共查询到20条相似文献,搜索用时 46 毫秒
1.
Monique van Scherpenzeel Ed E. Moret Dr. Lluis Ballell Dr. Rob M. J. Liskamp Prof. Dr. Ulf J. Nilsson Dr. Hakon Leffler Dr. Roland J. Pieters Dr. 《Chembiochem : a European journal of chemical biology》2009,10(10):1724-1733
Light up galectin: Photoprobes based on thiodigalactoside were prepared for galectin‐3, a lectin linked to cancer. The probes contained either benzophenone or acetophenone moieties as the photolabel for covalent attachment to the protein. One particular probe labeled galectin‐3 selectively, even in the presence of cell lysate.
2.
Isao Miyazaki Hideo Okumura Dr. Siro Simizu Dr. Yoshikazu Takahashi Dr. Naoki Kanoh Dr. Yasuhiko Muraoka Dr. Yoshiaki Nonomura Dr. Hiroyuki Osada Prof. 《Chembiochem : a European journal of chemical biology》2009,10(5):845-852
Natural product libraries for SAR studies : We used a chemical array platform to study the SARs of bleomycin (BLM) derivatives and Shble protein. The on‐chip SARs suggested that several domains are important for recognition of BLMs by Shble protein. In particular, the C‐terminal tail and the propionamide moiety in pyrimidoblamic acid (PBA) were shown to be important for the binding.
3.
Vanessa Ahmed Yong Liu Dr. Scott D. Taylor Prof. 《Chembiochem : a European journal of chemical biology》2009,10(9):1457-1461
Unexpected inhibition : 2‐ and 4‐mono‐ and difluoromethyl estrone sulfate derivatives are suicide inhibitors of steroid sulfatase (STS). Kinetic studies suggest that inhibition by the monofluoro derivatives is a result of a quinone methide intermediate that reacts with active‐site nucleophiles, whereas the main inhibition pathway of the 4‐difluoromethyl derivative is a result of decomposition of the initial quinone methide to an aldehyde that acts as potent, almost irreversible inhibitor.
4.
Andrew C. Mercer Dr. Jordan L. Meier Justin W. Torpey Dr. Michael D. Burkart Prof. 《Chembiochem : a European journal of chemical biology》2009,10(6):1091-1100
Insider information : Selective labeling of endogenous proteins within cells has been an elusive goal. Here carrier protein labeling has been optimized for visualization, isolation, and protein sequencing.
5.
Yuya A. Lin Justin M. Chalker Benjamin G. Davis Prof. 《Chembiochem : a European journal of chemical biology》2009,10(6):959-969
Protein compatible . Olefin metathesis has emerged as a viable strategy for site‐selective protein modification. This minireview traces its development from early peptide models and metathesis in water to its ultimate application to protein substrates. Prospects in chemistry and biology are also discussed.
6.
Xiao‐Qing Feng Yong‐Hong Liang Zhao‐Sen Zeng Fen‐Er Chen Prof. Dr. Jan Balzarini Prof. Dr. Christophe Pannecouque Prof. Dr. Erik De Clercq Prof. Dr. 《ChemMedChem》2009,4(2):219-224
A novel series of diarylpyrimidine analogues (DAPYs) featuring a naphthyl moiety at the C4 position were designed, with all compounds exhibiting strong activity against wild‐type HIV‐1.
7.
Matthew R. Levengood Christopher C. Kerwood Champak Chatterjee Wilfred A. van der Donk Prof. 《Chembiochem : a European journal of chemical biology》2009,10(5):911-919
One enzyme, many substrates . The substrate specificity of a lantibiotic biosynthetic enzyme, lacticin 481 synthetase, was probed by using synthetic prepeptides containing a variety of nonproteinogenic amino acids, including unnatural α‐amino acids, β‐amino acids, D ‐amino acids, and peptoids.
8.
