Mapping and classifying molecules from a high-throughput structural database
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16-Membered meta,para-cyclophanes mimicking the vancomycin binding pocket (D-O-E ring) are designed and synthesized. The structural features of these biaryl ether contg. macrocycles are: (a) the deletion of the carboxyl group of vancomycin's central amino ...
Achieving practical biotechnol. processes for the prodn. of fine chems. requires optimization of metabolic fluxes. Attempts to alter the fluxes through a given pathway may be frustrated by compensatory changes in coupled pathways or by unexpected effects s ...
alpha -Isocyano-beta -phenylpropionamide is synthesized from the corresponding amino acid in excellent yield. The unique reactivity of this bifunctional compd. is exploited for the development of novel multicomponent synthesis of 5-aminooxazole, pyrrolo[3, ...
The asym. synthesis of two appropriately functionalized nonproteinogenic amino acids I (Troc = CO2CH2CCl3, TBS = SiMe2CMe3) and II (Boc = Me3CO2C) needed for the total synthesis of vancomycin is described. The assemblage of these amino acids into linear tr ...
The invention relates to human O6-alkylguanine-DNA alkyltransferase (hAGT) mutants showing, when compared to the wild type human AGT, two or more advantageous properties selected from (a) reduced DNA interaction; (b) localization of the expressed protein i ...
(EPFL Ecole Polytechnique Federale de Lausanne, Switz.).2005
This contribution describes the synthesis of polyphenylene dendrimers that are functionalized with up to 16 lysine residues or substituted with short peptide sequences composed of 5 lysine or glutamic acid repeats and a C- or N-terminal cysteine residue. P ...
The puromycin-sensitive aminopeptidase (PSA) is thought to contribute to the degradation of enkephalins. Besides being the most abundant aminopeptidase in the brain, PSA is expressed in other organs as well. From a human fetal brain cDNA library, we have i ...
The invention relates to AGT mutants showing, when compared to the wild type human AGT, two or more advantageous properties selected from (a) reduced DNA interaction (b) localisation of the expressed protein in eukaryotic cells that is no longer restricted ...
The smaller isoform of the GABA-synthesizing enzyme, glutamic acid decarboxylase 65 (GAD65), is unusually susceptible to becoming a target of autoimmunity affecting its major sites of expression, GABA-ergic neurons and pancreatic β-cells. In contrast, a hi ...
Two representatives of a new type of beta-amino acids, carrying two functionalized side chains, one in the 2- and one in the 3-position, have been prepd. stereoselectively: a beta-Ser deriv. with an addnl. CH2OH group in the 2-position, for beta-peptides w ...