Art

J-GLOBAL ID：201402226932896117   Reference number：14A1334299

Structure-Activity Relationship of 3,5-Diaryl-2-aminopyridine ALK2 Inhibitors Reveals Unaltered Binding Affinity for Fibrodysplasia Ossificans Progressiva Causing Mutants

3,5-ジアリール-2-アミノピリジンALK2阻害剤の構造-活性相関は進行性骨化線維異形成を引き起こす変異に対する変わらない結合親和性を明らかにする

Author (10)： MOHEDAS Agustin H. (Massachusetts Inst. of Technol., Massachusetts, USA) ,  WANG You (Brigham and Women’s Hospital and Harvard Medical School, Massachusetts, USA) ,  SANVITALE Caroline E. (Univ. Oxford, Oxford, GBR) ,  CANNING Peter (Univ. Oxford, Oxford, GBR) ,  CHOI Sungwoon (Brigham and Women’s Hospital and Harvard Medical School, Massachusetts, USA) ,  XING Xuechao (Brigham and Women’s Hospital and Harvard Medical School, Massachusetts, USA) ,  BULLOCK Alex N. (Univ. Oxford, Oxford, GBR) ,  CUNY Gregory D. (Brigham and Women’s Hospital and Harvard Medical School, Massachusetts, USA) ,  CUNY Gregory D. (Univ. Houston, Texas, USA) ,  YU Paul B. (Brigham and Women’s Hospital, Massachusetts, USA)
Material： Journal of Medicinal Chemistry  (J Med Chem)
Volume： 57  Issue： 19  Page： 7900-7915  Publication year： Oct. 09, 2014 
JST Material Number： D0102A  ISSN： 0022-2623  CODEN： JMCMAR  Document type： Article
Article type： 短報  Country of issue： United States (USA)  Language： ENGLISH (EN)

Thesaurus term： *Structure-Activity Relationship ,  *signal transduction receptor ,  connective tissue disease ,  affinity ,  *enzyme inhibitor ,  *chemical compound ,  HepG2 cell ,  cytotoxicity ,  osteogenic factor ,  TGF beta ,  activity (property) ,  chemical synthesis ,  toxicity test ,  heat denaturation ,  *Osteogenesis Imperfecta ,  drug design ,  *ALK2 ,  TGF-beta(1) ,  binding affinity ,  inhibitory activity ,  Signal Transduction ,  50% inhibitory concentration ,  *derivative compounds ,  molecular targeting drug
Semi thesaurus term： cellular signal transduction ,  IC50 ,  *Fibrodysplasia ossificans progressiva ,  Fibrodysplasia ,  *derivative

JST classification (4)： Structure-activity relationship of drugs  (GV01050B) ,  Synthesis of drugs  (GV01030F) ,  Basic research of enzyme preparations and enzyme inhibitor preparations  (GW21010W) ,  Congenital diseases,deformities in general.  (GD03010V)

Substance index (15)： 2-Aminopyridine ,  DMH1 ,  K-02288 ,  LDN-193189 ,  LDN-212838 ,  LDN-212854 ,  LDN-214117 ,  Imatinib ,  Crizotinib ,  Sunitinib ,  Sorafenib ,  Dasatinib ,  Dorsomorphin ,  Ruxolitinib ,  Vemurafenib

Terms in the title (8)： 2-アミノピリジン ,  ALK2 ,  阻害剤 ,  構造-活性相関 ,  骨化 ,  異形成 ,  変異 ,  結合親和性