD resistance in multiple myeloma

(2019) Santiago Barrio et al.   HAEMATOLOGICA

Development of targeted protein degradation therapeutics

(2019) Philip P. Chamberlain et al.   Nature Chemical Biology

Degradation of proteins by PROTACs and other strategies

(2019) Yang Wang et al.   Acta Pharmaceutica Sinica B

Cancer Testis Antigens in Sarcoma: Expression, Function and Immunotherapeutic Application

(2019) Ran Wei et al.   CANCER LETTERS

Antibody Conjugation of a Chimeric BET Degrader Enables in vivo Activity

(2019) Thomas H. Pillow et al.   ChemMedChem

The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity

(2019) Jude Canon et al.   NATURE

Allele-selective lowering of mutant HTT protein by HTT–LC3 linker compounds

(2019) Zhaoyang Li et al.   NATURE

Structural complementarity facilitates E7820-mediated degradation of RBM39 by DCAF15

(2019) Tyler B. Faust et al.   Nature Chemical Biology

Targeted protein degradation: expanding the toolbox

(2019) Matthieu Schapira et al.   NATURE REVIEWS DRUG DISCOVERY

Structural Basis and Kinetic Pathway of RBM39 Recruitment to DCAF15 by a Sulfonamide Molecular Glue E7820

(2019) Xinlin Du et al.   STRUCTURE

Evolution of Cereblon-Mediated Protein Degradation as a Therapeutic Modality

(2019) Philip P. Chamberlain et al.   ACS Medicinal Chemistry Letters

Structural basis of Cullin 2 RING E3 ligase regulation by the COP9 signalosome

(2019) Sarah V. Faull et al.   Nature Communications

The KRASG12C Inhibitor MRTX849 Provides Insight toward Therapeutic Susceptibility of KRAS-Mutant Cancers in Mouse Models and Patients

(2019) Jill Hallin et al.   Cancer Discovery

Aryl Sulfonamides Degrade RBM39 and RBM23 by Recruitment to CRL4-DCAF15

(2019) Tabitha C. Ting et al.   Cell Reports

AUTACs: Cargo-Specific Degraders Using Selective Autophagy

(2019) Daiki Takahashi et al.   MOLECULAR CELL

Structural basis of indisulam-mediated RBM39 recruitment to DCAF15 E3 ligase complex

(2019) Dirksen E. Bussiere et al.   Nature Chemical Biology

A selective BCL-XL PROTAC degrader achieves safe and potent antitumor activity

(2019) Sajid Khan et al.   NATURE MEDICINE

Targeted Protein Degradation by Chimeric Small Molecules, PROTACs and SNIPERs

(2019) Mikihiko Naito et al.   Frontiers in Chemistry

Targeting the C481S Ibrutinib-Resistance Mutation in Bruton’s Tyrosine Kinase Using PROTAC-Mediated Degradation

(2018) Alexandru D. Buhimschi et al.   BIOCHEMISTRY

Practical application of ligand efficiency metrics in lead optimisation

(2018) James S. Scott et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Targeting KRAS Mutant Cancers with a Covalent G12C-Specific Inhibitor

(2018) Matthew R. Janes et al.   CELL

PROTAC-induced BTK degradation as a novel therapy for mutated BTK C481S induced ibrutinib-resistant B-cell malignancies

(2018) Yonghui Sun et al.   CELL RESEARCH

Discovery of a Keap1-dependent peptide PROTAC to knockdown Tau by ubiquitination-proteasome degradation pathway

(2018) Mengchen Lu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Mapping the Efficiency and Physicochemical Trajectories of Successful Optimizations

(2018) Robert J. Young et al.   JOURNAL OF MEDICINAL CHEMISTRY

Lipophilic Efficiency as an Important Metric in Drug Design

(2018) Ted W. Johnson et al.   JOURNAL OF MEDICINAL CHEMISTRY

The dTAG system for immediate and target-specific protein degradation

(2018) Behnam Nabet et al.   Nature Chemical Biology

Plasticity in binding confers selectivity in ligand-induced protein degradation

(2018) Radosław P. Nowak et al.   Nature Chemical Biology

Delineating the role of cooperativity in the design of potent PROTACs for BTK

(2018) Adelajda Zorba et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Principles of Ubiquitin-Dependent Signaling

(2018) Eugene Oh et al.   Annual Review of Cell and Developmental Biology

Early Clinical PET Imaging Results with the Novel PHF-Tau Radioligand [F-18]-T807

