The <scp>BACE</scp> ‐1 inhibitor <scp>CNP</scp> 520 for prevention trials in Alzheimer's disease

Ulf Neumann, Mike Ufer, Laura H. Jacobson, +29

EMBO Molecular Medicine

A novel BACE inhibitor NB-360 shows a superior pharmacological profile and robust reduction of amyloid-β and neuroinflammation in APP transgenic mice

Ulf Neumann, Heinrich Rueeger, Rainer Machauer, +11

Molecular Neurodegeneration

Discovery of Cyclic Sulfone Hydroxyethylamines as Potent and Selective β-Site APP-Cleaving Enzyme 1 (BACE1) Inhibitors: Structure-Based Design and in Vivo Reduction of Amyloid β-Peptides

Heinrich Rueeger, Rainer Lueoend, Olivier Rogel, +7

Journal of Medicinal Chemistry

Pharmaceutical ScienceCore Scaffold SelectionPeptide ScienceChemical BiologyCyclic Sulfone Hydroxyethylamines +21

JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRAS^G12C for the Treatment of Solid Tumors

Edwige Lorthiois, Marc Gerspacher, Kim S. Beyer, +28

Journal of Medicinal Chemistry

Enantioselective synthesis of (+)-anatoxin-a via enyne metathesis

Jehrod Brenneman, Rainer Machauer, Stephen F. Martin

Tetrahedron

Asymmetric CatalysisEnantioselective SynthesisEnyne MetathesisBiomolecular Engineering

Pharmacological BACE1 and BACE2 inhibition induces hair depigmentation by inhibiting PMEL17 processing in mice

Derya R. Shimshek, Laura H. Jacobson, Carine Kolly, +15

Scientific Reports

Discovery of Novel Dot1L Inhibitors through a Structure-Based Fragmentation Approach

Chao Chen, Hugh Zhu, Frédéric Stauffer, +14

ACS Medicinal Chemistry Letters

Drug TargetMolecular BiologyChemical BiologyPharmaceutical ChemistryRecruit Dot1l +18

Macrocyclic BACE-1 inhibitors acutely reduce Aβ in brain after po application

Andreas Lerchner, Rainer Machauer, Claudia Betschart, +12

Bioorganic & Medicinal Chemistry Letters

Molecular PharmacologyNeurodegenerative DiseasesMolecular NeuroscienceMedicineNeuropharmacology +11

Macrocyclic peptidomimetic β-secretase (BACE-1) inhibitors with activity in vivo

Rainer Machauer, Kurt Laumen, Siem J. Veenstra, +9

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryMedicinePharmacotherapyMacrocyclic Peptidomimetic β-SecretaseDrug Development +3

Discovery of Potent, Selective, and Structurally Novel Dot1L Inhibitors by a Fragment Linking Approach

Henrik Möbitz, Rainer Machauer, Philipp Holzer, +12

ACS Medicinal Chemistry Letters

Drug TargetMolecular BiologyPharmacotherapyChemical BiologyMedicinal Chemistry +15