Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer
- Author
- QING DONG1 ; DOUGAN, Douglas R1 ; FENG ZHOU1 ; XIANCHANG GONG1 ; HALKOWYCZ, Petro1 ; BOHAN JIN1 ; KANOUNI, Toufike1 ; O'CONNELL, Shawn M1 ; SCORAH, Nicholas1 ; LIHONG SHI1 ; WALLACE, Michael B1
[1] Takeda San Diego;10410 Science Center Drive, San Diego, CA 92121, United States - Source
Bioorganic & medicinal chemistry letters (Print). 2011, Vol 21, Num 5, pp 1315-1319, 5 p ; ref : 22 ref
- ISSN
- 0960-894X
- Scientific domain
- Biochemistry, molecular biology, biophysics; Pharmacology drugs
- Publisher
- Elsevier, Amsterdam
- Publication country
- Netherlands
- Document type
- Article
- Language
- English
- Author keyword
- Allosteric Kinase MEK Oncology Pyridopyrimidinedione SBDD
- Keyword (fr)
- Animal Anticancéreux Cellule tumorale Complexe enzyme inhibiteur Composé bicyclique Cytotoxicité Côlon Dérivé du benzène Homme Hétérocycle azote In vitro In vivo Inhibiteur enzyme Lactame Lignée cellulaire Modèle moléculaire Modélisation Mélanome malin Pharmacocinétique Relation structure activité Site allostérique Synthèse chimique Sélectivité Transferases Voie orale Inhibiteur MEK1 Lignée A375 Lignée COLO205 Mitogen-activated protein kinase kinase Pyrido[2,3-d]pyrimidine-4,7-dione(3-[2,3-dihydroxypropyl]-6-fluoro-5-[2-fluoro-4-iodoanilino]-8-méthyl) Pyridopyrimidine TAK 733 Enzyme Fluor Composé organique
- Keyword (en)
- Animal Antineoplastic agent Tumor cell Inhibitor enzyme complex Bicyclic compound Cytotoxicity Colon Benzene derivatives Human Nitrogen heterocycle In vitro In vivo Enzyme inhibitor Lactam Cell line Molecular model Modeling Malignant melanoma Pharmacokinetics Structure activity relation Allosteric site Chemical synthesis Selectivity Transferases Oral administration Enzyme Fluorine Organic compounds
- Keyword (es)
- Animal Anticanceroso Célula tumoral Complejo enzima inhibidor Compuesto bicíclico Citotoxicidad Colón Benceno derivado Hombre Heterociclo nitrógeno In vitro In vivo Inhibidor enzima Lactamo Línea celular Modelo molecular Modelización Melanoma maligno Farmacocinética Relación estructura actividad Sitio alostérico Síntesis química Selectividad Transferases Vía oral Enzima Fluor Compuesto orgánico
- Classification
- Pascal
- 002 Biological and medical sciences / 002B Medical sciences / 002B02 Pharmacology. Drug treatments / 002B02R Antineoplastic agents / 002B02R01 General aspects
- Discipline
- Pharmacological treatments
- Origin
- Inist-CNRS
- Database
- PASCAL
- INIST identifier
- 23919094
Sauf mention contraire ci-dessus, le contenu de cette notice bibliographique peut être utilisé dans le cadre d’une licence CC BY 4.0 Inist-CNRS / Unless otherwise stated above, the content of this bibliographic record may be used under a CC BY 4.0 licence by Inist-CNRS / A menos que se haya señalado antes, el contenido de este registro bibliográfico puede ser utilizado al amparo de una licencia CC BY 4.0 Inist-CNRS
Access to the document
Install on your browser
