- Novel Inverse Binding Mode of Indirubin Derivatives Yields Improved Selectivity for DYRK Kinases
[作者：MYRIANTHOPOULOS VASSILIOS; KRITSANIDA MARINA; GABORIAUDKOLAR NICOLAS; MAGIATIS PROKOPIOS; FERANDIN YOAN; DURIEU EMILIE; LOZACH OLIVIER; CAPPEL DANIEL; SOUNDARARAJAN MEERA; FILIPPAKOPOULOS PANAGIS; SHERMAN WOODY; KNAPP STEFAN; MEIJER LAURENT; MIKROS EMMANUEL; SKALTSOUNIS ALEXIOSLEANDROS,期刊：ACS Medicinal Chemistry Letters, 页码：22-26 , 文章类型： Article，,卷期：2013年4-1]
- DYRK kinases are involved in alternative pre-mRNA splicing as well as in neuropathological states such as Alzheimer's disease and Down syndrome. In this study, we present the design, synthesis, and biological evaluation ...
- Structure-Based Design of Irreversible Human KAT II Inhibitors: Discovery of New Potency-Enhancing Interactions
[作者：TUTTLE JAMISON B; ANDERSON MARIE; BECHLE BRUCE M; CAMPBELL BRIAN M; CHANG CHENG; DOUNAY AMY B; EVRARD EDELWEISS; FONSECA KARI R; GAN XINMIN; GHOSH SOMRAJ; HORNER WELDON; JAMES LARRY C; KIM JIYOUNG; MCALLISTER LAURA A; PANDIT JAYVARDHAN; PARIKH VINOD D; RAGO BRIAN J; SALAFIA MICHELLE A; STRICK CHRISTINE A; ZAWADZKE LAURA E; VERHOEST PATRICK R,期刊：ACS Medicinal Chemistry Letters, 页码：37-40 , 文章类型： Article，,卷期：2013年4-1]
- A series of aryl hydroxamates recently have been disclosed as irreversible inhibitors of kynurenine amino transferase II (KAT II), an enzyme that may play a role in schizophrenia and other psychiatric and neurological di...
- Azepines and Piperidines with Dual Norepinephrine Dopamine Uptake Inhibition and Antidepressant Activity
[作者：BROWN DEAN G; BERNSTEIN PETER R; WU YE; URBANEK REBECCA A; BECKER CHRISTOPHER W; THRONER SCOTT R; DEMBOFSKY BRUCE T; STEELMAN GARY B; LAZOR LOIS A; SCOTT CLAY W; WOOD MICHAEL W; WESOLOWSKI STEVEN S; NUGIEL DAVID A; KOCH STEPHANIE; YU JIAN; PIVONKA DONALD E; LI SHUANG; THOMPSON CAROL; ZACCO ANNA; ELMORE CHARLES S; SCHROEDER PATRICIA; LIU JIANWEI; HURLEY CHRISTOPHER A; WARD STUART; HUNT HAZEL J; WILLIAMS KAREN; MCLAUGHLIN JOSEPH; HOESCH VALERIE; SYDSERFF SIMON; MAIER DONNA; AHARONY DAVID,期刊：ACS Medicinal Chemistry Letters, 页码：46-51 , 文章类型： Article，,卷期：2013年4-1]
- Herein, we describe the discovery of inhibitors of norepinephrine (NET) and dopamine (DAT) transporters with reduced activity relative to serotonin transporters (SERT). Two compounds, 8b and 21a, along with nomifensine w...
|