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

Optical Control of Small Molecule-Induced Protein Degradation

(2020) Yuta Naro et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

A Small Molecule-Controlled Cas9 Repressible System

(2020) Youjun Wu et al.   Molecular Therapy-Nucleic Acids

Light-induced control of protein destruction by opto-PROTAC

(2020) Jing Liu et al.   Science Advances

Azo-PROTAC: Novel Light-Controlled Small-Molecule Tool for Protein Knockdown

(2020) Yu-Hui Jin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Combining scaling relationships overcomes rate versus overpotential trade-offs in O2 molecular electrocatalysis

(2020) Daniel J. Martin et al.   Science Advances

Chk1-mediated Cdc25A degradation as a critical mechanism for normal cell-cycle progression

(2019) Hidemasa Goto et al.   JOURNAL OF CELL SCIENCE

Peptidic degron for IMiD-induced degradation of heterologous proteins

(2019) Vidyasagar Koduri et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Development of Dual and Selective Degraders of Cyclin-Dependent Kinases 4 and 6

(2019) Baishan Jiang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

SPR-Measured Dissociation Kinetics of PROTAC Ternary Complexes Influence Target Degradation Rate

(2019) Michael J. Roy et al.   ACS Chemical Biology

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

Rapid and Reversible Knockdown of Endogenously Tagged Endosomal Proteins via an Optimized HaloPROTAC Degrader

(2019) Hannah Tovell et al.   ACS Chemical Biology

Accumulation of PNPLA3 on lipid droplets is the basis of associated hepatic steatosis

(2019) Soumik BasuRay et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

HsSAS-6-dependent cartwheel assembly ensures stabilization of centriole intermediates

(2019) Satoko Yoshiba et al.   JOURNAL OF CELL SCIENCE

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

An efficient auxin-inducible degron system with low basal degradation in human cells

(2019) Shiqian Li et al.   NATURE METHODS

Illustrate: Software for Biomolecular Illustration

(2019) David S. Goodsell et al.   STRUCTURE

Reversible Spatiotemporal Control of Induced Protein Degradation by Bistable PhotoPROTACs

(2019) Patrick Pfaff et al.   ACS Central Science

Light-Induced Protein Degradation with Photocaged PROTACs

(2019) Gang Xue et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Structural complementarity facilitates E7820-mediated degradation of RBM39 by DCAF15

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

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

(2019) Xinlin Du et al.   STRUCTURE

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

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

Condensin locates at transcriptional termination sites in mitosis, possibly releasing mitotic transcripts

(2019) Norihiko Nakazawa et al.   Open Biology

pSILAC method coupled with two complementary digestion approaches reveals PRPF39 as a new E7070-dependent DCAF15 substrate

(2019) Xinglong Jia et al.   Journal of Proteomics

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

Development of the first small molecule histone deacetylase 6 (HDAC6) degraders

(2018) Ka Yang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Phthalimide conjugations for the degradation of oncogenic PI3K

(2018) Wenlu Li et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

In Vivo Assessment of the Effect of CYP1A2 Inhibition and Induction on Pomalidomide Pharmacokinetics in Healthy Subjects

(2018) Yan Li et al.   JOURNAL OF CLINICAL PHARMACOLOGY

Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766)

(2018) Nicola E. A. Chessum 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

A small-molecule inhibitor of the ubiquitin activating enzyme for cancer treatment

(2018) Marc L Hyer et al.   NATURE MEDICINE

Chaperone-mediated autophagy: Advances from bench to bedside

(2018) Wenming Li et al.   NEUROBIOLOGY OF DISEASE

Modulating PCAF/GCN5 Immune Cell Function through a PROTAC Approach

(2018) Zuni I. Bassi et al.   ACS Chemical Biology

Quantitative Live-Cell Kinetic Degradation and Mechanistic Profiling of PROTAC Mode of Action

(2018) Kristin M. Riching et al.   ACS Chemical Biology

CrbnI391Vis sufficient to conferin vivosensitivity to thalidomide and its derivatives in mice

(2018) Emma C. Fink et al.   BLOOD

Mutant NPM1 Maintains the Leukemic State through HOX Expression

(2018) Lorenzo Brunetti et al.   CANCER CELL

SALL4 mediates teratogenicity as a thalidomide-dependent cereblon substrate

(2018) Mary E. Matyskiela et al.   Nature Chemical Biology

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

(2018) Katherine A Donovan et al.   eLife

Degron mediated BRM/SMARCA2 depletion uncovers novel combination partners for treatment of BRG1/SMARCA4-mutant cancers

(2018) Florencia Rago et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

MDM2-Recruiting PROTAC Offers Superior, Synergistic Antiproliferative Activity via Simultaneous Degradation of BRD4 and Stabilization of p53

(2018) John Hines et al.   CANCER RESEARCH

Transcription Factors Activate Genes through the Phase-Separation Capacity of Their Activation Domains

(2018) Ann Boija et al.   CELL

Enhancing Antiproliferative Activity and Selectivity of a FLT-3 Inhibitor by Proteolysis Targeting Chimera Conversion

(2018) George M. Burslem et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Humanized cereblon mice revealed two distinct therapeutic pathways of immunomodulatory drugs

(2018) Yohannes Gemechu et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

(2018) Quinlan L. Sievers et al.   SCIENCE

Protac-Induced Protein Degradation in Drug Discovery: Breaking the Rules or Just Making New Ones?

