Structural Analysis of the Mechanism of Inhibition and Allosteric Activation of the Kinase Domain of HER2 Protein

Kathleen Aertgeerts, R.J. Skene, Jason K. Yano, +12

Journal of Biological Chemistry

Crystal StructureMolecular BiologyCancer BiologyTumor BiologyHer2 Protein +20

High-resolution structure of the human GPR40 receptor bound to allosteric agonist TAK-875

Ankita Srivastava, Jason K. Yano, Yoshihiko Hirozane, +9

Nature

Molecular PharmacologyDrug TargetSignal TransductionMolecular PhysiologyG Protein-coupled Receptor +9

Plasminogen activator inhibitor-1 detaches cells from extracellular matrices by inactivating integrins

Ralf‐Peter Czekay, Kathleen Aertgeerts, Scott A. Curriden, +1

The Journal of Cell Biology

Structural and Kinetic Analysis of the Substrate Specificity of Human Fibroblast Activation Protein α

Kathleen Aertgeerts, Irena Levin, Lihong Shi, +9

Journal of Biological Chemistry

Crystal structure of human dipeptidyl peptidase IV in complex with a decapeptide reveals details on substrate specificity and tetrahedral intermediate formation

Kathleen Aertgeerts, Sheng Ye, Mike Tennant, +6

Protein Science

Crystal StructureProtein AssemblyMolecular BiologyChemical BiologyProtein Folding +14

Design and Synthesis of Novel Human Epidermal Growth Factor Receptor 2 (HER2)/Epidermal Growth Factor Receptor (EGFR) Dual Inhibitors Bearing a Pyrrolo[3,2-<i>d</i>]pyrimidine Scaffold

Tomoyasu Ishikawa, Masaki Seto, Hiroshi Banno, +14

Journal of Medicinal Chemistry

Dual Inhibitors BearingMedicinal ChemistryDual InhibitorsMedicineX-ray Cocrystal Structures +10

The Low Density Lipoprotein Receptor-related Protein Is a Motogenic Receptor for Plasminogen Activator Inhibitor-1

Bernard Degryse, Jaap G. Neels, Ralf‐Peter Czekay, +3

Journal of Biological Chemistry

Design and Synthesis of Pyrimidinone and Pyrimidinedione Inhibitors of Dipeptidyl Peptidase IV

Zhiyuan Zhang, Michael B. Wallace, Jun Feng, +12

Journal of Medicinal Chemistry

Pharmaceutical SciencePlasma Dpp-4 ActivityPharmacotherapyPharmaceutical ChemistryPyrimidinedione Inhibitors +14

Discovery of a Selective Kinase Inhibitor (TAK-632) Targeting Pan-RAF Inhibition: Design, Synthesis, and Biological Evaluation of <i>C</i>-7-Substituted 1,3-Benzothiazole Derivatives

Masanori Okaniwa, Masaaki Hirose, Takeo Arita, +14

Journal of Medicinal Chemistry

Pharmacology and Mechanism of Action of Suzetrigine, a Potent and Selective NaV1.8 Pain Signal Inhibitor for the Treatment of Moderate to Severe Pain

Jeremiah D. Osteen, Swapna Immani, Tim L. Tapley, +6

Pain and Therapy