共查询到20条相似文献,搜索用时 15 毫秒
1.
Michael O. Frederick Dr. Sandra De Lamo Marin Dr. Kim D. Janda Prof. Dr. K. C. Nicolaou Prof. Dr. Tobin J. Dickerson Prof. Dr. 《Chembiochem : a European journal of chemical biology》2009,10(10):1625-1629
Azaspiracid antibodies : Immunization of azaspiracid immunoconjugates has elicited monoclonal antibodies with distinct epitopes on the marine toxin; this will open the way toward azaspiracid diagnostics and the detection of contaminated shellfish before they can enter the food supply.
2.
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.
3.
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.
4.
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.
5.
Kanchan Taori Yanxia Liu Dr. Valerie J. Paul Dr. Hendrik Luesch Prof. Dr. 《Chembiochem : a European journal of chemical biology》2009,10(10):1634-1639
Combinatorial biosynthesis meets combinatorial pharmacology, cyanobacterial style : A new antimitotic natural product with features of both dolastatins 10 and 15 was isolated from the same Floridian Symploca sp. sample that produced the histone deacetylase inhibitor largazole. Both agents in combination are more effective in inhibiting cancer cell proliferation than either agent alone.
6.
Wei Huang Stan Groothuys Alonso Heredia Brian H. M. Kuijpers Floris P. J. T. Rutjes Dr. Floris L. van Delft Dr. Lai‐Xi Wang Dr. 《Chembiochem : a European journal of chemical biology》2009,10(7):1234-1242
Long‐lasting sweet proteins : The chemoenzymatic synthesis of a triazole (T)‐linked glycosylated C34 fragment from HIV‐1 gp41 is described. The glycopeptide shows high solubility, excellent fusion inhibition, and as shown in the graph, promising protease resistance.
7.
Gianluca Degliesposti Dr. Vinod Kasam Dr. Ana Da Costa Dr. Hee‐Kyoung Kang Prof. Nahyun Kim Dr. Do‐Won Kim Dr. Vincent Breton Dr. Doman Kim Prof. Giulio Rastelli Prof. 《ChemMedChem》2009,4(7):1164-1173
Novel and potent inhibitors of Plasmodium falciparum plasmepsin II were identified by post‐processing the results of a docking screening with BEAR, a recently reported procedure for the refinement and rescoring of docked ligands in virtual screening. FRET substrate degradation assays performed on the 30 most promising compounds resulted in 26 inhibitors with IC50 values ranging from 4.3 nM to 1.8 μM .
8.
Teresa Sardon Dr. Thomas Cottin Jing Xu Athanassios Giannis Prof. Dr. Isabelle Vernos Prof. Dr. 《Chembiochem : a European journal of chemical biology》2009,10(3):464-478
Stop dividing : In the quest for antitumorigenic compounds, aurora A kinase has recently emerged as a potential drug target. In this paper three novel aurora inhibitors (shown in the illustration) have been tested for their biological activity in cultured cells. One of them (TC‐28) appears to be a promising specific aurora A inhibitor in vivo.
9.
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.
10.
S. Bay Dr. S. Fort Dr. L. Birikaki Dr. C. Ganneau E. Samain Y‐M. Coïc F. Bonhomme E. Dériaud C. Leclerc Prof. Dr. R. Lo‐Man Dr. 《ChemMedChem》2009,4(4):582-587
Human tumor cell‐specific antibodies were induced in mice after immunization with a synthetic glycopeptide, which is based on the GM2 ganglioside carbohydrate moiety produced on a gram scale in bacteria. Such neoglycopeptides represent a promising cancer vaccine strategy for active immunotherapy targeting carbohydrates.
11.
Bridging the gap : The differences between medicinal chemistry at the industrial and academic levels raises the question: Is there a significant gap between the two spheres that requires attention, or should such differences be deemed natural, without the need to close the gap? Herein we provide perspectives on this issue, based in part on opinions expressed at a forum discussion held at ISMC 2008 in Vienna.
12.
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.
13.
Suming Chen Xiaohua Li Dr. Huimin Ma Prof. Dr. 《Chembiochem : a European journal of chemical biology》2009,10(7):1200-1207
Designer label : A newly developed polarity‐sensitive fluorescent probe (DBHA) was combined with a tyrosine‐specific labelling method that uses transition metal catalysis, and was successfully used in local structural analysis of the Tyr108 domain in Cu/Zn superoxide dismutase (SOD; see scheme). The strategy presented here provides a new approach for studying the local polarity and conformation changes of this tyrosine domain in SOD under acid or heat denaturation conditions.
14.
Aiko Umeda Gabrielle Nina Thibodeaux Jie Zhu YungAh Lee Zhiwen Jonathan Zhang Prof. 《Chembiochem : a European journal of chemical biology》2009,10(8):1302-1304
Come together right now with L ‐DOPA : Chemical cross‐linking is widely used to study protein–protein interactions. However, many cross‐linking agents suffer from low reactivity or selectivity. An efficient and selective reaction of site‐specific protein cross‐linking was achieved using genetically incorporated 3,4‐dihydroxy‐L ‐phenylalanine.
15.
Joachim Mittendorf Prof. Dr. Stefan Weigand Dr. Cristina Alonso‐Alija Dr. Erwin Bischoff Dr. Achim Feurer Dr. Michael Gerisch Dr. Armin Kern Dr. Andreas Knorr Dr. Dieter Lang Dr. Klaus Muenter Dr. Martin Radtke Dr. Hartmut Schirok Dr. Karl‐Heinz Schlemmer Dr. Elke Stahl Dr. Alexander Straub Dr. Frank Wunder Dr. Johannes‐Peter Stasch Dr. 《ChemMedChem》2009,4(5):853-865
Direct stimulation of soluble guanylate cyclase (sGC) represents a promising therapeutic strategy for the treatment of a range of diseases, including the severely disabling pulmonary hypertension (PH). Optimization of the unfavorable DMPK profile of previous sGC stimulators provided riociguat, which is currently being investigated in phase III clinical trials for the oral treatment of PH.
16.
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.
17.
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.
18.
Kimberly M. Bonger Dr. Richard J. B. H. N. van den Berg Dr. Annemiek D. Knijnenburg Laura H. Heitman Dr. Chris J. van Koppen Dr. Cornelis M. Timmers Dr. Herman S. Overkleeft Prof. Dr. Gijsbert A. van der Marel Prof. Dr. 《ChemMedChem》2009,4(7):1189-1195
Two series of dimeric ligands for a G‐protein‐coupled receptor were prepared that differ by the interconnecting spacer system. Biological evaluation revealed that both dimeric series exhibit unique biological properties relative to their monomeric counterparts.
19.
Laura E. Pedró Rosa D. Rajasekhar Reddy Dr. Sherry F. Queener Prof. Lawrence W. Miller Prof. 《Chembiochem : a European journal of chemical biology》2009,10(9):1462-1464
Antifolate labels : Molecules that bind specifically and with high affinity to proteins can be developed into powerful tools for chemical biology. The interaction between substituted 5‐benzyl pyrimidines and dihydrofolate reductase can be exploited for chemically labeling fusion proteins in mammalian cells.
20.
Fragment formal concept analysis (FragFCA) for compound classification: Signature fragment combinations for compound classes with closely related biological activity were identified using FragFCA. These combinations are used to accurately classify active test compounds on the basis of fragment mapping. FragFCA can extract class‐specific fragment combinations from compounds active against different target families that have signature character and practical utility in compound classification and database searching.