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1.
Antonio Carrieri Prof. Violeta I. Pérez‐Nueno Dr. Alessandra Fano Dr. Carlo Pistone Dr. David W. Ritchie Dr. Jordi Teixidó Prof. 《ChemMedChem》2009,4(7):1153-1163
Molecular requirements and determinants for efficient binding to CCR5 were interpreted by computational techniques based on comparative receptor structure modeling, advanced 3D‐QSAR, docking, and shape‐based virtual screening of commercially available entry blockers. Results of this study may be valuable for predicting new HIV entry‐blocking leads.
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Prodigiosin : Amido‐functionalised prodigiosin‐derived compounds were synthesised via a robust and efficient synthetic route. These compounds were then evaluated against 60 human cell lines consisting of nine diverse tumour cell types and their anticancer activities were assessed.
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Tobias Rosenkranz Alexandros Katranidis Diaa Atta Ingo Gregor Dr. Jörg Enderlein Prof. Mariusz Grzelakowski Dr. Per Rigler Dr. Wolfgang Meier Prof. Jörg Fitter Dr. 《Chembiochem : a European journal of chemical biology》2009,10(4):702-709
Protein unfolding inside immobilized polymerosomes : One of the most interesting properties of polymeric vesicles is their remarkable stability against extreme temperatures and osmotic stress, and their longevity even under harsh environmental conditions. We have demonstrated, in an application on protein folding, that surface‐tethered polymerosomes are suitable for performing time‐resolved single molecule studies with encapsulated proteins, as illustrated here.
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An inference network model for molecular similarity searching: The similarity search problem is modeled using inference or evidential reasoning under uncertainty. The inference network model treats similarity searching as an evidential reasoning process in which multiple sources of evidence about compounds and reference structures are combined to estimate resemblance probabilities.
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Madan Kumar Kharel Dr. Pallab Pahari Dr. Hui Lian Jürgen Rohr Prof. Dr. 《Chembiochem : a European journal of chemical biology》2009,10(8):1305-1308
Last at last : The terminal step of the gilvocarcin V (GV) biosynthetic pathway is an unusual lactone formation. Here we show that the enzyme, GilR, dehydrogenates the hemiacetal moiety of pregilvocarcin V to the lactone found in GV by using covalently bound FAD.
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Jens Ripcke Kim Zarse Michael Ristow Prof. Dr. Marc Birringer Dr. 《Chembiochem : a European journal of chemical biology》2009,10(10):1689-1696
Reversible mitochondrial shuttle : A novel concept in mitochondrial pharmacology allows the transport of bioactive compounds into the mitochondrial compartment and their subsequent release. A lipoic acid derivative containing a cleavable (“reversible”) triphenylphosphonium tag is endogenously cleaved by the mitochondrial aldehyde dehydrogenase (ALDH‐2) after mitochondrial accumulation.
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Monpichar Srisa‐Art Dong‐Ku Kang Dr. Jongin Hong Dr. Hyun Park Robin J. Leatherbarrow Prof. Joshua B. Edel Dr. Soo‐Ik Chang Prof. Andrew J. deMello Prof. 《Chembiochem : a European journal of chemical biology》2009,10(10):1605-1611
Every little drop : The KD values of angiogenin (ANG) interactions as shown by FRET analysis of thousands of pL‐sized droplets agree with data from bulk‐fluorescence polarization measurements. Importantly, the use of fluorophores does not affect the activity of ANG or the binding of anti‐ANG antibodies to ANG. Such an experimental platform could be applied to the high‐throughput analysis of protein–protein interactions.
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Johanna M. Rodriguez Dr. Laura Nevola Nathan T. Ross Dr. Gui‐in Lee Dr. Andrew D. Hamilton Prof. 《Chembiochem : a European journal of chemical biology》2009,10(5):829-833
Turn Bak : We present rationally designed scaffolds that mimic the spatial projection of the i, i+4, i+7, and i+11 residues of an α‐helix. A library of biphenyl derivatives was shown by competition fluorescence polarization and ITC to mimic Bak and disrupt the Bak/Bcl‐xL protein–protein interaction. 15N HSQC experiments confirmed that the surface of Bcl‐xL normally occupied by Bak was the target area of our new synthetic inhibitors.
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Raffaella Caglio Dr. Francesca Valetti Dr. Patrizia Caposio Dr. Giorgio Gribaudo Prof. Dr. Enrica Pessione Prof. Dr. Carlo Giunta Prof. Dr. 《Chembiochem : a European journal of chemical biology》2009,10(6):1015-1024
Choosing chloro : By reshaping the catalytic pocket of a catechol 1,2‐dioxygenase through a structural route alternative to evolution, novel engineered chlorocatechol dioxygenase‐like enzymes were obtained. Variants show an inversion of specificity with a preference for 4‐chlorocatechol and activity on the rarely recognised substrate 4,5‐dichlorocatechol.
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Benoit R. M. Villiers Florian Hollfelder Dr. 《Chembiochem : a European journal of chemical biology》2009,10(4):671-682
The limits and potential of substrate promiscuity of the adenylation domain of tyrocidine synthetase 1 were systematically explored. Substrate acceptance is governed by hydrophobic effects (as shown by the correlation of kcat/KM and side‐chain log P), shape complementarity and steric exclusion. The quantification of these factors provides ground rules for understanding and possibly evolving substrate specificity in this class of enzymes.
