The adipocyte cGMP-inhibited cyclic nucleotide phosphodiesterase (PDE3B) as a target for lipolytic and thermogenic agents for the treatment of obesity

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Abstract
Agents that stimulate breakdown of adipocyte triglyceride to glycerol and free fatty acids (lipolysis) and increase basal metabolic rate (thermogenesis) have potential benefit as therapeutics for obesity. In the adipocyte, cAMP levels regulate both lipolysis and thermogenesis. PDE3B is one of the major cAMP-hydrolysing cyclic nucleotide phosphodiesterases in the adipocyte and PDE3 inhibitors induce lipolysis in vitro and in vivo. PDE3 inhibitors also elevate metabolic rate in human subjects, though the mechanism of this effect has not yet been determined. Hence, PDE3 inhibitors have a combination of metabolic properties that suggests their utility for the treatment of obesity. PDE3 inhibitors may also have effects on glucose homeostasis, and the relevance of this finding to the possible use of PDE3 inhibitors in obese diabetics is discussed.

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