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

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

Structure-Based Approach for the Discovery of Pyrrolo[3,2-<i>d</i>]pyrimidine-Based EGFR T790M/L858R Mutant Inhibitors

Satoshi Sogabe, Youichi Kawakita, S. Igaki, +7

ACS Medicinal Chemistry Letters

Molecular BiologyEgfr InhibitorsChemical BiologyPharmaceutical ChemistryTumor Biology +17

Studies on Disease-Modifying Antirheumatic Drugs:  Synthesis of Novel Quinoline and Quinazoline Derivatives and Their Anti-inflammatory Effect

Atsuo Baba, Noriaki Kawamura, Haruhiko Makino, +3

Journal of Medicinal Chemistry

Novel QuinolineAa Rat ModelAntiparasitic AgentImmunologyPharmacotherapy +15

Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors

Youichi Kawakita, Masaki Seto, Tomohiro Ohashi, +9

Bioorganic & Medicinal Chemistry

Increased phosphorylation of Akt in triple‐negative breast cancers

Shinobu Umemura, Sei Yoshida, Yoshikazu Ohta, +3

Cancer Science

Analysis of circulating tumor cells derived from advanced gastric cancer

Kosei Toyoshima, Akira Hayashi, Masahide Kashiwagi, +6

International Journal of Cancer

Biological Characterization of TAK-901, an Investigational, Novel, Multitargeted Aurora B Kinase Inhibitor

Pamela Farrell, Lihong Shi, Jennifer Matuszkiewicz, +16

Molecular Cancer Therapeutics

Design and Synthesis of Pyrrolo[3,2-<i>d</i>]pyrimidine Human Epidermal Growth Factor Receptor 2 (HER2)/Epidermal Growth Factor Receptor (EGFR) Dual Inhibitors: Exploration of Novel Back-Pocket Binders

Youichi Kawakita, Hiroshi Banno, Tomohiro Ohashi, +11

Journal of Medicinal Chemistry

Design and synthesis of pyrrolo[3,2-d]pyrimidine HER2/EGFR dual inhibitors: Improvement of the physicochemical and pharmacokinetic profiles for potent in vivo anti-tumor efficacy

Youichi Kawakita, Kazuhiro Miwa, Masaki Seto, +10

Bioorganic & Medicinal Chemistry

Medicinal ChemistryMedicinePharmacokinetic ProfilesVivo Anti-tumor EfficacyPharmacotherapy +7