- Monoacylglycerol lipase regulates 2-arachidonoylglycerol action and arachidonic acid levels
[作者:Nomura, DK; Hudak, CSS; Ward, AM; Burston, JJ; Issa, RS; Fisher, KJ; Abood, ME; Wiley, JL; Lichtman, AH; Casida, JE,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5875-5878 , 文章类型: Article,,卷期:2008年18-22]
- The structure-activity relationships of organophosphorus (OP) and organosulfur compounds were examined in vitro and in vivo as inhibitors of mouse brain monoacylglycerol lipase (MAGL) hydrolysis of 2-arachidonoylglycerol...
- Evaluating the potential of Vacuolar ATPase inhibitors as anticancer agents and multigram synthesis of the potent salicylihalamide analog saliphenylhalamide
[作者:Lebreton, S; Jaunbergs, J; Roth, MG; Ferguson, DA; De Brabander, JK,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5879-5883 , 文章类型: Article,,卷期:2008年18-22]
- The natural product salicylihalamide is a potent inhibitor of the Vacuolar ATPase (V-ATPase), a potential target for antitumor chemotherapy. We generated salicylihalamide- resistant tumor cell lines typified by an overex...
- Discovery of inhibitors of the channel-activating protease prostasin (CAP1/PRSS8) utilizing structure-based design
[作者:Tully, DC; Vidal, A; Chatterjee, AK; Williams, JA; Roberts, MJ; Petrassi, HM; Spraggon, G; Bursulaya, B; Pacoma, R; Shipway, A; Schumacher, AM; Danahay, H; Harris, JL,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5895-5899 , 文章类型: Article,,卷期:2008年18-22]
- Structure-based design was utilized to guide the early stage optimization of a substrate-like inhibitor to afford potent peptidomimetic inhibitors of the channel-activating protease prostasin. The first X-ray crystal str...
- Immucillins in custom catalytic-site cavities
[作者:Murkin, AS; Clinch, K; Mason, JM; Tyler, PC; Schramm, VL,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5900-5903 , 文章类型: Article,,卷期:2008年18-22]
- Neighboring-group participation in the reaction catalyzed by purine nucleoside phosphorylase involves a compression mode between the 5'- and 4'-ribosyl oxygens, facilitated by His257. The His257Gly mutant opens a space i...
- Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase
[作者:Hur, W; Velentza, A; Kim, S; Flatauer, L; Jiang, XN; Valente, D; Mason, DE; Suzuki, M; Larson, B; Zhang, JM; Zagorska, A; DiDonato, M; Nagle, A; Warmuth, M; Balk, SP; Peters, EC; Gray, NS,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5916-5919 , 文章类型: Article,,卷期:2008年18-22]
- Irreversible HER/erbB inhibitors selectively inhibit HER-family kinases by targeting a unique cysteine residue located within the ATP-binding pocket. Sequence alignment reveals that this rare cysteine is also present in ...
- Development of bestatin-based activity-based probes for metallo-aminopeptidases
[作者:Harbut, MB; Velmourougane, G; Reiss, G; Chandramohanadas, R; Greenbaum, DC,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5932-5936 , 文章类型: Article,,卷期:2008年18-22]
- A novel set of activity-based probes (ABPs) for functionally pro. ling metallo-aminopeptidases was synthesized based on the bestatin inhibitor scaffold, the first synthesis of bestatin analogues using solid-phase techniq...
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