An electrochemically switched smart surface for peptide immobilization and conformation control
We report an electrochemically switched smart surface for controlled peptide immobilization and conformation control. This dynamic surface is based on self-assembled monolayers (SAMs) containing surface-bound trimethoxybenzene moieties, which can undergo
Synthesis of galactoclusters by metal-free thiol "click chemistry" and their binding affinities for pseudomonas aeruginosa lectin leca
Mannose-centered galactoclusters specific for lectin I of Pseudomonas aeruginosa (LecA) were synthesised by a combination of phosphoramidite chemistry and metal-free thiol click chemistry (i.e., thiol addition to acrylamide or nucleophilic displacement of
New chemical tools for investigating human mitotic kinesin Eg5
We have designed and synthesized a series of monastrol derivatives, an allosteric inhibitor of Eg5, a motor protein responsible for the formation and maintenance of the bipolar spindle in mitotic cells. Sterically demanding structural modifications have been introduced on the skeleton of the parent drug either via a multicomponent Biginelli reaction or a stepwise modification of monastrol. The ability of these compounds to inhibit Eg5 activity has been investigated using two in vitro steady-state ATPase assays (basal and microtubule-stimulated) as well as a cell-based assay. One compound in the series appeared more potent than monastrol by a fivefold factor. Three other compounds that were unable to inhibit Eg5 ATPase activity in vitro proved potent Eg5 inhibitors in the cell-based assay. The results obtained led to the identification of structure-activity relationships further used to design an affinity matrix that can be used for fast and efficient purification of Eg5 from crude lysate of eukaryotic cells.
Dynamic synthesis of a macrocycle containing a porphyrin and an electron donor
New macrocycles incorporating a porphyrin and a π electron-rich aromatic were prepared from a dynamic disulfide library. The outcome could be influenced by use of templates. The Royal Society of Chemistry 2005.
Kieran, Amy L.,Pascu, Sofia I.,Jarrosson, Thibaut,Gunter, Maxwell J.,Sanders, Jeremy K. M.
p. 1842 - 1844
(2007/10/03)
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