(2018) David T. Chien et al.   JOURNAL OF ALZHEIMERS DISEASE

Two Decades under the Influence of the Rule of Five and the Changing Properties of Approved Oral Drugs

(2018) Michael D. Shultz   JOURNAL OF MEDICINAL CHEMISTRY

Thalidomide promotes degradation of SALL4, a transcription factor implicated in Duane Radial Ray syndrome

(2018) Katherine A Donovan et al.   eLife

UbiHub: a data hub for the explorers of ubiquitination pathways

(2018) Lihua Liu et al.   BIOINFORMATICS

Bruton's Tyrosine Kinase degradation as a therapeutic strategy for cancer

(2018) Dennis Dobrovolsky et al.   BLOOD

Genome-wide CRISPR Screens in Primary Human T Cells Reveal Key Regulators of Immune Function

(2018) Eric Shifrut et al.   CELL

The Next Generation of Immunotherapy for Cancer: Small Molecules Could Make Big Waves

(2018) William G. Kerr et al.   JOURNAL OF IMMUNOLOGY

Defining the human C2H2 zinc finger degrome targeted by thalidomide analogs through CRBN

(2018) Quinlan L. Sievers et al.   SCIENCE

Molecular recognition of ternary complexes: a new dimension in the structure-guided design of chemical degraders

(2017) Scott J. Hughes et al.   Essays in Biochemistry

A Cereblon Modulator (CC-220) with Improved Degradation of Ikaros and Aiolos

(2017) Mary E. Matyskiela et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Comprehensive Guide to the MAGE Family of Ubiquitin Ligases

(2017) Anna K. Lee et al.   JOURNAL OF MOLECULAR BIOLOGY

Selective degradation of splicing factor CAPERα by anticancer sulfonamides

(2017) Taisuke Uehara et al.   Nature Chemical Biology

Structural basis of PROTAC cooperative recognition for selective protein degradation

(2017) Morgan S Gadd et al.   Nature Chemical Biology

Targeted protein degradation by PROTACs

(2017) Taavi K. Neklesa et al.   PHARMACOLOGY & THERAPEUTICS

Anticancer sulfonamides target splicing by inducing RBM39 degradation via recruitment to DCAF15

(2017) Ting Han et al.   SCIENCE

Tau reduction prevents neuronal loss and reverses pathological tau deposition and seeding in mice with tauopathy

(2017) Sarah L. DeVos et al.   Science Translational Medicine

Structural Studies of HHARI/UbcH7∼Ub Reveal Unique E2∼Ub Conformational Restriction by RBR RING1

(2017) Katja K. Dove et al.   STRUCTURE

Two Distinct Types of E3 Ligases Work in Unison to Regulate Substrate Ubiquitylation

(2016) Daniel C. Scott et al.   CELL

System-Wide Modulation of HECT E3 Ligases with Selective Ubiquitin Variant Probes

(2016) Wei Zhang et al.   MOLECULAR CELL

A novel cereblon modulator recruits GSPT1 to the CRL4CRBN ubiquitin ligase

(2016) Mary E. Matyskiela et al.   NATURE

Structure of the E6/E6AP/p53 complex required for HPV-mediated degradation of p53

(2016) Denise Martinez-Zapien et al.   NATURE

Allosteric inhibition of SHP2 phosphatase inhibits cancers driven by receptor tyrosine kinases

(2016) Ying-Nan P. Chen et al.   NATURE

Structural basis of lenalidomide-induced CK1α degradation by the CRL4CRBN ubiquitin ligase

(2016) Georg Petzold et al.   NATURE

The increasing complexity of the ubiquitin code

(2016) Richard Yau et al.   NATURE CELL BIOLOGY

The DDB1–DCAF1–Vpr–UNG2 crystal structure reveals how HIV-1 Vpr steers human UNG2 toward destruction

(2016) Ying Wu et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Tripartite degrons confer diversity and specificity on regulated protein degradation in the ubiquitin-proteasome system

(2016) Mainak Guharoy et al.   Nature Communications

The DDB1–DCAF1–Vpr–UNG2 crystal structure reveals how HIV-1 Vpr steers human UNG2 toward destruction

(2016) Ying Wu et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

A recombinant chimeric protein specifically induces mutant KRAS degradation and potently inhibits pancreatic tumor growth

(2016) Ting Pan et al.   Oncotarget

An affinity-directed protein missile system for targeted proteolysis

(2016) Luke J. Fulcher et al.   Open Biology

HaloPROTACS: Use of Small Molecule PROTACs to Induce Degradation of HaloTag Fusion Proteins

