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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18条记录   Evolution of a Compact Photoprobe for the Dopamine Transporter Based on (+/-)-threo-Methylphenidate [作者：LAPINSKY DAVID J; YARRAYARAPU NAGESWARI; NOLAN TAMMY L; SURRATT CHRISTOPHER K; LEVER JOHN R; TOMLINSON MICHAEL; VAUGHAN ROXANNE A; DEUTSCH HOWARD M,期刊：ACS Medicinal Chemistry Letters, 页码：378-382 , 文章类型： Article，,卷期：2012年3-5] The development of photoaffinity ligands for determining covalent points of attachment to the dopamine transporter (DAT) has predominantly focused on tropane-based compounds bearing variable-length linkers between the ph... Targeted Kinase Selectivity from Kinase Profiling Data [作者：MILLETTI FRANCESCA; HERMANN JOHANNES C,期刊：ACS Medicinal Chemistry Letters, 页码：383-386 , 文章类型： Article，,卷期：2012年3-5] Kinase selectivity plays a major role in the design strategy of lead series and in the ultimate success of kinase drug discovery programs. Although profiling compounds against a large panel of protein kinases has become ... Fungal bis-Naphthopyrones as Inhibitors of Botulinum Neurotoxin Serotype A [作者：CARDELLINA JOHN H II; ROXASDUNCAN VIRGINIA I; MONTGOMERY VICKI; ECCARD VANESSA; CAMPBELL YVETTE; HU XIN; KHAVRUTSKII ILJA; TAWA GREGORY J; WALLQVIST ANDERS; GLOER JAMES B; PHATAK NISARGA L; HOELLER ULRICH; SOMAN ASHISH G; JOSHI BIREN K; HEIN SARA M; WICKLOW DONALD T; SMITH LEONARD A,期刊：ACS Medicinal Chemistry Letters, 页码：387-391 , 文章类型： Article，,卷期：2012年3-5] An in silico screen of the NIH Molecular Library Small Molecule Repository (MLSMR) of similar to 350000 compounds and confirmatory bioassays led to identification of chaetochromin A (1) as an inhibitor of botulinum neuro... Boron-Based 4-Hydroxytamoxifen Bioisosteres for Treatment of de Novo Tamoxifen Resistant Breast Cancer [作者：JIANG QUAN; ZHONG QIU; ZHANG QIANG; ZHENG SHILONG; WANG GUANGDI,期刊：ACS Medicinal Chemistry Letters, 页码：392-396 , 文章类型： Article，,卷期：2012年3-5] Tamoxifen remains the first line therapy for estrogen receptor positive (ER+) breast cancer. However, polymorphisms of the gene encoding P450 2D6 could result in no protein expression or no CYP2D6 enzymatic activity and ... Design of a Potent CB1 Receptor Antagonist Series: Potential Scaffold for Peripherally-Targeted Agents [作者：DOW ROBERT L; CARPINO PHILIP A; GAUTREAU DENISE; HADCOCK JOHN R; IREDALE PHILIP A; KELLYSULLIVAN DAWN; LIZANO JEFFREY S; OCONNOR REBECCA E; SCHNEIDER STEVEN R; SCOTT DENNIS O; WARD KAREN M,期刊：ACS Medicinal Chemistry Letters, 页码：397-401 , 文章类型： Article，,卷期：2012年3-5] Antagonism of cannabinoid-1 (CB1) receptor signaling has been demonstrated to inhibit feeding behaviors in humans, but CB1-mediated central nervous system (CNS) side effects have halted the marketing and further developm... HIV-1 Integrase Inhibitor-Inspired Antibacterials Targeting Isoprenoid Biosynthesis [作者：ZHANG YONGHUI; LIN FUYANG; LI KAI; ZHU WEI; LIU YILIANG; CAO RANG; PANG RAN; LEE EUNHAE; AXELSON JORDAN; HENSLER MARY; WANG KE; MOLOHON KATIE J; WANG YANG; MITCHELL DOUGLAS A; NIZET VICTOR; ODFIED ERIC,期刊：ACS Medicinal Chemistry