DOI
10.1016/j.bmcl.2011.01.071 
https://dx.doi.org/10.1016/j.bmcl.2011.01.071
"O:13:\"PanistOpenUrl\":36:{s:10:\"\u0000*\u0000openUrl\";N;s:6:\"\u0000*\u0000idc\";N;s:6:\"\u0000*\u0000fmt\";s:7:\"journal\";s:6:\"\u0000*\u0000doi\";s:26:\"10.1016\/j.bmcl.2011.01.071\";s:6:\"\u0000*\u0000pii\";s:0:\"\";s:7:\"\u0000*\u0000pmid\";s:0:\"\";s:9:\"\u0000*\u0000atitle\";s:102:\"Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer\";s:9:\"\u0000*\u0000jtitle\";s:48:\"Bioorganic & medicinal chemistry letters (Print)\";s:9:\"\u0000*\u0000stitle\";s:32:\"Bioorg. med. chem. lett. (Print)\";s:7:\"\u0000*\u0000date\";s:4:\"2011\";s:9:\"\u0000*\u0000volume\";s:2:\"21\";s:8:\"\u0000*\u0000issue\";s:1:\"5\";s:8:\"\u0000*\u0000spage\";s:4:\"1315\";s:8:\"\u0000*\u0000epage\";s:4:\"1319\";s:8:\"\u0000*\u0000pages\";s:0:\"\";s:7:\"\u0000*\u0000issn\";s:9:\"0960-894X\";s:8:\"\u0000*\u0000eissn\";s:0:\"\";s:9:\"\u0000*\u0000aulast\";s:9:\"QING DONG\";s:10:\"\u0000*\u0000aufirst\";s:0:\"\";s:9:\"\u0000*\u0000auinit\";s:0:\"\";s:10:\"\u0000*\u0000auinitm\";s:0:\"\";s:5:\"\u0000*\u0000au\";a:10:{i:0;s:17:\"DOUGAN, Douglas R\";i:1;s:9:\"FENG ZHOU\";i:2;s:14:\"XIANCHANG GONG\";i:3;s:16:\"HALKOWYCZ, Petro\";i:4;s:9:\"BOHAN JIN\";i:5;s:16:\"KANOUNI, Toufike\";i:6;s:18:\"O'CONNELL, Shawn M\";i:7;s:16:\"SCORAH, Nicholas\";i:8;s:10:\"LIHONG SHI\";i:9;s:18:\"WALLACE, Michael B\";}s:9:\"\u0000*\u0000aucorp\";s:0:\"\";s:7:\"\u0000*\u0000isbn\";s:0:\"\";s:8:\"\u0000*\u0000coden\";s:0:\"\";s:8:\"\u0000*\u0000genre\";s:7:\"article\";s:7:\"\u0000*\u0000part\";s:0:\"\";s:9:\"\u0000*\u0000btitle\";s:0:\"\";s:8:\"\u0000*\u0000title\";s:102:\"Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer\";s:8:\"\u0000*\u0000place\";s:9:\"Amsterdam\";s:6:\"\u0000*\u0000pub\";s:8:\"Elsevier\";s:10:\"\u0000*\u0000edition\";s:0:\"\";s:9:\"\u0000*\u0000tpages\";s:1:\"5\";s:9:\"\u0000*\u0000series\";s:0:\"\";s:8:\"\u0000*\u0000proxy\";s:30:\"http:\/\/proxyout.inist.fr:8080\/\";s:12:\"\u0000*\u0000integrite\";b:1;}"
Panist access
"O:12:\"IstexOpenUrl\":35:{s:10:\"\u0000*\u0000openUrl\";N;s:6:\"\u0000*\u0000fmt\";s:7:\"journal\";s:6:\"\u0000*\u0000doi\";s:26:\"10.1016\/j.bmcl.2011.01.071\";s:6:\"\u0000*\u0000pii\";s:0:\"\";s:7:\"\u0000*\u0000pmid\";s:0:\"\";s:9:\"\u0000*\u0000atitle\";s:102:\"Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer\";s:9:\"\u0000*\u0000jtitle\";s:48:\"Bioorganic & medicinal chemistry letters (Print)\";s:9:\"\u0000*\u0000stitle\";s:32:\"Bioorg. med. chem. lett. (Print)\";s:7:\"\u0000*\u0000date\";s:4:\"2011\";s:9:\"\u0000*\u0000volume\";s:2:\"21\";s:8:\"\u0000*\u0000issue\";s:1:\"5\";s:8:\"\u0000*\u0000spage\";s:4:\"1315\";s:8:\"\u0000*\u0000epage\";s:4:\"1319\";s:8:\"\u0000*\u0000pages\";s:0:\"\";s:7:\"\u0000*\u0000issn\";s:9:\"0960-894X\";s:8:\"\u0000*\u0000eissn\";s:0:\"\";s:9:\"\u0000*\u0000aulast\";s:9:\"QING DONG\";s:10:\"\u0000*\u0000aufirst\";s:0:\"\";s:9:\"\u0000*\u0000auinit\";s:0:\"\";s:10:\"\u0000*\u0000auinitm\";s:0:\"\";s:5:\"\u0000*\u0000au\";a:10:{i:0;s:17:\"DOUGAN, Douglas