(2017) Ian Churcher   JOURNAL OF MEDICINAL CHEMISTRY

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

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

Transcription control by the ENL YEATS domain in acute leukaemia

(2017) Michael A. Erb et al.   NATURE

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

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

(2017) Ting Han et al.   SCIENCE

Waste disposal—An attractive strategy for cancer therapy

(2017) Jemilat Salami et al.   SCIENCE

MELK is not necessary for the proliferation of basal-like breast cancer cells

(2017) Hai-Tsang Huang et al.   eLife

Clinical Pharmacokinetics and Pharmacodynamics of Lenalidomide

(2016) Nianhang Chen et al.   CLINICAL PHARMACOKINETICS

A novel cereblon modulator recruits GSPT1 to the CRL4CRBN ubiquitin ligase

(2016) Mary E. Matyskiela et al.   NATURE

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

(2016) Georg Petzold et al.   NATURE

Targeted inhibition of the COP9 signalosome for treatment of cancer

(2016) Anita Schlierf et al.   Nature Communications

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

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

CC-122, a pleiotropic pathway modifier, mimics an interferon response and has antitumor activity in DLBCL

(2015) P. R. Hagner et al.   BLOOD

Targeting the AAA ATPase p97 as an Approach to Treat Cancer through Disruption of Protein Homeostasis

(2015) Daniel J. Anderson et al.   CANCER CELL

Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4

(2015) Jing Lu et al.   CHEMISTRY & BIOLOGY

Tunable and reversible drug control of protein production via a self-excising degron

(2015) Hokyung K Chung et al.   Nature Chemical Biology

Catalytic in vivo protein knockdown by small-molecule PROTACs

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

Degradation of HaloTag-fused nuclear proteins using bestatin-HaloTag ligand hybrid molecules

(2015) Shusuke Tomoshige et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Phthalimide conjugation as a strategy for in vivo target protein degradation

(2015) G. E. Winter et al.   SCIENCE

Engineering FKBP-Based Destabilizing Domains to Build Sophisticated Protein Regulation Systems

(2015) Wenlin An et al.   PLoS One

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

(2014) Eric S. Fischer et al.   NATURE

Targeted protein destabilization reveals an estrogen-mediated ER stress response

(2014) Kanak Raina et al.   Nature Chemical Biology

Rapid and reversible knockdown of endogenous proteins by peptide-directed lysosomal degradation

(2014) Xuelai Fan et al.   NATURE NEUROSCIENCE

Lenalidomide induces degradation of IKZF1 and IKZF3

(2014) Jan Krönke et al.   OncoImmunology

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

A LOV2 Domain-Based Optogenetic Tool to Control Protein Degradation and Cellular Function

(2013) Christian Renicke et al.   CHEMISTRY & BIOLOGY

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

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

The application and biology of immunomodulatory drugs (IMiDs) in cancer

(2012) Beiqing Pan et al.   PHARMACOLOGY & THERAPEUTICS

Global Identification of Modular Cullin-RING Ligase Substrates

(2011) Michael J. Emanuele et al.   CELL

Small-molecule hydrophobic tagging–induced degradation of HaloTag fusion proteins

(2011) Taavi K Neklesa et al.   Nature Chemical Biology

Fluorescent fusion protein knockout mediated by anti-GFP nanobody

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

Protein Knockdown Using Methyl Bestatin−Ligand Hybrid Molecules: Design and Synthesis of Inducers of Ubiquitination-Mediated Degradation of Cellular Retinoic Acid-Binding Proteins

(2010) Yukihiro Itoh et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Jasmonate perception by inositol-phosphate-potentiated COI1–JAZ co-receptor

(2010) Laura B. Sheard et al.   NATURE

Identification of a Primary Target of Thalidomide Teratogenicity

(2010) T. Ito et al.   SCIENCE

Efficient protection and isolation of ubiquitylated proteins using tandem ubiquitin-binding entities

(2009) Roland Hjerpe et al.   EMBO REPORTS

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

Regulated expression of the Leishmania major surface virulence factor lipophosphoglycan using conditionally destabilized fusion proteins

(2009) L. Madeira da Silva et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

HaloTag: A Novel Protein Labeling Technology for Cell Imaging and Protein Analysis

(2008) Georgyi V. Los et al.   ACS Chemical Biology

Structural elements of the ubiquitin-independent proteasome degron of ornithine decarboxylase

(2008) Junko Takeuchi et al.   BIOCHEMICAL JOURNAL