- Tuning RNA Interference by Enhancing siRNA/PAZ Recognition
[作者:GAGLIONE MARIA; POTENZA NICOLETTA; DI FABIO GIOVANNI; ROMANUCCI VALERIA; MOSCA NICOLA; RUSSO ANIELLO; NOVELLINO ETTORE; COSCONATI SANDRO; MESSERE ANNA,期刊:ACS Medicinal Chemistry Letters, 页码:75-78 , 文章类型: Article,,卷期:2013年4-1]
- Chemically modified siRNAs were synthesized to enhance the corresponding silencing activities. The introduced modifications endowed siRNAs with high silencing effect, long RNAi persistence, and better serum resistance. T...
- Discovery of a Highly Selective, Brain-Penetrant Aminopyrazole LRRK2 Inhibitor
[作者:CHAN BRYAN K; ESTRADA ANTHONY A; CHEN HUFFEN; ATHERALL JOHN; BAKERGLENN CHARLES; BERESFORD ALAN; BURDICK DANIEL J; CHAMBERS MARK; DOMINGUEZ SARA L; DRUMMOND JASON; GILL ANDREW; KLEINHEINZ TRACY; LE PICHON CLAIRE E; MEDHURST ANDREW D; LIU XINGRONG; MOFFAT JOHN G; NASH KEVIN; SCEARCELEVIE KIMBERLY; SHENG ZEJUAN; SHORE DANIEL G; VAN DE POEL HERVE; ZHANG SHUO; ZHU HAITAO; SWEENEY ZACHARY K,期刊:ACS Medicinal Chemistry Letters, 页码:85-90 , 文章类型: Article,,卷期:2013年4-1]
- The modulation of LRRK2 kinase activity by a selective small molecule inhibitor has been proposed as a potentially viable treatment for Parkinson's disease. By using aminopyrazoles as aniline bioisosteres, we discovered ...
- Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349
[作者:PEI ZHONGHUA; BLACKWOOD ELIZABETH; LIU LICHUAN; MALEK SHIVA; BELVIN MARCIA; KOEHLER MICHAEL F T; ORTWINE DANIEL F; CHEN HUIFEN; COHEN FREDERICK; KENNY JANE R; BERGERON PHILIPPE; LAU KEVIN; LY CUONG; ZHAO XIANRUI; ESTRADA ANTHONY A; TOM TRUONG; EPLER JENNIFER A; NONOMIYA JIM; LAN TRINH; SIDERIS STEVE; LESNICK JOHN; BAO LINDA; VIJAPURKAR ULKA; MUKADAM SOPHIE; TAY SUZANNE; DESHMUKH GAURI; CHEN YUNGHSIANG; DING XIAO; FRIEDMAN LORI S; LYSSIKATOS JOSEPH P,期刊:ACS Medicinal Chemistry Letters, 页码:103-107 , 文章类型: Article,,卷期:2013年4-1]
- Aberrant activation of the PI3K-Akt-mTOR signaling pathway has been observed in human tumors and tumor cell lines, indicating that these protein kinases may be attractive therapeutic targets for treating cancer. Optimiza...
- Discovery of HSD-621 as a Potential Agent for the Treatment of Type 2 Diabetes
[作者:WAN ZHAOKUI; CHENAIL EVA; LI HUANQIU; IPEK MANUS; XIANG JASON; SURI VIPIN; HAHM SEUNG; BARD JOEL; SVENSON KRISTINE; XU XIN; TIAN XIANBIN; WANG MENGMENG; LI XIANGPING; JOHNSON CHRISTIAN E; QADRI ARIFUL; PANZA DARRELL; PERREAULT MYLENE; MANSOUR TAREK S; TOBIN JAMES F; SAIAH EDDINE,期刊:ACS Medicinal Chemistry Letters, 页码:118-123 , 文章类型: Article,,卷期:2013年4-1]
- 11 beta-Hydroxysteroid dehydrogenase type 1 (11 beta-HSD1) catalyzes the conversion of inactive glucocorticoid cortisone to its active form, cortisol. The glucocorticoid receptor (GR) signaling pathway has been linked to...
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