R\";i:1;s:9:\"FENG ZHOU\";i:2;s:14:\"XIANCHANG GONG\";i:3;s:16:\"HALKOWYCZ, Petro\";i:4;s:9:\"BOHAN JIN\";i:5;s:16:\"KANOUNI, Toufike\";i:6;s:18:\"O'CONNELL, Shawn M\";i:7;s:16:\"SCORAH, Nicholas\";i:8;s:10:\"LIHONG SHI\";i:9;s:18:\"WALLACE, Michael B\";}s:9:\"\u0000*\u0000aucorp\";s:0:\"\";s:7:\"\u0000*\u0000isbn\";s:0:\"\";s:8:\"\u0000*\u0000coden\";s:0:\"\";s:8:\"\u0000*\u0000genre\";s:7:\"article\";s:7:\"\u0000*\u0000part\";s:0:\"\";s:9:\"\u0000*\u0000btitle\";s:0:\"\";s:8:\"\u0000*\u0000title\";s:102:\"Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer\";s:8:\"\u0000*\u0000place\";s:9:\"Amsterdam\";s:6:\"\u0000*\u0000pub\";s:8:\"Elsevier\";s:10:\"\u0000*\u0000edition\";s:0:\"\";s:9:\"\u0000*\u0000tpages\";s:1:\"5\";s:9:\"\u0000*\u0000series\";s:0:\"\";s:8:\"\u0000*\u0000proxy\";s:30:\"http:\/\/proxyout.inist.fr:8080\/\";s:12:\"\u0000*\u0000integrite\";b:1;}"
Istex access
"O:16:\"UnpaywallOpenUrl\":35:{s:8:\"\u0000*\u0000email\";s:27:\"assistance-portail@inist.fr\";s:6:\"\u0000*\u0000fmt\";N;s:6:\"\u0000*\u0000doi\";s:26:\"10.1016\/j.bmcl.2011.01.071\";s:6:\"\u0000*\u0000pii\";N;s:7:\"\u0000*\u0000pmid\";N;s:9:\"\u0000*\u0000atitle\";N;s:9:\"\u0000*\u0000jtitle\";N;s:9:\"\u0000*\u0000stitle\";N;s:7:\"\u0000*\u0000date\";N;s:9:\"\u0000*\u0000volume\";N;s:8:\"\u0000*\u0000issue\";N;s:8:\"\u0000*\u0000spage\";N;s:8:\"\u0000*\u0000epage\";N;s:8:\"\u0000*\u0000pages\";N;s:7:\"\u0000*\u0000issn\";N;s:8:\"\u0000*\u0000eissn\";N;s:9:\"\u0000*\u0000aulast\";N;s:10:\"\u0000*\u0000aufirst\";N;s:9:\"\u0000*\u0000auinit\";N;s:10:\"\u0000*\u0000auinitm\";N;s:5:\"\u0000*\u0000au\";N;s:9:\"\u0000*\u0000aucorp\";N;s:7:\"\u0000*\u0000isbn\";N;s:8:\"\u0000*\u0000coden\";N;s:8:\"\u0000*\u0000genre\";N;s:7:\"\u0000*\u0000part\";N;s:9:\"\u0000*\u0000btitle\";N;s:8:\"\u0000*\u0000title\";N;s:8:\"\u0000*\u0000place\";N;s:6:\"\u0000*\u0000pub\";N;s:10:\"\u0000*\u0000edition\";N;s:9:\"\u0000*\u0000tpages\";N;s:9:\"\u0000*\u0000series\";N;s:8:\"\u0000*\u0000proxy\";s:30:\"http:\/\/proxyout.inist.fr:8080\/\";s:12:\"\u0000*\u0000integrite\";N;}"
Unpaywall access
"O:16:\"EuropePMCOpenUrl\":35:{s:10:\"\u0000*\u0000openUrl\";N;s:6:\"\u0000*\u0000fmt\";s:7:\"journal\";s:6:\"\u0000*\u0000doi\";s:26:\"10.1016\/j.bmcl.2011.01.071\";s:6:\"\u0000*\u0000pii\";s:0:\"\";s:7:\"\u0000*\u0000pmid\";s:0:\"\";s:9:\"\u0000*\u0000atitle\";s:102:\"Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer\";s:9:\"\u0000*\u0000jtitle\";s:48:\"Bioorganic & medicinal chemistry letters (Print)\";s:9:\"\u0000*\u0000stitle\";s:32:\"Bioorg. med. chem. lett. (Print)\";s:7:\"\u0000*\u0000date\";s:4:\"2011\";s:9:\"\u0000*\u0000volume\";s:2:\"21\";s:8:\"\u0000*\u0000issue\";s:1:\"5\";s:8:\"\u0000*\u0000spage\";s:4:\"1315\";s:8:\"\u0000*\u0000epage\";s:4:\"1319\";s:8:\"\u0000*\u0000pages\";s:0:\"\";s:7:\"\u0000*\u0000issn\";s:9:\"0960-894X\";s:8:\"\u0000*\u0000eissn\";s:0:\"\";s:9:\"\u0000*\u0000aulast\";s:9:\"QING