Letters, 页码：402-406 , 文章类型： Article，,卷期：2012年3-5] We report the discovery of antibacterial leads, keto- and diketo-acids, targeting two prenyl transferases: undecaprenyl diphosphate synthase (UPPS) and dehydrosqualene synthase (CrtM). The leads were suggested by the obs... Anti-inflammatory Effect of a Cell-Penetrating Peptide Targeting the Nrf2/Keap1 Interaction [作者：STEEL RICHARD; COWAN JONATHAN; PAYERNE ESTELLE; OCONNELL MARIA A; SEARCEY MARK,期刊：ACS Medicinal Chemistry Letters, 页码：407-410 , 文章类型： Article，,卷期：2012年3-5] Nuclear factor (erythroid-derived 2)-like 2 (Nrf2) is increasingly recognized as a central regulator of multiple signaling pathways in inflammation and cancer, and the ability to use chemical biological tools to investig... Intestinally Targeted Diacylglycerol Acyltransferase 1 (DGAT1) Inhibitors Robustly Suppress Postprandial Triglycerides [作者：SERRANOWU MICHAEL H; COPPOLA GARY M; GONG YONGJIN; NEUBERT ALAN D; CHATELAIN RICARDO; CLAIRMONT KEVIN B; COMMERFORD RENEE; COSKER THERESA; DANIELS THOMAS; HOU YING; JAIN MONISH; JUEDES MARLENE; LI LISHA; MULLARKEY TARA; ROCHEFORD ERIK; SUNG MOO JE; TYLER ANDREW; YANG QING; YOON TAEYOUNG; HUBBARD BRIAN K,期刊：ACS Medicinal Chemistry Letters, 页码：411-415 , 文章类型： Article，,卷期：2012年3-5] High DGAT1 expression levels in the small intestine highlight the critical role this enzyme plays in nutrient absorption. Identification of inhibitors which predominantly inhibit DGAT1 in the gut is an attractive drug di... Novel Carboxamide-Based Allosteric MEK Inhibitors: Discovery and Optimization Efforts toward XL518 (GDC-0973) [作者：RICE KENNETH D; AAY NAING; ANAND NEEL K; BLAZEY CHARLES M; BOWLES OWEN J; BUSSENIUS JOERG; COSTANZO SIMONA; CURTIS JEFFRY K; DEFINA STEVEN C; DUBENKO LARISA; ENGST STEFAN; JOSHI ANAGHA A; KENNEDY ABIGAIL R; KIM ANGIE I; KOLTUN ELENA S; LOUGHEED JULIE C; MANALO JEANCLAIRE L; MARTINI JEANFRANCOIS; NUSS JOHN M; PETO CSABA J; TSANG TSZE H; YU PEIWEN; JOHNSTON STUART,期刊：ACS Medicinal Chemistry Letters, 页码：416-421 , 文章类型： Article，,卷期：2012年3-5] The ERK/MAP kinase cascade is a key mechanism subject to dysregulation in cancer and is constitutively activated or highly upregulated in many tumor types. Mutations associated with upstream pathway components RAS and Ra... beta-Lactones Inhibit N-acylethanolamine Acid Amidase by S-Acylation of the Catalytic N-Terminal Cysteine [作者：ARMIROTTI ANDREA; ROMEO ELISA; PONZANO STEFANO; MENGATTO LUISA; DIONISI MAURO; KARACSONYI CLAUDIA; BERTOZZI FABIO; GARAU GIANPIERO; TAROZZO GLAUCO; REGGIANI ANGELO; BANDIERA TIZIANO; TARZIA GIORGIO; MOR MARCO; PIOMELLI DANIELE,期刊：ACS Medicinal Chemistry Letters, 页码：422-426 , 文章类型： Article，,卷期：2012年3-5] The cysteine amidase N-acylethanolamine acid amidase (NAAA) is a member of the N-terminal nucleophile class of enzymes and a potential target for anti-inflammatory drugs. We investigated the mechanism of inhibition of hu... RXR Partial Agonist CBt-PMN Exerts Therapeutic Effects on Type 2 Diabetes without the Side Effects of RXR Full Agonists [作者：KAKUTA HIROKI; YAKUSHIJI NOBUMASA; SHINOZAKI RYOSUKE; OHSAWA FUMINORI; YAMADA SHOYA; OHTA