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Christian Müller Dr. Maria Antonia Gomez‐Zurita Frau Dr. Dario Ballinari Dr. Sonia Colombo Dr. Alessandro Bitto Dr. Enzo Martegani Prof. Cristina Airoldi Dr. Anske Stephanie van Neuren Dr. Matthias Stein Dr. Jörg Weiser Dr. Carlo Battistini Dr. Francesco Peri Prof. 《ChemMedChem》2009,4(4):524-528
A panel of new potential Ras ligands was generated by decorating a tricyclic levoglucosenone‐derived scaffold with aromatic moieties. Some members of the panel show in vitro inhibitory activity toward the nucleotide exchange process on Ras and are toxic to some human cancer cell lines.
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John Yan Shuchi Gupta Dr. David H. Sherman Prof. Dr. Kevin A. Reynolds Prof. Dr. 《Chembiochem : a European journal of chemical biology》2009,10(9):1537-1543
Working together or apart : Separating multimodular PKS enzymes into their respective monomodules by replacing the natural intraprotein linkers (illustrated in red in the figure) with a matched docking domain pair from a heterologous PKS system, leads to only small losses in overall in vivo polyketide product and increased efficiency at utilizing polyketide pathway intermediates to prime the biosynthetic process.
13.
Guojie Wang Dr. Georgii V. Bobkov Sergey N. Mikhailov Prof. Guy Schepers Arthur Van Aerschot Prof. Jef Rozenski Prof. Mark Van der Auweraer Prof. Piet Herdewijn Prof. Steven De Feyter Prof. 《Chembiochem : a European journal of chemical biology》2009,10(7):1175-1185
Powerful pyrene probes : Two kinds of pyrene‐labeled oligonucleotides (HNA‐ and RNA‐skeleton probes) were explored. The enhanced fluorescence intensity in the monomer region and the disappearance of aggregate/excimer emission in duplexes has been successfully used to detect the hybridization of oligonucleotides.
14.
Margit Winkler Dr. Thomas Moraux Hesham A. Khairy Roderick H. Scott Dr. Alexandra M. Z. Slawin Prof. David O'Hagan Prof. 《Chembiochem : a European journal of chemical biology》2009,10(5):823-828
Spicing it up with fluorine : Enantiomers of α‐fluorinated capsaicin 2 , have been prepared by organocatalytic electrophilic fluorination and have been used as probes for the binding conformation of capsaicin to the TRPV1 pain receptor. No enantiomeric bias is observed, thus suggesting an extended binding conformation along the molecular axis.
15.
Carlo Morasso Dr. Tommaso Bellini Prof. Dr. Daniela Monti Dr. Mattia Bassi Davide Prosperi Dr. Sergio Riva Dr. 《Chembiochem : a European journal of chemical biology》2009,10(4):639-644
Stretch out : An elastic light‐scattering‐based method that makes use of phantom nanoparticles as a substrate organizer (see illustration) allowed the quantitative evaluation of the molecular recognition events between a series of inactivated mutants of phospholipase D and lysophosphatidylcholine. The results highlight the remarkable effects on binding capability caused by single amino acid substitutions.
16.
Leo Leung Dr. Cyrille Tomassi Dr. Katrien Van Beneden Dr. Tine Decruy Matthias Trappeniers Dirk Elewaut Prof. Dr. Yifang Gao Tim Elliott Prof. Aymen Al‐Shamkhani Prof. Christian Ottensmeier Prof. Jörn M. Werner Dr. Anthony Williams Dr. Serge Van Calenbergh Prof. Dr. Bruno Linclau Dr. 《ChemMedChem》2009,4(3):329-334
The synthesis of 2′,2′‐difluoro KRN7000 is described. In vivo evaluation demonstrates that this fluorinated glycolipid induces CD1d‐dependent TCR activation of NKT cells, with a bias towards Th2 cytokine production.
17.
Stefano Chimichi Prof. Marco Boccalini Dr. Alessia Salvador Dr. Francesco Dall'Acqua Prof. Giuseppe Basso Prof. Giampietro Viola Dr. 《ChemMedChem》2009,4(5):769-779
New geiparvarin derivatives modified at the alkenyloxy bridge, where the 3′‐methyl group was replaced by a hydrogen atom, were synthesized and evaluated against a panel of human tumor cell lines in vitro. Compounds (R)‐ 4 and (R)‐ 5 show greater inhibitory activity toward cell growth than the parent geiparvarin.
18.
Ulrike Holzgrabe Prof. 《ChemMedChem》2009,4(7):1051-1053
The Great White Plague : Mycobacterium tuberculosis, the bacteria causing tuberculosis, is a continuing threat to global health through the emergence of resistant strains and the lack of novel therapeutic agents. Recently reported results on this important work are highlighted.
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Martin Hintersteiner Dr. Thierry Kimmerlin Dr. Geraldine Garavel Dr. Thorsten Schindler Dr. Roman Bauer Dr. Nicole‐Claudia Meisner Dr. Jan‐Marcus Seifert Dr. Volker Uhl Dr. Manfred Auer Prof. Dr. 《Chembiochem : a European journal of chemical biology》2009,10(6):994-998
New and improved : The incorporation of a 6‐chlorotryptophan (6‐Cl‐Trp) into a β‐peptide (M)‐314 helix leads to a high‐affinity hDM2 inhibitor, as demonstrated by fluorescence fluctuation analysis at single molecule resolution. When conjugated to penetratin, the newly derived hDM2 binder specifically inhibits tumour cell growth in vitro.