-We have described a class of molecules, called tethered oligonucleotide probes (TOPs), that bind RNA on the basis of both sequence and structure. TOPs consist of two short oligonucleotides joined by a tether whose length and composition may be varied using chemical synthesis. In a triplex TOP, one oligonucleotide recognizes a short single-stranded region in a target RNA through the formation o...

ÐConjugates of bisphosphonates (potential bone resorption inhibitors) and prostaglandin E2 (a bone formation enhancer) were prepared and evaluated for their ability to bind to bone and to liberate, enzymatically, free PGE2. The conjugate 3, an amide at C-1 of PGE2 proved to be too stable in vivo while conjugate 6, a thioester, was too labile. Several PGE2, C-15 ester-linked conjugates (18, 23, ...

-A pharmacophore derived from the structure of the dithiolane derivative of haloperidol bound in the active site of the HIV-1 protease (HIV-1 PR) has been used to search a three-dimensional database for new inhibitory frameworks. This search identified an FMOC-protected N-tosyl arginine as a lead candidate. A derivative in which the arginine carboxyl has been converted to an amide has been crys...

Ðb-Carboline-benzoquinolizidine plant alkaloid deoxytubulosine (DTB) was evaluated and assessed for the ®rst time for its biochemical and biological activity employing the biomarker dihydrofolate reductase (DHFR) (5,6,7,8-tetrahydrofolate: NADP oxidoreductase, EC 1.5.1.3) as the probe enzyme, a key target in cancer chemotherapy. DHFR, employed in the present investigations was puri®ed from Lact...

ÐStereochemically constrained amino acid residues that strongly favour speci®c backbone conformations may be used to nucleate and stabilize speci®c secondary structures in designed peptides. An overview of the use of aa-dialkyl amino acids in stabilizing helical structures in synthetic peptides is presented, with an emphasis on work carried out in the authors laboratory. a-Aminoisobutyric acid ...

ÐA number of model compounds resembling the fundamental bonding patterns of residual kraft lignin, including a series of stilbenes, were incubated with laccase from Trametes versicolor in the presence and absence of deligni®cation `mediators' ABTS and HBT. The condensed kraft lignin model compounds seem to undergo initial degradation by laccase mainly via benzylic oxidation, demethylation and h...

ÐSeveral RGD peptidomimetics have been prepared, in a convergent way, from the common ortho-aminotyrosine template (O-substituted with an anchorage-arm or a methyl group, and aN-substituted with a ̄uorine tag for XPS analysis), and various o-aminoacid derivatives. The most ̄exible compounds have shown a biological activity similar to that of the peptide reference (RGDS) in the platelet aggregat...

Purpose. To evaluate the relationship between internal carotid artery (ICA) stenosis and subfoveal choroidal thickness (SFCT) in the elderly population. Methods. A total of 42 eyes of 21 patients with more than 70% ICA stenosis (Group 1) on one side and less than 70% stenosis (Group 2) on the other side were recruited for this study. ICA stenosis was diagnosed using both the B-mode and Doppler ...

Abstract Introduction Sleep deprivation is a common seizure trigger in adults with epilepsy (AWE). Yet, few prospective studies explore the relationship between control and sleep duration. We studied factors associated duration AWE participating prospective, cross sectional study investigating prevalence of disorders. hypothesized frequency would be inversely Methods Participants were quantifia...