D. Dovala

A small molecule VHL molecular glue degrader for cysteine dioxygenase 1

The paper identifies a small molecule that acts as a molecular glue degrader for CDO1 by recruiting it into the VHL E3 ligase complex, leading to its degradation.

Contributions of hyperactive mutations in Mpro from SARS-CoV-2 to drug resistance

This study identifies hyperactive mutations in SARS-CoV-2 Mpro that increase enzyme activity and contribute to drug resistance, finding them more prevalent than binding-reducing mutations.

Ophiobolin A Covalently Targets Complex IV Leading to Mitochondrial Metabolic Collapse in Cancer Cells

This study identifies Ophiobolin A's covalent targets in complex IV of mitochondria, revealing a mechanism of metabolic collapse and cell death in cancer cells.

Crystal Structures of Inhibitor-Bound Main Protease from Delta- and Gamma-Coronaviruses

The paper determines inhibitor-bound crystal structures of main proteases from delta and gamma coronaviruses to inform structure-based inhibitor design.

Targeted Protein Degradation through E2 Recruitment

This study identifies a covalent recruiter for the E2 ubiquitin conjugating enzyme UBE2D, enabling targeted protein degradation via PROTACs.

Rational Chemical Design of Molecular Glue Degraders

This paper develops a strategy to convert protein-targeting ligands into molecular glue degraders by identifying a covalent handle that induces proteasome-mediated degradation of target proteins.

Chemoproteomics-Enabled Discovery of a Covalent Molecular Glue Degrader Targeting NF-κB

This study identifies a covalent molecular glue degrader, EN450, that induces the degradation of NFKB1 via a ternary complex with UBE2D, leading to anti-proliferative effects in leukemia cells.

Discovery of Potent Pyrazoline-Based Covalent SARS-CoV-2 Main Protease Inhibitors

This study identifies and optimizes potent pyrazoline-based covalent inhibitors of SARS-CoV-2 Mpro, showing activity against multiple coronaviruses.

Defining the Substrate Envelope of SARS-CoV-2 Main Protease to Predict and Avoid Drug Resistance

This study defines the substrate envelope of SARS-CoV-2 main protease using cocrystal structures to identify vulnerable sites that may lead to drug resistance.

Deubiquitinase-Targeting Chimeras for Targeted Protein Stabilization

This paper introduces the DUBTAC platform for targeted protein stabilization by linking a covalent OTUB1 recruiter to lumacaftor, demonstrating stabilization of ΔF508-CFTR in human cells.

Screening a library of FDA-approved and bioactive compounds for antiviral activity against SARS-CoV-2

This study screens FDA-approved compounds for antiviral activity against SARS-CoV-2 and identifies 13 effective compounds, including seven new candidates and one synergistic combination with remdesivir.