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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36条记录   Design of Triazole-Stapled BCL9 alpha-Helical Peptides to Target the beta-Catenin/B-Cell CLL/lymphoma 9 (BCL9) Protein-Protein Interaction [作者：KAWAMOTO STEVEN A; COLESKA ADRIANA; RAN XU; YI HAN; YANG CHAOYIE; WANG SHAOMENG,期刊：Journal of Medicinal Chemistry, 页码：1137-1146 , 文章类型： Article，,卷期：2012年55-3] The interaction between beta-catenin and B-cell CLL/lymphoma 9 (BCL9), critical for the transcriptional activity of beta-catenin, is mediated by a helical segment from BCL9 and a large binding groove in beta-catenin. Des... The Bivalent Ligand Approach Leads to Highly Potent and Selective Acylguanidine-Type Histamine H-2 Receptor Agonists [作者：BIRNKAMMER TOBIAS; SPICKENREITHER ANJA; BRUNSKOLE IRENA; LOPUCH MIROSLAW; KAGERMEIER NICOLE; BERNHARDT GUENTHER; DOVE STEFAN; SEIFERT ROLAND; ELZ SIGURD; BUSCHAUER ARMIN,期刊：Journal of Medicinal Chemistry, 页码：1147-1160 , 文章类型： Article，,卷期：2012年55-3] Bivalent histamine H-2 receptor (H2R) agonists were synthesized by connecting pharmacophoric 3-(2-amino-4-methylthiazol-5-yl)-, 3-(2-aminothiazol-5-yl)-, 3-(imidazol-4-yl)-, or 3-(1,2,4-triazol-5-yl)propylguanidine moiet... Latent Hit Series Hidden in High-Throughput Screening Data [作者：VARIN THIBAULT; DIDIOT MARIECECILE; PARKER CHRISTIAN N; SCHUFFENHAUER ANSGAR,期刊：Journal of Medicinal Chemistry, 页码：1161-1170 , 文章类型： Article，,卷期：2012年55-3] Recently a novel method termed compound set enrichment (CSE) has been described that uses the activity distribution of a structural class of compounds to identify hit series from primary screening data. This report descr... A New Strategy for the Development of Highly Potent and Selective Plasmin Inhibitors [作者：SAUPE SEBASTIAN M; STEINMETZER TORSTEN,期刊：Journal of Medicinal Chemistry, 页码：1171-1180 , 文章类型： Article，,卷期：2012年55-3] A new structure-based strategy for the design of potent and selective plasmin inhibitors was developed. These compounds could be prepared by cyclizations between the P3 and P2 amino acid residues of substrate-analogue in... Structure-Activity Relationship Study of Opiorphin, a Human Dual Ectopeptidase Inhibitor with Antinociceptive Properties [作者：ROSA MONICA; ARSEQUELL GEMMA; ROUGEOT CATHERINE; CALLE LUIS P; MARCELO FILIPA; PINTO MARTA; CENTENO NURIA B; JIMENEZBARBERO JESUS; VALENCIA GREGORIO,期刊：Journal of Medicinal Chemistry, 页码：1181-1188 , 文章类型： Article，,卷期：2012年55-3] Toward developing new potential analgesics, this first structure activity relationship study of opiorphin (H-Gln-Arg-Phe-Ser-Arg-OH), a human peptide inhibiting enkephalin degradation, was performed. A systematic Ala sca... Synthesis and Structure-Activity Relationships of (Aryloxy)quinazoline Ureas as Novel, Potent, and Selective Vascular Endothelial Growth Factor Receptor-2 Inhibitors [作者：GAROFALO ANTONIO; FARCE AMAURY; RAVEZ SEVERINE; LEMOINE AMELIE; SIX PERRINE; CHAVATTE PHILIPPE; GOOSSENS LAURENCE; DEPREUX PATRICK,期刊：Journal of Medicinal Chemistry, 页码：1189-1204 , 文章类型： Article，,卷期：2012年55-3] In our continuing search for medicinal agents to treat proliferative diseases, quinazoline derivatives were synthesized and evaluated pharmacologically as epithelial growth factor receptor and vascular endothelial growth... Ligand-Based Design of a Potent and Selective Inhibitor of Cytochrome P450 2C19 [作者：FOTI ROBERT S; ROCK DAN A; HAN XIAOGANG; FLOWERS ROBERT A II; WIENKERS LARRY C; WAHLSTROM JAN L,期刊：Journal of Medicinal Chemistry, 页码：1205-1214 , 文章类型： Article，,卷期：2012年55-3] A series of omeprazole-based analogues was synthesized and assessed for inhibitory activity against CYP2C19. The data was used to build a CYP2C19 inhibition pharmacophore model for the series. The model was employed to d... Directed R-Group Combination Graph: A Methodology To Uncover Structure-Activity Relationship Patterns in a Series of Analogues [作者：WASSERMANN ANNE MAI; BAJORATH JUERGEN,期刊：Journal of Medicinal Chemistry, 页码：1215-1226 , 文章类型： Article，,卷期：2012年55-3] A graphical method is introduced to study details of structure activity relationships (SARs) in analogue series that further extends conventional analysis of analogues using R-group tables or related approaches and that ... 