YUI; KAWATA KOHEI; NAKAYAMA MARIKO; HAGAYA MANABU; FUJIWARA CHISA; MAKISHIMA MAKOTO; UNO SHIGEYUKI; TAI AKIHIRO; MAEHARA AMI; NAKAYAMA MASARU; OHASHI TOSHITAKA; YASUI HIROYUKI; YOSHIKAWA YUTAKA,期刊：ACS Medicinal Chemistry Letters, 页码：427-432 , 文章类型： Article，,卷期：2012年3-5] Treating insulin resistance and type 2 diabetes in rodents, currently known retinoid X receptor (RXR) agonists induce significant adverse effects. Here we introduce a novel RXR partial agonist CBt-PMN (11b), which shows ... Measurement of Atropisomer Racemization Kinetics Using Segmented Flow Technology [作者：DAVOREN JENNIFER E; BUNDESMANN MARK W; YAN QI T; COLLANTES ELIZABETH M; MENTE SCOT; NASON DEANE M; GRAY DAVID L,期刊：ACS Medicinal Chemistry Letters, 页码：433-435 , 文章类型： Article，,卷期：2012年3-5] When stable atropisomers are encountered by drug discovery teams, they can have important implications due to potential differences in their biological activity, pharmacokinetics, and toxicity. Knowledge of an atropisome... Inventorship and Ownership Considerations and Pitfalls with Collaborative Research [作者：ARMSTRONG MARY ANNE; MURPHY GERALD M JR,期刊：ACS Medicinal Chemistry Letters, 页码：349-351 , 文章类型： Editorial Material，,卷期：2012年3-5] Collaborations can be very productive and beneficial for research. However, there are a number of considerations and pitfalls with regard to issues of inventorship and ownership that should be considered before entering ... The Rhodadyns, a New Class of Small Molecule Inhibitors of Dynamin GTPase Activity [作者：ROBERTSON MARK J; HADZIC GORDANA; AMBRUS JOSEPH; POME D YURI; HYDE EMILY; WHITING AINSLIE; MARIANA ANNA; VON KEIST LISA; CHAU NGOC; HAUCKE VOLKER; ROBINSON PHILLIP J; MCCLUSKEY ADAM,期刊：ACS Medicinal Chemistry Letters, 页码：352-356 , 文章类型： Article，,卷期：2012年3-5] Six focused rhodanine-based libraries, 60 compounds in total, were synthesized and evaluated as potential dynamin I GTPase inhibitors. Twenty-six were more potent than the lead compound with 13 returning IC50 values <10 ... Small Molecule Suppression of Carbapenem Resistance in NDM-1 Producing Klebsiella pneumoniae [作者：WORTHINGTON ROBERTA J; BUNDERS CYNTHIA A; REED CATHERINE S; MELANDER CHRISTIAN,期刊：ACS Medicinal Chemistry Letters, 页码：357-361 , 文章类型： Article，,卷期：2012年3-5] The already considerable global public health threat of multidrug-resistant Gram-negative bacteria has become even more of a concern following the emergence of New Delhi metallo-beta-lactamase (NDM-1) producing strains o... Water-Soluble Progesterone Analogues Are Effective, Injectable Treatments in Animal Models of Traumatic Brain Injury [作者：GUTHRIE DAVID B; STEIN DONALD G; LIOTTA DENNIS C; LOCKWOOD MARK A; SAYEED IQBAL; ATIF FAHIM; ARRENDALE RICHARD F; REDDY G PRABHAKAR; EVERS TAYLOR J; MARENGO JOSE R; HOWARD RANDY B; CULVER DEBORAH G; NATCHUS MICHAEL G,期刊：ACS Medicinal Chemistry Letters, 页码：362-366 , 文章类型： Article，,卷期：2012年3-5] After more than 30 years of research and 30 failed clinical trials with as many different treatments, progesterone is the first agent to demonstrate robust clinical efficacy as a treatment for traumatic brain injuries. I...