|
| ||
|
|
||
Biological Screening (biological + screening)
Selected AbstractsBiosynthesis and Biological Screening of a Genetically Encoded Library Based on the Cyclotide MCoTI-ICHEMBIOCHEM, Issue 16 2009Jeffrey Austin Cell-ing point: This study shows that MCoTI-cyclotides can provide an ideal scaffold for the biosynthesis of large combinatorial libraries inside living E. coli cells. Coupled to an appropriate in vivo reporter system, this library may rapidly be screened, for example, by fluorescence-activated cell sorting. [source] ChemInform Abstract: Synthesis and Biological Screening of Some Fluorinated Dibenzofuran Containing 3-Chlorochromones and Benzothiazepines.CHEMINFORM, Issue 49 2009Pratibha Randhavane Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] Synthesis and Biological Screening of Bridgehead Nitrogen Heterocycles: Reactions of 4-(N-Pyridylcarboxamido)-5-mercapto-3-substituted-1,2,4-triazoles.CHEMINFORM, Issue 5 2003R. H. Udupi Abstract For Abstract see ChemInform Abstract in Full Text. [source] Synthesis and biological screening of some fluorinated dibenzofuran containing 3-chlorochromones and benzothiazepinesJOURNAL OF HETEROCYCLIC CHEMISTRY, Issue 4 2009Pratibha Randhavane Variously substituted chalcones were synthesized from 4-difluoromethoxy-dibenzofuran-1-carboxaldehyde. These chalcones were converted into corresponding 3-chlorochromones and dihydro-benzothiazepines. Synthesized compounds were tested for their antifungal, antibacterial, antiviral and antioxidant activities. J. Heterocyclic Chem., (2009). [source] Virtual Screening and Biological Characterization of Novel Histone Arginine Methyltransferase PRMT1 InhibitorsCHEMMEDCHEM, Issue 1 2009Ralf Heinke Abstract Lysine and arginine methyltransferases participate in the posttranslational modification of histones and regulate key cellular functions. Protein arginine methyltransferase,1 (PRMT1) has been identified as an essential component of mixed lineage leukemia (MLL) oncogenic complexes, revealing its potential as a novel therapeutic target in human cancer. The first potent arginine methyltransferase inhibitors were recently discovered by random- and target-based screening approaches. Herein we report virtual and biological screening for novel inhibitors of PRMT1. Structure-based virtual screening (VS) of the Chembridge database composed of 328,000 molecules was performed with a combination of ligand- and target-based in,silico approaches. Nine inhibitors were identified from the top-scored docking solutions; these were experimentally tested using human PRMT1 and an antibody-based assay with a time-resolved fluorescence readout. Among several aromatic amines, an aliphatic amine and an amide were also found to be active in the micromolar range. [source] | ||||||||||