DONG\";s:10:\"\u0000*\u0000aufirst\";s:0:\"\";s:9:\"\u0000*\u0000auinit\";s:0:\"\";s:10:\"\u0000*\u0000auinitm\";s:0:\"\";s:5:\"\u0000*\u0000au\";a:10:{i:0;s:17:\"DOUGAN, Douglas R\";i:1;s:9:\"FENG ZHOU\";i:2;s:14:\"XIANCHANG GONG\";i:3;s:16:\"HALKOWYCZ, Petro\";i:4;s:9:\"BOHAN JIN\";i:5;s:16:\"KANOUNI, Toufike\";i:6;s:18:\"O'CONNELL, Shawn M\";i:7;s:16:\"SCORAH, Nicholas\";i:8;s:10:\"LIHONG SHI\";i:9;s:18:\"WALLACE, Michael B\";}s:9:\"\u0000*\u0000aucorp\";s:0:\"\";s:7:\"\u0000*\u0000isbn\";s:0:\"\";s:8:\"\u0000*\u0000coden\";s:0:\"\";s:8:\"\u0000*\u0000genre\";s:7:\"article\";s:7:\"\u0000*\u0000part\";s:0:\"\";s:9:\"\u0000*\u0000btitle\";s:0:\"\";s:8:\"\u0000*\u0000title\";s:102:\"Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer\";s:8:\"\u0000*\u0000place\";s:9:\"Amsterdam\";s:6:\"\u0000*\u0000pub\";s:8:\"Elsevier\";s:10:\"\u0000*\u0000edition\";s:0:\"\";s:9:\"\u0000*\u0000tpages\";s:1:\"5\";s:9:\"\u0000*\u0000series\";s:0:\"\";s:8:\"\u0000*\u0000proxy\";s:30:\"http:\/\/proxyout.inist.fr:8080\/\";s:12:\"\u0000*\u0000integrite\";b:1;}"
Europe PubMed Central access
"O:12:\"ArXivOpenUrl\":35:{s:10:\"\u0000*\u0000openUrl\";N;s:6:\"\u0000*\u0000fmt\";s:7:\"journal\";s:6:\"\u0000*\u0000doi\";s:26:\"10.1016\/j.bmcl.2011.01.071\";s:6:\"\u0000*\u0000pii\";s:0:\"\";s:7:\"\u0000*\u0000pmid\";s:0:\"\";s:9:\"\u0000*\u0000atitle\";s:102:\"Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer\";s:9:\"\u0000*\u0000jtitle\";s:48:\"Bioorganic & medicinal chemistry letters (Print)\";s:9:\"\u0000*\u0000stitle\";s:32:\"Bioorg. med. chem. lett. (Print)\";s:7:\"\u0000*\u0000date\";s:4:\"2011\";s:9:\"\u0000*\u0000volume\";s:2:\"21\";s:8:\"\u0000*\u0000issue\";s:1:\"5\";s:8:\"\u0000*\u0000spage\";s:4:\"1315\";s:8:\"\u0000*\u0000epage\";s:4:\"1319\";s:8:\"\u0000*\u0000pages\";s:0:\"\";s:7:\"\u0000*\u0000issn\";s:9:\"0960-894X\";s:8:\"\u0000*\u0000eissn\";s:0:\"\";s:9:\"\u0000*\u0000aulast\";s:9:\"QING DONG\";s:10:\"\u0000*\u0000aufirst\";s:0:\"\";s:9:\"\u0000*\u0000auinit\";s:0:\"\";s:10:\"\u0000*\u0000auinitm\";s:0:\"\";s:5:\"\u0000*\u0000au\";a:10:{i:0;s:17:\"DOUGAN, Douglas R\";i:1;s:9:\"FENG ZHOU\";i:2;s:14:\"XIANCHANG GONG\";i:3;s:16:\"HALKOWYCZ, Petro\";i:4;s:9:\"BOHAN JIN\";i:5;s:16:\"KANOUNI, Toufike\";i:6;s:18:\"O'CONNELL, Shawn M\";i:7;s:16:\"SCORAH, Nicholas\";i:8;s:10:\"LIHONG SHI\";i:9;s:18:\"WALLACE, Michael B\";}s:9:\"\u0000*\u0000aucorp\";s:0:\"\";s:7:\"\u0000*\u0000isbn\";s:0:\"\";s:8:\"\u0000*\u0000coden\";s:0:\"\";s:8:\"\u0000*\u0000genre\";s:7:\"article\";s:7:\"\u0000*\u0000part\";s:0:\"\";s:9:\"\u0000*\u0000btitle\";s:0:\"\";s:8:\"\u0000*\u0000title\";s:102:\"Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer\";s:8:\"\u0000*\u0000place\";s:9:\"Amsterdam\";s:6:\"\u0000*\u0000pub\";s:8:\"Elsevier\";s:10:\"\u0000*\u0000edition\";s:0:\"\";s:9:\"\u0000*\u0000tpages\";s:1:\"5\";s:9:\"\u0000*\u0000series\";s:0:\"\";s:8:\"\u0000*\u0000proxy\";s:30:\"http:\/\/proxyout.inist.fr:8080\/\";s:12:\"\u0000*\u0000integrite\";b:1;}"
arXiv access
