Structure-based design of aliskiren, a novel orally effective renin inhibitor

Jeanette M. Wood, Jürgen Maibaum, Joseph Rahuel, +19

Biochemical and Biophysical Research Communications

Combinatorial ChemistryPharmaceutical ScienceBiochemistryMedicineRational Drug Design +5

Food intake in free-feeding and energy-deprived lean rats is mediated by the neuropeptide Y5 receptor.

Leoluca Criscione, Pascal Rigollier, Christine Batzl‐Hartmann, +13

Journal of Clinical Investigation

NutritionNew Neuropeptide YFood IntakeSocial SciencesGastrointestinal Peptide Hormone +20

Discovery, Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent, and Selective Covalent Oral Inhibitor of KRASG12C

Andreas Weiss, Edwige Lorthiois, Louise Barys, +36

Cancer Discovery

Structural Modification of the P2‘ Position of 2,7-Dialkyl-Substituted 5( <i>S</i> )-Amino-4( <i>S</i> )-hydroxy-8-phenyl-octanecarboxamides:  The Discovery of Aliskiren, a Potent Nonpeptide Human Renin Inhibitor Active after Once Daily Dosing in Marmosets

Jürgen Maibaum, Stefan Stutz, Richard Göschke, +11

Journal of Medicinal Chemistry

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

Target identification for a Hedgehog pathway inhibitor reveals the receptor GPR39

Frédéric Bassilana, Adam Carlson, Jennifer DaSilva, +26

Nature Chemical Biology

Signal TransductionReceptor Gpr39Signaling PathwayG Protein-coupled ReceptorMedicine +8

Novel 2,7-Dialkyl-Substituted 5(<i>S</i>)-Amino-4(<i>S</i>)-hydroxy-8-phenyl-octanecarboxamide Transition State Peptidomimetics Are Potent and Orally Active Inhibitors of Human Renin

Richard Göschke, Stefan Stutz, Vittorio Rasetti, +13

Journal of Medicinal Chemistry

HypertensionNovel 2,7-Dialkyl-substituted 5PharmacotherapyPharmaceutical ChemistryBlood Pressure +15

Design, synthesis and SAR of a series of 2-substituted 4-amino-quinazoline neuropeptide Y Y5 receptor antagonists

Heinrich Rueeger, Pascal Rigollier, Yasuchika Yamaguchi, +10

Bioorganic & Medicinal Chemistry Letters

Fragment-Based Screening by Biochemical Assays: Systematic Feasibility Studies with Trypsin and MMP12

Andreas Boettcher, Simon Ruedisser, P. Erbel, +6

SLAS DISCOVERY

EngineeringBiological Mass SpectrometryPeptide ScienceBioanalysisAnalytical Chemistry +22

Regioselective cyclopentane ring formation mediated by titanocene chloride

Pascal Rigollier, Jonathan R. Young, Lissa A. Fowley, +1

Journal of the American Chemical Society

HeterocyclicNatural SciencesAltmetric Attention ScoreMolecular BiologyTitanocene Chloridepascal Rigollier +6