3-Fluoro- and 3,3-Difluoro-3,4-dideoxy-KRN7000 Analogues as New Potent Immunostimulator Agents: Total Synthesis and Biological Evaluation in Human Invariant Natural Killer T Cells and Mice [作者：HUNAULT JULIE; DISWALL METTE; FRISON JEANCEDRIC; BLOT VIRGINIE; ROCHER JEZABEL; MARIONNEAULAMBOT SEVERINE; OULLIER THIBAULD; DOUILLARD JEANYVES; GUILLARME STEPHANE; SALUZZO CHRISTINE; DUJARDIN GILLES; JACQUEMIN DENIS; GRATON JEROME; LE QUESTEL JEANYVES; EVAIN MICHEL; LEBRETON JACQUES; DUBREUIL DIDIER; LE PENDU JACQUES; PIPELIER MURIEL,期刊：Journal of Medicinal Chemistry, 页码：1227-1241 , 文章类型： Article，,卷期：2012年55-3] We propose here the synthesis and biological evaluation of 0 3,4-dideoxy-GalCer derivatives. The absence of the 3- and 4-hydroxyls on the sphingoid base is combined with the introduction of mono or difluoro substituent a... Structure-Activity Relationships of Cyanoquinolines with Corrector-Potentiator Activity in Delta F508 Cystic Fibrosis Transmembrane Conductance Regulator Protein [作者：KNAPP JOHN M; WOOD ALEX B; PUAYWAH PHUAN; LODEWYK MICHAEL W; TANTILLO DEAN J; VERKMAN A S; KURTH MARK J,期刊：Journal of Medicinal Chemistry, 页码：1242-1251 , 文章类型： Article，,卷期：2012年55-3] Cystic fibrosis (CF) is caused by mutations in the cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel. The most common CF-causing mutation, Delta F508-CFTR, produces CFTR loss-of-function by impa... Impact of Lipophilic Efficiency on Compound Quality [作者：TARCSAY AKOS; NYIRI KINGA; KESERU GYORGY M,期刊：Journal of Medicinal Chemistry, 页码：1252-1260 , 文章类型： Article，,卷期：2012年55-3] Lipophilic efficiency indices such as LLE and LELP were suggested to support balanced optimization of potency and ADMET profile. Here we investigated the performance of LLE and LELP on multiple data sets representing dif... Diverse Heterocyclic Scaffolds as Allosteric Inhibitors of AKT [作者：KETTLE JASON G; BROWN SIMON; CRAFTER CLAIRE; DAVIES BARRY R; DUDLEY PHILLIPPA; FAIRLEY GARY; FAULDER PAUL; FILLERY SHAUN; GREENWOOD HANNAH; HAWKINS JANET; JAMES MICHAEL; JOHNSON KEITH; LANE CLARE D; PASS MARTIN; PINK JENNIFER H; PLANT HELEN; COSULICH SABINA C,期刊：Journal of Medicinal Chemistry, 页码：1261-1273 , 文章类型： Article，,卷期：2012年55-3] Wide-ranging exploration of potential replacements for a quinoline-based inhibitor of activation of AKT kinase led to number of alternative, novel scaffolds with potentially improved potency and physicochemical propertie... Drug-to-Genome-to-Drug, Step 2: Reversing Selectivity in a Series of Antiplasmodial Compounds [作者：BEGHYN TERENCE B; CHARTON JULIE; LEROUX FLORENCE; HENNINOT ANTOINE; REBOULE IRENA; COS PAUL; MAES LOUIS; DEPREZ BENOIT,期刊：Journal of Medicinal Chemistry, 页码：1274-1286 , 文章类型： Article，,卷期：2012年55-3] In a recent paper, we have described the discovery of antimalarial compounds derived from tadalafil, using a drug-to-genome-to-drug approach (J. Med. Chem. 2011, 54 (9), pp 3222-3240). We have shown that these derivative... Binding Evaluation of Fragment-Based Scaffolds for Probing Allosteric Enzymes [作者：KRIMM ISABELLE; LANCELIN JEANMARC; PRALY JEANPIERRE,期刊：Journal of Medicinal Chemistry, 页码：1287-1295 , 文章类型： Article，,卷期：2012年55-3] Fragment-based drug discovery has become a powerful method for the generation of drug leads against therapeutic targets. Beyond the identification of novel and effective starting points for drug design, fragments have em... Trivalent Ultrashort Lipopeptides are Potent pH Dependent Antifungal Agents [作者：ARNUSCH CHRISTOPHER J; ALBADA H BAUKE; VAN VAARDEGEM MARTIN; LISKAMP ROB M J; SAHL HANSGEORG; SHADKCHAN YANA; OSHEROV NIR; SHAI YECHIEL,期刊：Journal of Medicinal Chemistry, 页码：1296-1302 , 文章类型： Article，,卷期：2012年55-3] The activity of antimicrobial peptides (AMPs) that contain a large proportion of histidine residues (pK(a) similar to 6) depends on the physiological pH environment. Advantages of these AMPs include high activity in slig... The 1.8 angstrom Crystal Structure of ACTIBIND Suggests a Mode of Action for T2 Ribonucleases As Antitumorigenic Agents [作者：DE LEEUW MARINA; GONZALEZ ANA; LANIR ASSAF; ROIZ LEVAVA; SMIRNOFF PATRICIA; SCHWARTZ BETTY; SHOSEYOV ODED; ALMOG ORNA,期刊：Journal of Medicinal Chemistry, 页码：1013-1020 , 文章类型： Article，,卷期：2012年55-3] ACTIBIND and its human homologue RNASET2 are T2 ribonucleases (RNases). RNases are ubiquitous and efficient enzymes that hydrolyze RNA to 3' mononucleotides and also possess antitumorigenic and antiangiogenic activities....