The secondary structure of the coiled coil peptides was regulated by altering the azido content at the hydrophobic core. These peptides were further investigated to form higher-order assemblies presumably via azido-mediated interactions.

The strain-promoted "double-click" (SPDC) reaction using Sondheimer diyne, a novel convergent method conjugating three molecules spontaneously, has enabled us to readily modify an azido-biomolecule with a small reporter azido-molecule.

A radiolabeled photoaffinity ligand has been developed for the N-methyl-D-aspartate (NMDA)-preferring excitatory amino acid receptor complex. [3H]3-Azido-(5S, 10R)(+)-5-methyl-10,11-dihydro-5H- dibenzo[a,d]cyclohepten-5,10-imine [3H]3-azido-MK-801 demonstrated nearly identical affinity, density of binding sites, selectivity, pH sensitivity, and pharmacological profile in reversible binding assa...

A series of new fatty acids containing photosensitive groups at different positions on the paraffin chains supported the growth of an auxotroph of E. coli requiring unsaturated fatty acids. The derivatives were 6-, 9-, 11-, and 12-azidostearic acids, 12-azido-oleic acid, 16-azidopalmitelaidic acid, and 12-(4-azido-2-nitrophenoxy)-stearic and -oleic acids. Analyses of the phospholipids from cult...

Various azido-ubiquinone derivatives were synthesized and characterized. 3-Azido-2-methyl-5-methoxy-6-(3,7-dimethyloctyl)-1,4-benzoquinone was found to be suitable for the study of specific interaction between ubiquinone (Q) and protein. It was synthesized with high specific radioactivity and used to identify the Q-binding proteins in purified ubiquinol-cytochrome c reductase. This azido-Q deri...

Endogenous peroxidase activity in rat thyroid follicular cells is demonstrated cytochemically. Following perfusion fixation of the thyroid gland, small blocks of tissue are incubated in a medium containing substrate for peroxidase, before being postfixed in osmium tetroxide, and processed for electron microscopy. Peroxidase activity is found in thyroid follicular cells in the following sites: (...

Unnatural sugar-mediated metabolic labeling of cancer cells, coupled with efficient Click chemistry, has shown great potential for in vivo imaging and cancer targeting. Thus far, chemical labeling of cancer cells has been limited to the small-sized azido groups, with the large-sized and highly hydrophobic dibenzocyclooctyne (DBCO) being correspondingly used as the targeting ligand. However, sur...

Introduction During an evaluation of azido-α-amino acids and their utility in solid-phase peptide chemistry, the octapeptide angiotensin II and a tripeptide thyrotropin-releasing hormone (TRH) analog have been prepared using Meldal’s procedure [1]. A necessary novel step was the reduction of the azido moiety of L-proline, a secondary amine constrained by a ring, to the corresponding free amine ...

Within this work, a modified preparation of diethyl 4-azidobenzylphosphonate (L1) is presented and the family 4- or 4′-azido-substituted aromatic phosphonate esters increased by three new ligand platforms: diisopropyl (L2), ((4′-azido-[1,1′-biphenyl]-4-yl)methyl)phosphonate (L3), 4-azido-2,3,5,6-tetrafluorobenzylphosphonate (L4), which exhibit an anomalous splitting N3 stretching vibrations. Su...

a group of 1,3-biarylhydrazide derivatives possessing a cox-2 azido pharmacophore at the para- position of the c-1 phenyl ring in conjunction with a n-3 phenyl or substituted-phenyl ring (4-f,4-cl,4-ome) were designed and synthesized based on nucleophilic substitution reaction. a molecular modelling study of these compounds showed that the designed molecules were well bound with the active site...