Discovery of proteolysis-targeting chimera targeting undruggable proteins using a covalent ligand screening approach

Discovery of High-Affinity Amyloid Ligands Using a Ligand-Based Virtual Screening Pipeline

(2023) Timothy S. Chisholm et al.   Journal of the American Chemical Society

Pharmacophore-Based Machine Learning Model To Predict Ligand Selectivity for E3 Ligase Binders

(2023) Reagon Karki et al.   ACS Omega

PROTAC targeted protein degraders: the past is prologue

(2022) Miklós Békés et al.   NATURE REVIEWS DRUG DISCOVERY

Proteolysis-Targeting Chimeras as Therapeutics and Tools for Biological Discovery

(2020) George M. Burslem et al.   CELL

Crystallographic and electrophilic fragment screening of the SARS-CoV-2 main protease

(2020) Alice Douangamath et al.   Nature Communications

Rapid covalent-probe discovery by electrophile-fragment screening

(2019) Efrat Resnick et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

LC-MS bioanalysis of intact proteins and peptides

(2019) Lijuan Kang et al.   BIOMEDICAL CHROMATOGRAPHY

Comparison of Cytotoxicity Evaluation of Anticancer Drugs between Real-Time Cell Analysis and CCK-8 Method

(2019) Ling Cai et al.   ACS Omega

Structural basis of thalidomide enantiomer binding to cereblon

(2018) Tomoyuki Mori et al.   Scientific Reports

Structural analyses reveal the mechanism of inhibition of influenza virus NS1 by two antiviral compounds

(2018) Alex B. Kleinpeter et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Discovery of MD-224 as a First-in-Class, Highly Potent, and Efficacious Proteolysis Targeting Chimera Murine Double Minute 2 Degrader Capable of Achieving Complete and Durable Tumor Regression

(2018) Yangbing Li et al.   JOURNAL OF MEDICINAL CHEMISTRY

1,4,5-Trisubstituted Imidazole-Based p53–MDM2/MDMX Antagonists with Aliphatic Linkers for Conjugation with Biological Carriers

(2017) Aleksandra Twarda-Clapa et al.   JOURNAL OF MEDICINAL CHEMISTRY

Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4

(2015) Jing Lu et al.   CHEMISTRY & BIOLOGY

Phthalimide conjugation as a strategy for in vivo target protein degradation

(2015) G. E. Winter et al.   SCIENCE

A Fragment-Based Method to Discover Irreversible Covalent Inhibitors of Cysteine Proteases

(2014) Stefan G. Kathman et al.   JOURNAL OF MEDICINAL CHEMISTRY

The structure of an MDM2–Nutlin-3a complex solved by the use of a validated MDM2 surface-entropy reduction mutant

(2013) Burcu Anil et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

A Comprehensive Mathematical Model for Three-Body Binding Equilibria

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

Using chemical shift perturbation to characterise ligand binding

(2013) Mike P. Williamson   PROGRESS IN NUCLEAR MAGNETIC RESONANCE SPECTROSCOPY

Transient Protein States in Designing Inhibitors of the MDM2-p53 Interaction

(2013) Michal Bista et al.   STRUCTURE

MG132, a proteasome inhibitor, induces apoptosis in tumor cells

(2012) Na GUO et al.   Asia-Pacific Journal of Clinical Oncology

The Nedd8-Activating Enzyme Inhibitor MLN4924 Induces Autophagy and Apoptosis to Suppress Liver Cancer Cell Growth

(2012) Z. Luo et al.   CANCER RESEARCH

Cereblon is a direct protein target for immunomodulatory and antiproliferative activities of lenalidomide and pomalidomide

(2012) A Lopez-Girona et al.   LEUKEMIA

Platform-independent and Label-free Quantitation of Proteomic Data Using MS1 Extracted Ion Chromatograms in Skyline

(2012) Birgit Schilling et al.   MOLECULAR & CELLULAR PROTEOMICS

Weak affinity chromatography as a new approach for fragment screening in drug discovery

(2011) Minh-Dao Duong-Thi et al.   ANALYTICAL BIOCHEMISTRY

Identification of a Primary Target of Thalidomide Teratogenicity

(2010) T. Ito et al.   SCIENCE

YADA: a tool for taking the most out of high-resolution spectra

(2009) Paulo C. Carvalho et al.   BIOINFORMATICS