Mathematical Model for Covalent Proteolysis Targeting Chimeras: Thermodynamics and Kinetics Underlying Catalytic Efficiency

Discovery of a Covalent FEM1B Recruiter for Targeted Protein Degradation Applications

(2022) Nathaniel J. Henning et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Targeted Protein Degradation by Electrophilic PROTACs that Stereoselectively and Site-Specifically Engage DCAF1

(2022) Yongfeng Tao et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Targeted protein degraders crowd into the clinic

(2021) Asher Mullard   NATURE REVIEWS DRUG DISCOVERY

Ligandability of E3 Ligases for Targeted Protein Degradation Applications

(2021) Bridget P. Belcher et al.   BIOCHEMISTRY

The rise of covalent proteolysis targeting chimeras

(2021) Ronen Gabizon et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity

(2021) Satomi Imaide et al.   Nature Chemical Biology

Efficient Targeted Degradation via Reversible and Irreversible Covalent PROTACs

(2020) Ronen Gabizon et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

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

(2020) Bingqi Tong et al.   ACS Chemical Biology

Targeted Degradation of Oncogenic KRASG12C by VHL-Recruiting PROTACs

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

A suite of mathematical solutions to describe ternary complex formation and their application to targeted protein degradation by hetero-bifunctional ligands

(2020) Bomie Han   JOURNAL OF BIOLOGICAL CHEMISTRY

A kinetic proofreading model for bispecific protein degraders

(2020) Derek W. Bartlett et al.   JOURNAL OF PHARMACOKINETICS AND PHARMACODYNAMICS

Enhancing intracellular accumulation and target engagement of PROTACs with reversible covalent chemistry

(2020) Wen-Hao Guo et al.   Nature Communications

Bardoxolone conjugation enables targeted protein degradation of BRD4

(2020) Bingqi Tong et al.   Scientific Reports

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

Proteolysis targeting chimeras (PROTACs) in ‘beyond rule-of-five’ chemical space: Recent progress and future challenges

(2019) Scott D. Edmondson et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Targeted protein degradation: elements of PROTAC design

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

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

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

Electrophilic PROTACs that degrade nuclear proteins by engaging DCAF16

(2019) Xiaoyu Zhang et al.   Nature Chemical Biology

Development of targeted protein degradation therapeutics

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

Enzymatic Logic of Ubiquitin Chain Assembly

(2019) Kirandeep K. Deol et al.   Frontiers in Physiology

Targeted protein degradation and the enzymology of degraders

(2018) Stewart L Fisher et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

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

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

(2017) Ian Churcher   JOURNAL OF MEDICINAL CHEMISTRY

Structural basis of PROTAC cooperative recognition for selective protein degradation

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

Kinetic Analysis of Protein Stability Reveals Age-Dependent Degradation

(2016) Erik McShane et al.   CELL

The increasing complexity of the ubiquitin code

(2016) Richard Yau et al.   NATURE CELL BIOLOGY

Catalytic in vivo protein knockdown by small-molecule PROTACs

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

A Comprehensive Mathematical Model for Three-Body Binding Equilibria

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

Stalled Proteasomes Are Directly Relieved by P97 Recruitment

(2011) Elada Isakov et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Ubiquitin: Same Molecule, Different Degradation Pathways

(2010) Michael J. Clague et al.   CELL

Detection of sequential polyubiquitylation on a millisecond timescale

(2009) Nathan W. Pierce et al.   NATURE