Protection by picolinamide, a novel inhibitor of poly (ADP-ribose) synthetase, against both streptozotocin-induced depression of proinsulin synthesis and reduction of NAD content in pancreatic islets☆
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Interaction of nicotinamide and picolinamide with phosphatidylcholine and phosphatidylethanolamine membranes: A combined approach using dipole potential measurements and quantum chemical calculations
2009, Biochimica et Biophysica Acta - BiomembranesCitation Excerpt :Among bioactive species, those containing nitrogen atoms are of particular importance due to its direct function or as constituents of nucleic acids. Picolinamide (2-pyridine-carboxamide; PA) and nicotinamide (3-pyridine-carboxamide; NA) (Fig. 1) are two well known bioactive isomers of pyridine-carboxamide [9,10] which were found to take part in many important biological processes—production of energy, synthesis of fatty acids, cholesterol and steroids, signal transduction and maintenance of the integrity of the genome, inhibition of poly(ADP-ribose) synthetase [10–13]—and possess several therapeutic uses (e.g., in diabetes treatment and prevention, osteoarthritis and granuloma annulare [14–17]). The different relative position of the ring nitrogen atom and carboxamide substituent in NA and PA could be expected to influence the way each molecule binds to the phosphate and carbonyl groups of the membrane phospholipids and, thus, the changes they induce on the membrane surface properties.
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This work has been supported in part by Grants-in-Aid for Cancer Research and for Scientific Research from the Ministry of Education, Science and Culture, Japan.