Insights into Interactions of Mycobacteria with the Host Innate Immune System from a Novel Array of Synthetic Mycobacterial Glycans.

An array of homogeneous glycans representing all the major carbohydrate structures present in the cell wall of the human pathogen Mycobacterium tuberculosis and other mycobacteria has been probed with a panel of glycan-binding receptors expressed on cells of the mammalian innate immune system. The results provide an overview of interactions between mycobacterial glycans and receptors that mediate uptake and survival in macrophages, dendritic cells, and sinusoidal endothelial cells. A subset of the wide variety of glycan structures present on mycobacterial surfaces interact with cells of the innate immune system through the receptors tested.

Synthesis and activity of nucleoside-based antiprotozoan compounds.

Parasitic protozoa employ a salvage pathway to synthesize purines and generate essential active nucleotides, whereas mammals are capable of their de novo biosynthesis. This difference provides opportunity for the design of potential new antiprotozoan compounds. A series of 47 adenosine analogues was prepared with modifications at the 2-, 6- and 5'-positions, based on the hypothesis that such compounds would serve as substrates for protozoan nucleoside salvage enzymes, while remaining refractory in mammalian cells.

Novel nucleoside-based antimalarial compounds.

The malaria-causing parasite Plasmodium falciparum employs a salvage pathway for the biosynthesis of nucleotides, in contrast to de novo biosynthesis that is utilized by the human host. A series of twenty-two 2-, 6- and 5'-modified adenosine ribonucleosides was synthesized, with the expectation that these compounds would generate toxic metabolites instead of active nucleotides by the pathogen, while remaining inert in host cells. Bioassays with P.

Oligosaccharides and peptide displayed on an amphiphilic polymer enable solid phase assay of hapten specific antibodies.

Copovidone, a copolymer of vinyl acetate and N-vinyl-2-pyrrolidone, was synthesized via reversible addition-fragmentation chain transfer (RAFT) polymerization, and after deacetylation the polymer was functionalized by introduction of amino, azide, and alkyne pendant groups to allow attachment of glycans and peptide. Candida albicans β-mannan trisaccharides 1 and 2 and M. tuberculosis arabinan hexasaccharide 3 with appropriate tethers were conjugated to the polymers by squarate or click chemistry.

Corannulene and its penta-tert-butyl derivative co-crystallize 1:1 with pristine C60-fullerene.

The first X-ray structural determinations of pristine fullerene C(60), cocrystallized 1:1 with corannulene and with its pentaalkyl-substituted derivative, 1,3,5,7,9-penta-tert-butyl-corannulene, have now been achieved.

Multifunctional multivalency: a focused library of polymeric cholera toxin antagonists.

Structural pre-organization of the multivalent ligands is important for successful interaction with multimeric proteins. Polymer-based heterobifunctional ligands that contain pendant groups prearranged into heterodimers can be used to probe the active site and surrounding area of the receptor. Here we describe the synthesis and activities of a series of galactose conjugates on polyacrylamide and dextran.

Total syntheses of the marine illudalanes alcyopterosin I, L, M, N, and C.

The combination of a modular assembly of enantiopure triynes and a powerful rhodium-catalyzed [2 + 2 + 2] alkyne cyclotrimerization reaction opens new and efficient entries to a set of alcyopterosins, including the first total synthesis of the alcyopterosins L, M, and C.

C3v-symmetrical tribenzotriquinacenes as hosts for C60 and C70 in solution and in the solid state.

Various tribenzotriquinacenes (TBTQs), most of which incorporate six functional groups at the periphery of their C3v-symmetrical, rigid and convex-concave molecular framework, have been studied with respect to their ability to form supramolecular complexes with the C60 and C70 fullerenes, either in the solid state or in solution. The hexabromo derivative Br6-TBTQ was cocrystallized with C60 as [Br6-TBTQ View Article and Find Full Text PDF