- Enzyme redesign guided by cancer-derived IDH1 mutations
[作者：REITMAN ZACHARY J; CHOI BRYAN D; SPASOJEVIC IVAN; BIGNER DARELL D; SAMPSON JOHN H; YAN HAI,期刊：NATURE CHEMICAL BIOLOGY, 页码：887-889 , 文章类型： Article，,卷期：2012年8-11]
- Mutations in an enzyme can result in a neomorphic catalytic activity in cancers. We applied cancer-associated mutations from isocitrate dehydrogenases to homologous residues in the active sites of homoisocitrate dehydrog...
- A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells
[作者：KNUTSON SARAH K; WIGLE TIM J; WARHOLIC NATALIE M; SNEERINGER CHRISTOPHER J; ALLAIN CHRISTINA J; KLAUS CHRISTINE R; SACKS JOELLE D; RAIMONDI ALEJANDRA; MAJER CHRISTINA R; SONG JEFFREY; SCOTT MARGARET PORTER; JIN LEI; SMITH JESSE J; OLHAVA EDWARD J; CHESWORTH RICHARD; MOYER MIKEL P; RICHON VICTORIA M; COPELAND ROBERT A; KEILHACK HEIKE; POLLOCK ROY M; KUNTZ KEVIN W,期刊：NATURE CHEMICAL BIOLOGY, 页码：890-896 , 文章类型： Article，,卷期：2012年8-11]
- EZH2 catalyzes trimethylation of histone H3 lysine 27 (H3K27). Point mutations of EZH2 at Tyr641 and Ala677 occur in subpopulations of non-Hodgkin's lymphoma, where they drive H3K27 hypertrimethylation. Here we report th...
- The orphan nuclear receptor Nur77 regulates LKB1 localization and activates AMPK
[作者：ZHAN YANYAN; CHEN YAN; ZHANG QIAN; ZHUANG JIAJIA; TIAN MIN; CHEN HANGZI; ZHANG LIANRU; ZHANG HONGKUI; HE JIANPING; WANG WEIJIA; WU RONG; WANG YUAN; SHI CHUNFANG; YANG KAI; LI ANZHONG; XIN YONGZHEN; LI TERYTTY YANG; YANG JAMES Y; ZHENG ZHONGHUI; YU CHUNDONG; LIN SHENGCAI; CHANG CHAWNSHANG; HUANG PEIQIANG; LIN TIANWEI; WU QIAO,期刊：NATURE CHEMICAL BIOLOGY, 页码：897-904 , 文章类型： Article，,卷期：2012年8-11]
- Liver kinase B1 (LKB1) has important roles in governing energy homeostasis by regulating the activity of the energy sensor kinase AMP-activated protein kinase (AMPK). The regulation of LKB1 function, however, is still po...
- Systems-pharmacology dissection of a drug synergy in imatinib-resistant CML
[作者：WINTER GEORG E; RIX UWE; CARLSON SCOTT M; GLEIXNER KAROLINE V; GREBIEN FLORIAN; GRIDLING MANUELA; MUELLER ANDRE C; BREITWIESER FLORIAN P; BILBAN MARTIN; COLINGE JACQUES; VALENT PETER; BENNETT KEIRYN L; WHITE FOREST M; SUPERTIFURGA GIULIO,期刊：NATURE CHEMICAL BIOLOGY, 页码：905-912 , 文章类型： Article，,卷期：2012年8-11]
- Occurrence of the BCR-ABL(T315I) gatekeeper mutation is among the most pressing challenges in the therapy of chronic myeloid leukemia (CML). Several BCR-ABL inhibitors have multiple targets and pleiotropic effects that c...
- Discovery of an allosteric mechanism for the regulation of HCV NS3 protein function
[作者：SAALAUBETHELL SUSANNE M; WOODHEAD ANDREW J; CHESSARI GIANNI; CARR MARIA G; COYLE JOSEPH; GRAHAM BRENT; HISCOCK STEVEN D; MURRAY CHRISTOPHER W; PATHURI PUJA; RICH SHARNA J; RICHARDSON CAROLINE J; WILLIAMS PAMELA A; JHOTI HARREN,期刊：NATURE CHEMICAL BIOLOGY, 页码：920-925 , 文章类型： Article，,卷期：2012年8-11]
- Here we report a highly conserved new binding site located at the interface between the protease and helicase domains of the hepatitis C virus (HCV) NS3 protein. Using a chemical lead, identified by fragment screening an...
- A RubisCO-like protein links SAM metabolism with isoprenoid biosynthesis
[作者：ERB TOBIAS J; EVANS BRADLEY S; CHO KYUIL; WARLICK BENJAMIN P; SRIRAM JAYA; WOOD B MCKAY; IMKER HEIDI J; SWEEDLER JONATHAN V; TABITA F ROBERT; GERLT JOHN A,期刊：NATURE CHEMICAL BIOLOGY, 页码：926-932 , 文章类型： Article，,卷期：2012年8-11]
- Functional assignment of uncharacterized proteins is a challenge in the era of large-scale genome sequencing. Here, we combine in extracto NMR, proteomics and transcriptomics with a newly developed (knock-out) metabolomi...
- An enzyme-trap approach allows isolation of intermediates in cobalamin biosynthesis
[作者：DEERY EVELYNE; SCHROEDER SUSANNE; LAWRENCE ANDREW D; TAYLOR SAMANTHA L; SEYEDARABI AREFEH; WATERMAN JITKA; WILSON KEITH S; BROWN DAVID; GEEVES MICHAEL A; HOWARD MARK J; PICKERSGILL RICHARD W; WARREN MARTIN J,期刊：NATURE CHEMICAL BIOLOGY, 页码：933-940 , 文章类型： Article，,卷期：2012年8-11]
- The biosynthesis of many vitamins and coenzymes has often proven difficult to elucidate owing to a combination of low abundance and kinetic lability of the pathway intermediates. Through a serial reconstruction of the co...
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