(2015) Dennis L. Buckley et al.   ACS Chemical Biology

Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4

(2015) Michael Zengerle et al.   ACS Chemical Biology

Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL

(2015) Ashton C. Lai et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Degradation of AMPK by a Cancer-Specific Ubiquitin Ligase

(2015) Carlos T. Pineda et al.   CELL

The MAGE protein family and cancer

(2015) Jenny L Weon et al.   CURRENT OPINION IN CELL BIOLOGY

Comparison of plant hormone signalling systems

(2015) A. Larrieu et al.   Essays in Biochemistry

Oral Selective Estrogen Receptor Downregulators (SERDs), a Breakthrough Endocrine Therapy for Breast Cancer

(2015) Donald P. McDonnell et al.   JOURNAL OF MEDICINAL CHEMISTRY

Lenalidomide induces ubiquitination and degradation of CK1α in del(5q) MDS

(2015) Jan Krönke et al.   NATURE

Catalytic in vivo protein knockdown by small-molecule PROTACs

(2015) Daniel P Bondeson et al.   Nature Chemical Biology

Tau in physiology and pathology

(2015) Yipeng Wang et al.   NATURE REVIEWS NEUROSCIENCE

The Structural Differences between a Glycoprotein Specific F-Box Protein Fbs1 and Its Homologous Protein FBG3

(2015) Taichi Kumanomidou et al.   PLoS One

Oral Druggable Space beyond the Rule of 5: Insights from Drugs and Clinical Candidates

(2014) Bradley Croy Doak et al.   CHEMISTRY & BIOLOGY

KLHL40 deficiency destabilizes thin filament proteins and promotes nemaline myopathy

(2014) Ankit Garg et al.   JOURNAL OF CLINICAL INVESTIGATION

E3 ubiquitin ligases and human papillomavirus-induced carcinogenesis

(2014) Zhifeng Lou et al.   JOURNAL OF INTERNATIONAL MEDICAL RESEARCH

Structure of the DDB1–CRBN E3 ubiquitin ligase in complex with thalidomide

(2014) Eric S. Fischer et al.   NATURE

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

(2014) Yingying Guo et al.   NATURE

Identification of KLHL41 Mutations Implicates BTB-Kelch-Mediated Ubiquitination as an Alternate Pathway to Myofibrillar Disruption in Nemaline Myopathy

(2013) Vandana A. Gupta et al.   AMERICAN JOURNAL OF HUMAN GENETICS

Immunomodulatory agents lenalidomide and pomalidomide co-stimulate T cells by inducing degradation of T cell repressors Ikaros and Aiolos via modulation of the E3 ubiquitin ligase complex CRL4CRBN

(2013) Anita K. Gandhi et al.   BRITISH JOURNAL OF HAEMATOLOGY

Targeted Degradation of KRAS by an Engineered Ubiquitin Ligase Suppresses Pancreatic Cancer Cell Growth In Vitro and In Vivo

(2013) Y. Ma et al.   MOLECULAR CANCER THERAPEUTICS

K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions

(2013) Jonathan M. Ostrem et al.   NATURE

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

Mechanism of ubiquitin ligation and lysine prioritization by a HECT E3

(2013) Hari B Kamadurai et al.   eLife

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

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

The Ubiquitin Code

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

Structural Insights into the Conformation and Oligomerization of E2∼Ubiquitin Conjugates

(2012) Richard C. Page et al.   BIOCHEMISTRY

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

Structural regulation of cullin-RING ubiquitin ligase complexes

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

Fluorescent fusion protein knockout mediated by anti-GFP nanobody

(2011) Emmanuel Caussinus et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Structural assembly of cullin-RING ubiquitin ligase complexes

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

Roles of Vpr and Vpx in modulating the virus-host cell relationship

(2010) Vicente Planelles et al.   MOLECULAR ASPECTS OF MEDICINE

Impact of linker length on the activity of PROTACs

(2010) Kedra Cyrus et al.   Molecular BioSystems

Identification of a Primary Target of Thalidomide Teratogenicity

(2010) T. Ito et al.   SCIENCE

Bioorthogonal Chemistry: Fishing for Selectivity in a Sea of Functionality

(2009) Ellen M. Sletten et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Diversity in Tissue Expression, Substrate Binding, and SCF Complex Formation for a Lectin Family of Ubiquitin Ligases

(2008) Kevin A. Glenn et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

A novel brain-enriched E3 ubiquitin ligase RNF182 is up regulated in the brains of Alzheimer's patients and targets ATP6V0C for degradation

(2008) Qing Liu et al.   Molecular Neurodegeneration