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文章名     作者     期刊名     摘要     卷     期         如果没有找到您所需要的文献，请点击 ——此处申请     共35条记录   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... Identification of Potent and Selective Diphenylpropanamide ROR gamma Inhibitors [作者：HUH JUN R; ENGLUND ERIKA E; WANG HANG; HUANG RUILI; HUANG PENGXIANG; RASTINEJAD FRAYDOON; INGLESE JAMES; AUSTIN CHRISTOPHER P; JOHNSON RONALD L; HUANG WENWEI; LITTMAN DAN R,期刊：ACS Medicinal Chemistry Letters, 页码：79-84 , 文章类型： Article，,卷期：2013年4-1] Retinoic acid-related orphan receptor ROR gamma t plays a pivotal role in the differentiation of T(H)17 cells. Antagonizing ROR gamma t transcriptional activity is a potential means to treat T(H)17-related autoimmune dis... Modulators of the GPR119 Receptor for the Treatment of Metabolic Syndrome [作者：ROSSE GERARD,期刊：ACS Medicinal Chemistry Letters, 页码：8-9 , 文章类型： Editorial Material，,卷期：2013年4-1] 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 of the Highly Potent PI3K/mTOR Dual Inhibitor PF-04979064 through Structure-Based Drug Design [作者：CHENG HENGMIAO; LI CHUNZE; BAILEY SIMON; BAXI SANGITA M; GOULET LANCE; GUO LISA; HOFFMAN JACQUI; JIANG YING; JOHNSON THEODORE OTTO; JOHNSON TED W; KNIGHTON DANIEL R; LI JOHN; LIU KEVIN K C; LIU ZHENGYU; MARX MATTHEW A; WALLS MARLENA; WELLS PETER A; YIN MINJEAN; ZHU JINJIANG; ZIENTEK MICHAEL,期刊：ACS Medicinal Chemistry Letters, 页码：91-97 , 文章类型： Article，,卷期：2013年4-1] PI3K, AKT, and mTOR are key kinases from PI3K signaling pathway being extensively pursued to treat a variety of cancers in oncology. To search for a structurally differentiated back-up candidate to PF-04691502, which is ... Multivalent Interactions: Synthesis and Evaluation of Melanotropin Multimers-Tools for Melanoma Targeting [作者：BRABEZ NABILA; SAUNDERS KARA; NGUYEN KEVIN L; JAYASUNDERA THANUJA; WEBER CRAIG; LYNCH RONALD M; CHASSAING GERARD; LAVIELLE SOLANGE; HRUBY VICTOR J,期刊：ACS Medicinal Chemistry Letters, 页码：98-102 , 文章类型： Article，,卷期：2013年4-1] To develop agents for early detection and selective treatment of melanomas, high affinity and high specificity molecular tools are required. Enhanced specificity may be obtained by simultaneously binding to multiple cell... Novel Amino-Nicotinamide Derivatives as Modulators of KCNQ2/3 Potassium Channels [作者：ROSSE GERARD,期刊：ACS Medicinal Chemistry Letters, 页码：10-11 , 文章类型： Editorial Material，,卷期：2013年4-1] 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... De Novo Prediction of P-Glycoprotein-Mediated Efflux Liability for Druglike Compounds [作者：GUNAYDIN HAKAN; WEISS MATTHEW M; SUN YAXIONG,期刊：ACS Medicinal Chemistry Letters, 页码：108-112 , 文章类型： Article，,卷期：2013年4-1] P-glycoprotein (Pgp) is capable of recognizing and transporting a wide range of chemically diverse compounds in vivo. Overcoming Pgp-mediated efflux can represent a significant challenge when penetration into the central... Imidazopyridine-Based Fatty Acid Synthase Inhibitors That Show Anti-HCV Activity and in Vivo Target Modulation [作者：OSLOB JOHAN D; JOHNSON RUSSELL J; CAI HAIYING; FENG SHIRLEY Q; HU LILY; KOSAKA YUKO; LAI JULIE; SIVARAJA MOHANRAM; TEP SAMNANG; YANG HANBIAO; ZAHARIA CRISTIANA A; EVANCHIK MARC J; MCDOWELL ROBERT S,期刊：ACS Medicinal Chemistry Letters, 页码：113-117 , 文章类型： Article，,卷期：2013年4-1] Potent imidazopyridine-based inhibitors of fatty acid synthase (FASN) are described. The compounds are shown to have antiviral (HCV replicon) activities that track with their biochemical activities. The most potent analo... 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... Multifunctional Radical Quenchers for the Treatment of Mitochondrial Dysfunction [作者：ROSSE GERARD,期刊：ACS Medicinal Chemistry Letters, 页码：12-13 , 文章类型： Editorial Material，,卷期：2013年4-1] Visible Light Controlled Release of Anticancer Drug through Double Activation of Prodrug [作者：HOSSION ABUGAFAR M L; BIO MOSES; NKEPANG GREGORY; AWUAH SAMUEL G; YOU YOUNGJAE,期刊：ACS Medicinal Chemistry Letters, 页码：124-127 , 文章类型： Article，,卷期：2013年4-1] We designed and synthesized a novel double activatable prodrug system (drug linker deactivated photosensitizer), containing a photocleavable aminoacrylate-linker and a deactivated photosensitizer, to achieve the spatiote... Synthesis and Antiplasmodial and Antimycobacterial Evaluation of New Nitroimidazole and Nitroimidazooxazine Derivatives [作者：TUKULULA MATSHAWANDILE; SHARMA RAJNIKANT; MEURILLON MAIA; MAHAJAN AMAN; NARAN KRUPA; WARNER DIGBY; HUANG JIANXING; MEKONNEN BELEW; CHIBALE KELLY,期刊：ACS Medicinal Chemistry Letters, 页码：128-131 , 文章类型： Article，,卷期：2013年4-1] The synthesis and antiplasmodial and antimycobacterial evaluation of two new series of nitroimidazole and nitroimidazooxazine derivatives is described. The majority of these compounds, especially hybrids 9d, 9f, and 14b,... Biological Evaluation of New Largazole Analogues: Alteration of Macrocyclic Scaffold with Click Chemistry [作者：LI XIANLIN; TU ZHENCHAO; LI HUA; LIU CHUNPING; LI ZHENG; SUN QIAO; YAO YIWU; LIU JINSONG; JIANG SHENG,期刊：ACS Medicinal Chemistry Letters, 页码：132-136 , 文章类型： Article，,卷期：2013年4-1] We report the design, synthesis, and biological evaluation of a new series of largazole analogues in which a 4-methylthiazoline moiety was replaced with a triazole and tetrazole ring, respectively. Compound 7 bearing a t... Solvent Selection for Insoluble Ligands, a Challenge for Biological Assay Development: A TNF-alpha/SPD304 Study [作者：PAPANEOPHYTOU CHRISTOS P; METTOU ANTHI K; RINOTAS VAGELIS; DOUNI ELENI; KONTOPIDIS GEORGE A,期刊：ACS Medicinal Chemistry Letters, 页码：137-141 , 文章类型： Article，,卷期：2013年4-1] Many active compounds may be excluded from biological assays due to their low aqueous solubility. In this study, a simple method for the determination of the solubility of compounds containing aromatic rings is proposed....