The new-generation selective ROS1/NTRK inhibitor DS-6051b overcomes crizotinib resistant ROS1-G2032R mutation in preclinical models

Ryohei Katayama, Bo Gong, Noriko Togashi, +21

Nature Communications

U.S. Phase I First-in-human Study of Taletrectinib (DS-6051b/AB-106), a ROS1/TRK Inhibitor, in Patients with Advanced Solid Tumors

Kyriakos P. Papadopoulos, Erkut Borazanci, Alice T. Shaw, +21

Clinical Cancer Research

Identification of the fused bicyclic 4-amino-2-phenylpyrimidine derivatives as novel and potent PDE4 inhibitors

Taiji Goto, Akiko Shiina, Toshiharu Yoshino, +10

Bioorganic & Medicinal Chemistry Letters

Combinatorial ChemistryMedicinal ChemistryBiochemistryMedicineNatural Sciences +8

Natural ligand-nonmimetic inhibitors of the lipid-transfer protein CERT

Naoki Nakao, Masaharu Ueno, Shota Sakai, +7

Communications Chemistry

Identification of the 5,5-dioxo-7,8-dihydro-6H-thiopyrano[3,2-d]pyrimidine derivatives as highly selective PDE4B inhibitors

Taiji Goto, Akiko Shiina, Takeshi Murata, +16

Bioorganic & Medicinal Chemistry Letters

Combinatorial ChemistryBiochemistryMedicineRational Drug DesignPharmacotherapy +4

Novel LCAT (Lecithin:Cholesterol Acyltransferase) Activator DS-8190a Prevents the Progression of Plaque Accumulation in Atherosclerosis Models

Masato Sasaki, Mina Delawary, Hidetaka Sakurai, +11

Arteriosclerosis Thrombosis and Vascular Biology

Small Molecules with Similar Structures Exhibit Agonist, Neutral Antagonist or Inverse Agonist Activity toward Angiotensin II Type 1 Receptor

Shin-ichiro Miura, Yoshihiro Kiya, Hiroyuki Hanzawa, +9

PLoS ONE

Synthesis and biological evaluation of 5-carbamoyl-2-phenylpyrimidine derivatives as novel and potent PDE4 inhibitors

Taiji Goto, Akiko Shiina, Toshiharu Yoshino, +10

Bioorganic & Medicinal Chemistry

Molecular PharmacologyMedicinal ChemistryBiochemistryMedicineNatural Sciences +8

Reassessment of the Unique Mode of Binding between Angiotensin II Type 1 Receptor and Their Blockers

Shin-ichiro Miura, Naoki Nakao, Hiroyuki Hanzawa, +3

PLoS ONE

A covalent fragment-based strategy targeting a novel cysteine to inhibit activity of mutant EGFR kinase

Naoki Kuki, Lee Walmsley, Kazuo Kanai, +19

RSC Medicinal Chemistry