Melanocortin-1 (MC1) receptor is an attractive melanoma-specific target over-expressed on the surface of melanoma cells. Alpha-melanocyte stimulating hormone (alpha-MSH) peptide analogues can specifically bind MC1 receptors with nanomolar binding affinities, making alpha-MSH peptide analogues very promising candidates for developing effective melanoma-specific imaging probes. This review highli...

Postglycosylation acetylation of sialic acid imparts unique roles to sialoglycoconjugates in mammalian immune response making structural and functional understanding of these analogues important. Five partially O-acetylated Neu5Ac analogues have been synthesized. Reaction of per-O-silylated Neu5Ac ester with AcOH and Ac2O in pyridine promotes regioselective silyl ether/acetate exchange in the f...

Four conformationally restricted analogues of pentamidine were prepared. Then, different concentrations (0.039, 0.078, 0.156, 0.312 and 0.625 mg/mL) of each compound and two positive controls (amphotericin B and pentamidine, 0.625 mg/mL), one negative control (culture medium) and one solvent control (DMSO) were prepared and placed in 24-well plates containing 50000 parasite per well. Promastigo...

BACKGROUND Evidence comparing premixed insulin analogues (a mixture of rapid-acting and intermediate-acting insulin analogues) with other antidiabetic agents is urgently required to guide appropriate therapy. PURPOSE To summarize the English-language literature on the effectiveness and safety of premixed insulin analogues compared with other antidiabetic agents in adults with type 2 diabetes....

Ten synthetic dihydropyridine analogues were investigated for their ability to reverse drug resistance in a multidrug-resistant human carcinoma cell line, KB-Cl. Four dihydropyridine analogues completely reversed the resistance, three lowered the resistance, and three had little effect. The radioactive photoactive dihydropyridine calcium channel blocker, [3H]azidopine, photolabels P-glycoprotei...

The polyamines spermidine and spermine and their diamine precursor putrescine are essential for mammalian cell growth and viability, and strategies are sought for reducing polyamine levels in order to inhibit cancer growth. Several structural analogues of the polyamines have been found to decrease natural polyamine levels and inhibit cell growth, probably by stimulating normal feedback mechanis...

It has been previously shown (l-3) that the nicotinamide moiety of diphosphopyridine nucleotide can be replaced by other pyridine bases without the loss of the coenzyme function. The observation that both the 3-acetylpyridine and pyridine-3aldehyde analogues of diphosphopyridine nucleotide function as coensymes with various dehydrogenases (3) indicated that the amide group on DPN was not essent...