BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design

William Farnaby, Manfred Koegl, Michael J. Roy, +34

Nature Chemical Biology

Tumor BiologyMedicineNatural SciencesMolecular BiologyCancer Genomics +8

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

Michael J. Roy, Sandra Winkler, Scott J. Hughes, +5

ACS Chemical Biology

A selective and orally bioavailable VHL-recruiting PROTAC achieves SMARCA2 degradation in vivo

Christiane Kofink, Nicole Trainor, Barbara Mair, +27

Nature Communications

Targeting cancer with small-molecule pan-KRAS degraders

Johannes Popow, William Farnaby, Andreas Gollner, +40

Science

Tumor BiologyGenetic Kras AberrationsOncogenic KrasEngineeringOncogenic Agent +13

Soticlestat, a novel cholesterol 24-hydroxylase inhibitor shows a therapeutic potential for neural hyperexcitation in mice

Toshiya Nishi, Shinichi Kondo, Maki Miyamoto, +15

Scientific Reports

Assessing molecular scaffolds for CNS drug discovery

Joan Mayol-Llinàs, Adam Nelson, William Farnaby, +1

Drug Discovery Today

Medicinal ChemistryDrug TargetMedicineMolecular ScaffoldsPharmacology +4

Discovery of Soticlestat, a Potent and Selective Inhibitor for Cholesterol 24-Hydroxylase (CH24H)

Tatsuki Koike, Masato Yoshikawa, Haruhi Kamisaki Ando, +8

Journal of Medicinal Chemistry

Confounding Factors in Targeted Degradation of Short-Lived Proteins

Vesna Vetma, Laura Casares Perez, J. E. Elias, +23

ACS Chemical Biology

Drug TargetNatural Half-lifeProteasomeMolecular BiologyProtein Refolding +15

Design of a Cereblon construct for crystallographic and biophysical studies of protein degraders

Alena Kroupova, Valentina A. Spiteri, Zoe Rutter, +15

Nature Communications

A selective and orally bioavailable VHL-recruiting PROTAC achieves SMARCA2 degradation in vivo

Christiane Kofink, Nicole Trainor, Barbara Mair, +27

Drug TargetingNovel TherapyChromatin RemodelingSmarca2 DependencyMedicine +13