Tiffany S. Han Min‐Min Zhang Prof. Aleksandra Walewska Pawel Gruszczynski Charles R. Robertson Thomas E. Cheatham III Prof. Doju Yoshikami Prof. Baldomero M. Olivera Prof. Grzegorz Bulaj Prof. 《ChemMedChem》2009,4(3):406-414
Transforming the neuroactive toxins of cone snails into small‐size compounds poses a challenge due to the presence of multiple disulfide bridges. Herein we describe our successful efforts in minimizing the size of μ‐conotoxin while retaining its biological activity.
9.
Frank Streckenbach Gopinath Rangam Dr. Heiko M. Möller Prof. Dr. Andreas Marx Prof. Dr. 《Chembiochem : a European journal of chemical biology》2009,10(10):1630-1633
Finding the right fit : Herein, we report on the development of novel steric probes and present initial insights into their interplay with DNA polymerases. Our findings provide experimental evidence for varied enzyme–substrate interactions that might account for the varied selectivity previously observed.
10.
Marc‐André Frese Thomas Dierks Prof. Dr. 《Chembiochem : a European journal of chemical biology》2009,10(3):425-427
Oxidation of a specific cysteine residue to Cα‐formylglycine is a novel post‐translational modification that is directed by a short recognition motif commonly found in pro‐ and eukaryotic sulfatases. As recently shown by C. Bertozzi and co‐workers, this system can be employed in protein engineering to equip proteins with genetically encoded aldehyde tags for site‐specific labeling, conjugation and immobilization.
11.
Lisa Moni Dr. Gwladys Pourceau Jing Zhang Albert Meyer Sébastien Vidal Dr. Eliane Souteyrand Dr. Alessandro Dondoni Prof. Dr. François Morvan Dr. Yann Chevolot Dr. Jean‐Jacques Vasseur Dr. Alberto Marra Prof. Dr. 《Chembiochem : a European journal of chemical biology》2009,10(8):1369-1378
Sugar‐coated chips : Glycoside clusters are valuable tools for carbohydrate–lectin recognition studies. However, the spatial arrangement of the sugar residues is a key issue in the design of high‐affinity glycoclusters. Here the affinities of linear and antenna‐ and calixarene‐based galactoside clusters towards two lectins derived from Pseudomonas aeruginosa and Ricinus communis were compared by means of glycoarrays.
12.
Stefan Schäfer Dr. Laura Saunders Dr. Sonja Schlimme Dr. Vassil Valkov Dr. Julia M. Wagner Felix Kratz Dr. Wolfgang Sippl Prof. Dr. Eric Verdin Prof. Dr. Manfred Jung Prof. Dr. 《ChemMedChem》2009,4(2):283-290
Pyridylalanine inhibitors of histone deacetylase (HDAC) have been synthesized that show selectivity for the isoform HDAC6 over HDAC1 in vitro. This selectivity was also identified in cancer cells by analyzing tubulin versus histone acetylation. The compounds show decreased intrinsic cytotoxicity relative to pan‐HDAC inhibitors, but show antiproliferative synergy with the proteasome inhibitor bortezomib.
13.
Sara Montanaro Dr. Virginie Lhiaubet‐Vallet Dr. M. Consuelo Jiménez Dr. Miguel Blanca Prof. Miguel Angel Miranda Prof. 《ChemMedChem》2009,4(7):1196-1202
A mechanism for triflusal‐induced photoallergy involving complexation of 2‐hydroxy‐4‐trifluoromethylbenzoic acid with site I of human serum albumin and subsequent formation of a covalent adduct by photoreaction between a metabolite and a neighboring lysine residue is proposed. This is supported by the observed photobinding to poly‐L ‐lysine. Thereby, a photoantigen is generated, which is a likely trigger of the immune response.
14.
Feng Liu Annie J. Aubry Ian C. Schoenhofen Dr. Susan M. Logan Dr. Martin E. Tanner Prof. Dr. 《Chembiochem : a European journal of chemical biology》2009,10(8):1317-1320
Catch a tiger by the tail : We have demonstrated that by feeding nonmotile mutant C. jejuni bacteria with a neutral azide‐labelled pseudaminic acid precursor we can restore their ability to generate functional flagella. The presence of azido‐pseudaminic acid on the surface of the flagella provides a bio‐orthogonal chemical handle that can be used to modify the flagellar proteins.
