排序方式: 共有56条查询结果,搜索用时 187 毫秒
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Ulrik Hillaert Dr. Martijn Verdoes Bogdan I. Florea Dr. Anastasios Saragliadis Kim L. L. Habets Johan Kuiper Dr. Serge Van Calenbergh Prof. Ferry Ossendorp Dr. Gijsbert A. van der Marel Prof. Christoph Driessen Prof. Hermen S. Overkleeft Prof. 《Angewandte Chemie (International ed. in English)》2009,48(14):2442-2442
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Jian-Zhang Li Wei Hu Xi Chen Lei Yang Si-Yang Sun Sheng-Ying Qin 《Journal of Dispersion Science and Technology》2013,34(5):595-603
Schiff base complexes with aza-crown ether pendants have been synthesized and employed as models for hydrolase enzymes by studying the kinetics of their hydrolysis reactions with p-nitrophenyl picolinate (PNPP) in Brij35 surfactant micellar solution. A kinetic model of PNPP cleavage catalyzed by these complexes is proposed. The effects of complex structures and reaction temperature on the rate of catalytic PNPP hydrolysis have also been examined. The rate increases with pH of the buffered Brij35 micellar solution under 25°C; all four complexes exhibited high activity in the catalytic PNPP hydrolysis. The catalytic activity of the phenyl-bridged Schiff base complex is larger than that of ethyl-bridged Schiff base complex for the same substituent and metal. The catalytic activity of manganese(III) complex is superior over cobalt(II) complex in catalyzing hydrolysis of PNPP under the same ligand. The pseudo-first-order rate for PNPP hydrolysis catalyzed by CoL1 containing aza-crown ether is 2.96 × 104 times that of spontaneous hydrolysis of PNPP in Brij35 surfactant micellar solution at pH = 7.60, [S] = 2.0 × 10?4 mol dm?3. 相似文献
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Bogna Rudolf Michèle Salmain Janusz Zakrzewski 《Journal of organometallic chemistry》2009,694(6):908-915
Dialkyl- and diphenyl phosphites react with the (η5-C5H5)M(CO)x(η1-N-maleimidato) (M = Fe, Mo; x = 2 or 3) complexes giving products of the phospha-Michael addition to the η1-N-maleimidato ligand. One of these complexes (M = Fe, x = 2) was characterized by X-ray diffraction. The synthesized metallocarbonyl azaphosphonates and the corresponding iron phosphonic acid act as inhibitors of certain serine hydrolases (AChE and BChE). The kinetic assays were performed and revealed that inhibition mechanism depends strongly on the enzyme and the structure of the inhibitor. 相似文献
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Structural Snapshots for Mechanism‐Based Inactivation of a Glycoside Hydrolase by Cyclopropyl Carbasugars
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Christopher Adamson Robert J. Pengelly Saeideh Shamsi Kazem Abadi Dr. Saswati Chakladar Jason Draper Prof. Robert Britton Dr. Tracey M. Gloster Prof. Andrew J. Bennet 《Angewandte Chemie (International ed. in English)》2016,55(48):14978-14982
Glycoside hydrolases (GHs) have attracted considerable attention as targets for therapeutic agents, and thus mechanism‐based inhibitors are of great interest. We report the first structural analysis of a carbocyclic mechanism‐based GH inactivator, the results of which show that the two Michaelis complexes are in 2H3 conformations. We also report the synthesis and reactivity of a fluorinated analogue and the structure of its covalently linked intermediate (flattened 2H3 half‐chair). We conclude that these inactivator reactions mainly involve motion of the pseudo‐anomeric carbon atom, knowledge that should stimulate the design of new transition‐state analogues for use as chemical biology tools. 相似文献
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M. Sc. Marc P. Baggelaar M. Sc. Freek J. Janssen Annelot C. M. van Esbroeck Ing. Hans den Dulk M. Sc. Marco Allarà M. Sc. Sascha Hoogendoorn Dr. Ross McGuire Dr. Bogdan I. Florea Ing. Nico Meeuwenoord Ing. Hans van den Elst Prof. Dr. Gijsbert A. van der Marel Prof. Dr. Jaap Brouwer Prof. Dr. Vincenzo Di Marzo Prof. Dr. Herman S. Overkleeft Dr. Mario van der Stelt 《Angewandte Chemie (International ed. in English)》2013,52(46):12081-12085
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Audrey Hottin Daniel W. Wright Agata Steenackers Prof. Philippe Delannoy Dr. Faustine Dubar Prof. Christophe Biot Prof. Gideon J. Davies Dr. Jean‐Bernard Behr 《Chemistry (Weinheim an der Bergstrasse, Germany)》2013,19(29):9526-9533
Enhanced metabolism of fucose through fucosidase overexpression is a signature of some cancer types, thus suggesting that fucosidase‐targetted ligands could play the role of drug‐delivery vectors. Herein, we describe the synthesis of a new series of pyrrolidine–ferrocene conjugates, consisting of a L ‐fuco‐configured dihydroxypyrrolidine as the fucosidase ligand armed with a cytotoxic ferrocenylamine moeity. Three‐dimensional structures of several of these fucosidase inhibitors reveal transition‐state‐mimicking 3E conformations. Elaboration with the ferrocenyl moiety results in sub‐micromolar inhibitors of both bovine and bacterial fucosidases, with the 3D structure of the latter revealing electron density indicative of highly mobile alkylferrocene compounds. The best compounds show a strong antiproliferative effect, with up to 100 % inhibition of the proliferation of MDA‐MB‐231 cancer cells at 50 μM . 相似文献
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A Convenient Approach to Stereoisomeric Iminocyclitols: Generation of Potent Brain‐Permeable OGA Inhibitors
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Milan Bergeron‐Brlek Dr. Jake Goodwin‐Tindall Nevena Cekic Dr. Christian Roth Dr. Wesley F. Zandberg Dr. Xiaoyang Shan Dr. Vimal Varghese Sherry Chan Prof. Gideon J. Davies Prof. David J. Vocadlo Prof. Robert Britton 《Angewandte Chemie (International ed. in English)》2015,54(51):15429-15433
Pyrrolidine‐based iminocyclitols are a promising class of glycosidase inhibitors. Reported herein is a convenient epimerization strategy that provides direct access to a range of stereoisomeric iminocyclitol inhibitors of O‐GlcNAcase (OGA), the enzyme responsible for catalyzing removal of O‐GlcNAc from nucleocytoplasmic proteins. Structural details regarding the binding of these inhibitors to a bacterial homologue of OGA reveal the basis for potency. These compounds are orally available and permeate into rodent brain to increase O‐GlcNAc, and should prove useful tools for studying the role of OGA in health and disease. 相似文献