Mapping the Degradable Kinome Provides a Resource for Expedited Degrader Development

Proteolysis-Targeting Chimeras as Therapeutics and Tools for Biological Discovery

(2020) George M. Burslem et al.   CELL

CSK promotes innate immune response to DNA virus by phosphorylating MITA

(2020) Peng Gao et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Critical Assessment of Targeted Protein Degradation as a Research Tool and Pharmacological Modality

(2020) Milka Kostic et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Tubulin Resists Degradation by Cereblon-Recruiting PROTACs

(2020) Ivana Gasic et al.   Cells

Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase

(2019) Blake E. Smith et al.   Nature Communications

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

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

Properties of FDA-approved small molecule protein kinase inhibitors

(2019) Robert Roskoski   PHARMACOLOGICAL RESEARCH

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

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

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

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

(2019) M Catarina Silva et al.   eLife

Targeted protein degradation: elements of PROTAC design

(2019) Stacey-Lynn Paiva et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Development of Multifunctional Histone Deacetylase 6 Degraders with Potent Antimyeloma Activity

(2019) Hao Wu et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

Properties of FDA-approved small molecule protein kinase inhibitors: A 2020 update

(2019) Robert Roskoski   PHARMACOLOGICAL RESEARCH

Pervasive Protein Thermal Stability Variation during the Cell Cycle

(2018) Isabelle Becher et al.   CELL

Quantitative metrics for drug–target ligandability

(2018) Sinisa Vukovic et al.   DRUG DISCOVERY TODAY

Phthalimide conjugations for the degradation of oncogenic PI3K

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

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

Peptide Level Turnover Measurements Enable the Study of Proteoform Dynamics

(2018) Jana Zecha et al.   MOLECULAR & CELLULAR PROTEOMICS

Plasticity in binding confers selectivity in ligand-induced protein degradation

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

Unexplored therapeutic opportunities in the human genome

(2018) Tudor I. Oprea et al.   NATURE REVIEWS DRUG DISCOVERY

Glimmers in illuminating the druggable genome

(2018) Griffin Rodgers et al.   NATURE REVIEWS DRUG DISCOVERY

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

Systematic analysis of protein turnover in primary cells

(2018) Toby Mathieson et al.   Nature Communications

Chemically induced degradation of CK2 by proteolysis targeting chimeras based on a ubiquitin–proteasome pathway

(2018) Hong Chen et al.   BIOORGANIC CHEMISTRY

Structural Basis for Regulation of Phosphoinositide Kinases and Their Involvement in Human Disease

(2018) John E. Burke   MOLECULAR CELL

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

(2018) Katherine A Donovan et al.   eLife

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

(2018) Dennis Dobrovolsky et al.   BLOOD

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

(2018) John Hines et al.   CANCER RESEARCH

Addressing Kinase-Independent Functions of Fak via PROTAC-Mediated Degradation

(2018) Philipp M. Cromm et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

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

(2018) Quinlan L. Sievers et al.   SCIENCE

Protein degradation: a validated therapeutic strategy with exciting prospects

(2017) Honorine Lebraud et al.   Essays in Biochemistry

In VivoKnockdown of Pathogenic Proteins via Specific and Nongenetic Inhibitor of Apoptosis Protein (IAP)-dependent Protein Erasers (SNIPERs)

(2017) Nobumichi Ohoka et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds

(2017) Kwok-Ho Chan et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2017) Ian Churcher   JOURNAL OF MEDICINAL CHEMISTRY

Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation

(2017) Calla M Olson 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

PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer

(2016) Kanak Raina et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4

(2015) Jing Lu et al.   CHEMISTRY & BIOLOGY

DISEASES: Text mining and data integration of disease–gene associations

(2015) Sune Pletscher-Frankild et al.   METHODS

Catalytic in vivo protein knockdown by small-molecule PROTACs

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

limma powers differential expression analyses for RNA-sequencing and microarray studies

(2015) Matthew E. Ritchie et al.   NUCLEIC ACIDS RESEARCH

Phthalimide conjugation as a strategy for in vivo target protein degradation

(2015) G. E. Winter et al.   SCIENCE

MultiNotch MS3 Enables Accurate, Sensitive, and Multiplexed Detection of Differential Expression across Cancer Cell Line Proteomes

(2014) Graeme C. McAlister et al.   ANALYTICAL CHEMISTRY

QuasR: quantification and annotation of short reads in R

(2014) Dimos Gaidatzis et al.   BIOINFORMATICS

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

A Comprehensive Mathematical Model for Three-Body Binding Equilibria

(2013) Eugene F. Douglass et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

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

(2013) J. Kronke et al.   SCIENCE

Discovery of Dabrafenib: A Selective Inhibitor of Raf Kinases with Antitumor Activity against B-Raf-Driven Tumors

(2013) Tara R. Rheault et al.   ACS Medicinal Chemistry Letters

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

Affinity-purification coupled to mass spectrometry: Basic principles and strategies

(2012) Wade H. Dunham et al.   PROTEOMICS

Specific degradation of CRABP-II via cIAP1-mediated ubiquitylation induced by hybrid molecules that crosslink cIAP1 and the target protein

(2011) Keiichiro Okuhira et al.   FEBS LETTERS

Cdc48/p97 Mediates UV-Dependent Turnover of RNA Pol II

(2011) Rati Verma et al.   MOLECULAR CELL

Comprehensive analysis of kinase inhibitor selectivity

(2011) Mindy I Davis et al.   NATURE BIOTECHNOLOGY

Technological Innovation Leads to Fundamental Understanding in Cell Biology

(2010) David Botstein   MOLECULAR BIOLOGY OF THE CELL

Identification of a Primary Target of Thalidomide Teratogenicity

(2010) T. Ito et al.   SCIENCE

edgeR: a Bioconductor package for differential expression analysis of digital gene expression data

(2009) M. D. Robinson et al.   BIOINFORMATICS

A quantitative analysis of kinase inhibitor selectivity

(2008) Mazen W Karaman et al.   NATURE BIOTECHNOLOGY