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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10条记录   Exploiting Enzyme Plasticity in Virtual Screening: High Efficiency Inhibitors of Glutamate Racemase [作者：WHALEN KATIE L; PANKOW KATHERINE L; BLANKE STEVEN R; SPIES M ASHLEY,期刊：ACS Medicinal Chemistry Letters, 页码：9-13 , 文章类型： Article，,卷期：2010年1-1] Glutamate racemase is an attractive antimicrobial drug target. Virtual screening using a transition-state conformation of the enzyme resulted in the discovery of several mu M competitive inhibitors, dissimilar from curre... Discovery of a Potent and Orally Bioavailable CCR2 and CCR5 Dual Antagonist [作者：PASTERNAK ALEXANDER; GOBLE STEPHEN D; STRUTHERS MARY; VICARIO PASQUALE P; AYALA JULIA M; DI SALVO JERRY; KILBURN RUTH; WISNIEWSKI THOMAS; DEMARTINO JULIE A; MILLS SANDER G; YANG LIHU,期刊：ACS Medicinal Chemistry Letters, 页码：14-18 , 文章类型： Article，,卷期：2010年1-1] This report describes the discovery of a potent, orally bioavailable CC chemokine receptor 2 (CCR2) antagonist which, while optimized for CCR2 potency, also had potent CC chemokine receptor 5 (CCR5) activity Mechanistic Studies of Sansalvamide A-Amide: An Allosteric Modulator of Hsp90 [作者：VASKO ROBERT C; RODRIGUEZ RODRIGO A; CUNNINGHAM CHRISTIAN N; ARDI VERONICA C; AGARD DAVID A; MCALPINE SHELLI R,期刊：ACS Medicinal Chemistry Letters, 页码：4-8 , 文章类型： Article，,卷期：2010年1-1] Herein, we show that sansalvarnide A-amide (San A-amide), a structurally unique molecule, influences a subset of cancer-related pathways involving heat shock protein 90 (Hsp90) We show that San A-amide specifically binds... Synthesis and SAR of Benzisothiazole- and Indolizine-beta-D-glucopyranoside Inhibitors of SGLT2 [作者：ZHOU HUIQIANG; DANGER DANA P; DOCK STEVEN T; HAWLEY LORA; ROLLER SHANE G; SMITH CHARI D; HANDLON ANTHONY L,期刊：ACS Medicinal Chemistry Letters, 页码：19-23 , 文章类型： Article，,卷期：2010年1-1] A series of benzisothiazole- and indolizine-beta-D-glucopyranoside inhibitors of human SGLT2 are described. The synthesis of the Clinked heterocyclic glucosides took advantage of a palladium-catalyzed cross-coupling reac... Discovery of MK-3207: A Highly Potent, Orally Bioavailable CGRP Receptor Antagonist [作者：BELL IAN M; GALLICCHIO STEVEN N; WOOD MICHAEL R; QUIGLEY AMY G; STUMP CRAIG A; ZARTMAN C BLAIR; FAY JOHN F; LI CHICHUNG; LYNCH JOSEPH J; MOORE ERIC L; MOSSER SCOTT D; PRUEKSARITANONT THOMAYANT; REGAN CHRISTOPHER P; ROLLER SHANE; SALVATORE CHRISTOPHER A; KANE STEFANIE A; VACCA JOSEPH P; SELNICK HAROLD G,期刊：ACS Medicinal Chemistry Letters, 页码：24-29 , 文章类型： Article，,卷期：2010年1-1] Incorporation of polar functionality Into a series of highly potent calcitonin gene-related peptide (CGRP) receptor antagonists was explored in an effort to improve pharmacokinetics This strategy identified piperazinone ... Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin [作者：KNIGHT STEVEN D; ADAMS NICHOLAS D; BURGESS JOEILE L; CHAUDHARI AMITA M; DARCY MICHAEL G; DONATELLI CARLA A; LUENGO JUAN I; NEWLANDER KEN A; PARRISH CYNTHIA A; RIDGERS LANCE H; SARPONG MARTHA A; SCHMIDT STANLEY J; VAN ALLER GLENN S; CARSON JEFFREY D; DIAMOND MELODY A; ELKINS PATRICIA A; GARDINER CHRISTINE M; GARVER ERIC; GILBERT SETH A; GONTAREK RICHARD R; JACKSON JEFFREY R; KERSHNER KEVIN L; LUO LUSONG; RAHA KAUSHIK; SHERK CHRISTIAN S; SUNG CHIUMEI; SUTTON DAVID; TUMMINO PETER J; WEGRZYN RONALD J; AUGER KURT R; DHANAK DASHYANT,期刊：ACS Medicinal Chemistry Letters, 页码：39-43 , 文章类型： Article，,卷期：2010年1-1] Phosphomositide 3-kinase alpha (PI3K alpha) is a critical regulator of cell growth and transformation, and its signaling pathway is the most commonly mutated pathway in human cancers The mammalian target of rapamycin (mT... Discovery of the First Potent and Selective Inhibitor of Centromere-Associated Protein E: GSK923295 [作者：QIAN XIANGPING; MCDONALD ANDREW; ZHOU HANJIE; ADAMS NICHOLAS D; PARRISH CYNTHIA A; DUFFY KEVIN J; FITCH DUKE M; TEDESCO ROSANNA; ASHCRAFT LUKE W; YAO BING; JIANG HONG; HUANG JENNIFER K; MARIN MELCHOR V; AROYAN CARRIE E; WANG JIANCHAO; AHMED SEYED; BURGESS JOELLE L; CHAUDHARI AMITA M; DONATELLI CARLA A; DARCY MICHAEL G; RIDGERS LANCE H; NEWLANDER KEN A; SCHMIDT STANLEY J; CHAI DEPING; COLON MARIELA; ZIMMERMAN MICHAEL N; LAD LATESH; SAKOWICZ ROMAN; SCHAUER STEPHEN; BELMONT LISA; BALIGA RAMESH; PIERCE DANIEL W; FINER JEFFREY T; WANG ZHENGPING; MORGAN BRADLEY P; MORGANS DAVID J JR; AUGER KURT R; SUNG CHIUMEI; CARSON JEFF D; LUO LUSONG; HUGGER ERIN D; COPELAND ROBERT A; SUTTON DAVID; ELLIOTT JOHN D; JACKSON JEFFREY R; WOOD KENNETH W; DHANAK DASHYANT; BERGNES GUSTAVE; KNIGHT STEVEN D,期刊：ACS Medicinal Chemistry Letters, 页码：30-34 , 文章类型： Article，,卷期：2010年1-1] Inhibition of mitotic kinesins represents a novel approach for the discovery of a new generation of anti-mitotic cancer chemotherapeutics We report here the discovery of the first potent and selective inhibitor of centro... Porphyrin - Apidaecin Conjugate as a New Broad Spectrum Antibacterial Agent [作者：DOSSELLI RYAN; GOBBO MARINA; BOLOGNINI ERIKA; CAMPESTRINI SANDRO; REDDI ELENA,期刊：ACS Medicinal Chemistry Letters, 页码：35-38 , 文章类型： Article，,卷期：2010年1-1] The conjugation of the cationic antimicrobial peptide, apidaecin Ib, to the anionic photosensitizer, 5(4'-carboxyphenyl)-10,15,20-triphenylporphyrin (cTPP), afforded a new antibacterial agent effective, under light activ... Fragment Screening by Surface Plasmon Resonance [作者：NAVRATILOVA IVA; HOPKINS ANDREW L,期刊：ACS Medicinal Chemistry Letters, 页码：44-48 , 文章类型： Article，,卷期：2010年1-1] Fragment-based drug discovery is a validated approach for the discovery of drug candidates However, the weak affinity of fragment compounds requires highly sensitive biophysical techniques, such as nuclear magnetic reson... Introductory Editorial for ACS Medicinal Chemistry Letters [作者：LIOTTA DENNIS,期刊：ACS Medicinal Chemistry Letters, 页码：1-1 , 文章类型： Editorial Material，,卷期：2010年1-1]