15.
Antoine Drevelle Dr. Agathe Urvoas Dr. Mériam Ben Hamida‐Rebaï Gérard Van Vooren Magali Nicaise Dr. Marie Valerio‐Lepiniec Dr. Michel Desmadril Dr. Charles H. Robert Dr. Philippe Minard Prof. 《Chembiochem : a European journal of chemical biology》2009,10(8):1349-1359
Breaking ties : The antitumour protein, neocarzinostatin (NCS), is one of the few drug‐carrying proteins used in human therapeutics. However, the presence of disulfide bonds limits this protein's potential development for many applications. This study describes a generic directed‐evolution approach starting from NCS‐3.24 (shown in the figure complexed with two testosterone molecules) to engineer stable disulfide‐free NCS variants suitable for a variety of purposes, including intracellular applications.
16.
Francesc Yraola Dr. Antonio Zorzano Prof. Dr. Fernando Albericio Prof. Dr. Miriam Royo Dr. 《ChemMedChem》2009,4(4):495-503
SSAO/VAP‐1 substrates may be valuable for the treatment or prevention of diabetes mellitus, as they show insulin‐mimetic properties. This review highlights the importance of studying the relevant steric and electronic features in the development of new ligands with better SSAO/VAP‐1 recognition, enhanced selectivity over other amine oxidases, and improved metabolic behavior.
17.
Verena Thiel Ramiro Vilchez Dr. Helena Sztajer Dr. Irene Wagner‐Döbler Prof. Dr. Stefan Schulz Prof. Dr. 《Chembiochem : a European journal of chemical biology》2009,10(3):479-485
Sensing the signal : A gas chromatography–mass spectrometry (GC–MS) method for the analysis of the quorum‐sensing autoinducer‐2 is described. It allows, for the first time, the direct analysis and accurate determination of this highly water soluble signaling compound, which exists in complex equilibria. The application on the caries‐causing bacterium Streptococcus mutans is described.
18.
Tsung‐Lin Li Dr. Dieter Spiteller Dr. Jonathan B. Spencer Dr. 《Chembiochem : a European journal of chemical biology》2009,10(5):896-901
By miscounting the number of malonyl‐CoA condensations, the stilbene synthase (STS) from Pinus sylvestris forms the previously unknown pentaketide, 2‐malonylresveratrol, in addition to the expected tetraketide resveratrol (see scheme). This is the first time that such tetra‐ and pentaketide‐CoA derivatives have been observed; this suggests that these products might be free intermediates in the biosynthesis of stilbenes.
19.
Alexander K. Buell Gian Gaetano Tartaglia Dr. Neil R. Birkett Dr. Christopher A. Waudby Michele Vendruscolo Dr. Xavier Salvatella Dr. Mark E. Welland Prof. Christopher M. Dobson Prof. Tuomas P. J. Knowles Dr. 《Chembiochem : a European journal of chemical biology》2009,10(8):1309-1312
Proteins with a high propensity to aggregate can be largely prevented from doing so with surprisingly small changes to their primary structure. By using a combination of rational design and quantitative measurements of aggregation rates, we show that adding a single charge in specific “gatekeeper” regions is sufficient to change the timescale for amyloid fibril growth from minutes to weeks, thereby dramatically reducing the efficiency of this process.
20.
Gunnar T. Dolphin Dr. Olivier Renaudet Dr. Myriam Ouberai Dr. Pascal Dumy Prof. Julian Garcia Prof. Jean‐Louis Reymond Prof. 《Chembiochem : a European journal of chemical biology》2009,10(8):1325-1329
See you later amyloid β : A screen of a small library of oxime oligomers with an HTS fluorescence assay for amyloid fibril inhibition and subsequent investigation by atomic force microscopy revealed two new micromolar inhibitors of amyloid fibril formation. These new inhibitors have IC50 values in the 10 μM range.