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1.
Rafael Gozalbes Dr. Frédérique Barbosa Dr. Eric Nicolaï Dr. Dragos Horvath Dr. Nicolas Froloff Dr. 《ChemMedChem》2009,4(2):204-209
A QSAR model for the prediction of CNS activity was developed and validated based on data from an in‐house database of “drug‐like” compounds. The model has demonstrated its applicability for novel chemical structures and its usefulness for the design of CNS‐focused compound libraries.
2.
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.
3.
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.
4.
Enrico Mugnaioli Dr. Filipe Natalio Ute Schloßmacher Xiaohong Wang Prof. Dr. Werner E. G. Müller Prof. Dr. Ute Kolb Dr. 《Chembiochem : a European journal of chemical biology》2009,10(4):683-689
In tandem : High‐resolution TEM shows that during the initial stages of demosponge spicule formation, a primordial crystalline structure is formed within the axial filament. The recently developed electron diffraction tomography technique (ADT) reveals that the nanorods have a layered structure that matches smectitic phyllosilicates. These intracellular nanorods have been considered as precursors of mature spicules.
5.
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.
6.
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.
7.
Chaoxuan Li Dr. Kathryn E. Roege Wendy L. Kelly Prof. 《Chembiochem : a European journal of chemical biology》2009,10(6):1064-1072
More than meets the I : The biosynthetic gene cluster for indanomycin was identified from Streptomyces antibioticus NRRL 8167. The framework of the indanomycins includes a tetrahydropyran and a central indane ring system. The final module of the indanomycin polyketide synthase possesses an unusual terminal module lacking an integrated thioesterase.
8.
Amanda K. Petrus Damian G. Allis Dr. Robert P. Smith Timothy J. Fairchild Prof. Robert P. Doyle Prof. 《ChemMedChem》2009,4(3):297-297
The cover picture shows three views of a vitamin B12–insulin conjugate bound to transcobalamin II, docked in the insulin receptor (IR). This study reveals how the structure of an orally deliverable insulin changes in solution after vitamin B12 conjugation and its effect on IR binding capacity. The results demonstrate that chemical modification of insulin by linking relatively large pendant groups does not interfere with IR recognition. For more details, see the Full Paper by T. J. Fairchild, R. P. Doyle, et al. on p. 421 ff.
9.
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.
10.
Eun‐Ju Lee Eugene W. L. Chan Dr. Muhammad N. Yousaf Prof. 《Chembiochem : a European journal of chemical biology》2009,10(10):1648-1653
Coculture control : We report a combined photochemical and electroactive self‐assembled monolayer (SAM)‐based substrate strategy to generate a coculture platform with spatial and temporal control of cell–cell interactions. These dynamic substrates can present a variety of ligands on the surface for biospecific interactions between the ligands and cell surface receptors. Photopatterning enables the ligands to be immobilized in patterns and even gradients.
11.
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.
12.
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.
13.
Woncheol Kim Dr. Dongho Lee Dr. Seong Su Hong Dr. Zhu Na Jin Chul Shin Su Heun Roh Cheng‐Zhu Wu Oksik Choi Kyeong Lee Dr. Yue‐Mao Shen Dr. Sang‐Gi Paik Dr. Jung Joon Lee Dr. Young‐Soo Hong Dr. 《Chembiochem : a European journal of chemical biology》2009,10(7):1243-1251
Tailor made : We report the rational biosynthesis of C15 hydroxylated non‐quinone geldanamycin analogues by site‐directed mutagenesis of the geldanamycin polyketide synthase (PKS), together with a combination of post‐PKS tailoring genes. Rational biosynthetic engineering allowed the generation of geldanamycin derivatives, such as DHQ3 illustrated in the figure, which had superior pharmacological properties in comparison to the parent compound.
14.
Matthias Hennemann Dr. Arno Friedl Dr. Mario Lobell Dr. Jörg Keldenich Dr. Alexander Hillisch Dr. Timothy Clark Prof. Dr. Andreas H. Göller Dr. 《ChemMedChem》2009,4(4):657-669
CypScore predicts the reactivity of competing positions in the same and different molecules to a variety of cytochrome P450 metabolic reactions on a single reactivity scale.
15.
《International Journal of Applied Ceramic Technology》2016,13(2):i-i
Cover Photograph : Cover photo from the MCARE conference Courtesy of the American Ceramic Society.
16.
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.
17.
Linda Lundström Dr. Bernd Kuhn Dr. Jennifer Beck Edilio Borroni Dr. Joseph G. Wettstein Dr. Thomas J. Woltering Dr. Silvia Gatti Dr. 《ChemMedChem》2009,4(7):1086-1094
Binding of the mGlu2/3 antagonist HYDIA in the closed conformation model of mGlu2 causes repulsive interactions with Y216 in lobe II of the binding pocket, preventing closure of the VFT.
18.
Sharon Anavi‐Goffer Dr. Jan Mulder Dr. 《Chembiochem : a European journal of chemical biology》2009,10(10):1591-1598
The spatiotemporal expression of cannabinoid receptors and endocannabinoid‐metabolising enzymes during brain development guides major developmental processes including neurogenesis, cell differentiation, cell migration, neuronal specification and synaptogenesis.
19.
Mei‐Jung Lai Ching‐Chuan Kuo Dr. Teng‐Kuang Yeh Dr. Hsing‐Pang Hsieh Dr. Li‐Tzong Chen Dr. Wen‐Yu Pan Kuang‐Yang Hsu Dr. Jang‐Yang Chang Dr. Jing‐Ping Liou Dr. 《ChemMedChem》2009,4(4):588-593
Combretastatin A‐4 derivatives : A series of combretastatin A‐4‐derived 1‐benzyl‐4,5,6‐trimethoxyindoles was designed and prepared as a novel class of potent antimitotic agents acting through the colchicine binding site on the microtubule.
20.
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.