Pharmacotherapy for the management of obesity

Patel, Dhiren

doi:10.1016/j.metabol.2015.08.001

Cited by 99 publications

(91 citation statements)

References 44 publications

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“…In terms of pharmacotherapy for obesity, only a few new drugs have been registered over the last few years (Arch 2015, Patel 2015. Despite the many known peptidic hormones involved in food intake regulation, only one of them, liraglutide, a peptidic drug acting through the GLP1 receptor, has recently been approved for anti-obesity treatment.…”

Section: Discussionmentioning

confidence: 99%

“…The ideal anti-obesity drug should produce sustained weight loss with minimal side effects. Recent progress in an understanding of peptidergic signaling of hunger and satiety, both from the gastrointestinal tract and its upstream pathways in the hypothalamus, have opened the possibility for using anorexigenic neuropeptides in obesity treatment (Arch 2015, Patel 2015.…”

Section: Introductionmentioning

confidence: 99%

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Palmitoylated PrRP analog decreases body weight in DIO rats but not in ZDF rats

Holubová

Zemenová

Mikulášková

et al. 2016

Journal of Endocrinology

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Anorexigenic neuropeptides produced and acting in the brain have the potential to decrease food intake and ameliorate obesity, but are ineffective after peripheral application, owing to a limited ability to cross the blood–brain barrier. We have designed lipidized analogs of prolactin-releasing peptide (PrRP), which is involved in energy balance regulation as demonstrated by obesity phenotypes of bothPrrp-knockout andPrrpreceptor-knockout mice. The aim of this study was to characterize the subchronic effect of a palmitoylated PrRP analog in two rat models of obesity and diabetes: diet-induced obese Sprague–Dawley rats and leptin receptor-deficient Zucker diabetic (ZDF) rats. In the rats with diet-induced obesity (DIO), a two-week intraperitoneal treatment with palmitoylated PrRP lowered food intake by 24% and body weight by 8%. This treatment also improved glucose tolerance and tended to decrease leptin levels and adipose tissue masses in a dose-dependent manner. In contrast, in ZDF rats, the same treatment with palmitoylated PrRP lowered food intake but did not significantly affect body weight or glucose tolerance, probably in consequence of severe leptin resistance due to a nonfunctional leptin receptor. Our data indicate a good efficacy of lipidized PrRP in DIO rats. Thus, the strong anorexigenic, body weight-reducing, and glucose tolerance-improving effects make palmitoylated PrRP an attractive candidate for anti-obesity treatment.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Palmitoylated PrRP analog decreases body weight in DIO rats but not in ZDF rats

Holubová

Zemenová

Mikulášková

et al. 2016

Journal of Endocrinology

View full text Add to dashboard Cite

show abstract

“…Obesity leads to multiple chronic morbidities such as fatty liver, type 2 diabetes and cardiovascular diseases, and even increases the risk of several cancers. Five drugs have been approved by the Food and Drug Administration (FDA) for long-term weight management; however, there is still a long way to go before achieving satisfactory clinical outcome due to modest efficacy and unfavorable side effects [2]. Current anti-obesity medications focus mainly on restricting energy intake either by decreasing fat absorption or by suppressing appetite.…”

Section: Dear Editormentioning

confidence: 99%

Artemisinin derivatives prevent obesity by inducing browning of WAT and enhancing BAT function

et al. 2016

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“…The ideal antiobesity drug should produce sustained weight loss with minimal side effects. Recent progress in an understanding of peptidergic signaling of hunger and satiety, both from the gastrointestinal tract and its upstream pathways in the hypothalamus, has opened the possibility for the use of anorexigenic neuropeptides in obesity treatment (Arch 2015, Patel 2015.…”

Section: Introductionmentioning

confidence: 99%

Prolactin-releasing peptide: a new tool for obesity treatment

Kuneš

Pražienková

Popelová

et al. 2016

Journal of Endocrinology

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Obesity is an escalating epidemic, but an effective noninvasive therapy is still scarce. For obesity treatment, anorexigenic neuropeptides are promising tools, but their delivery from the periphery to the brain is complicated because peptides have a low stability and limited ability to cross the blood-brain barrier. In this review, we summarize results of several studies with our newly designed lipidized analogs of prolactin-releasing peptide (PrRP). PrRP is involved in feeding and energy balance regulation as demonstrated by obesity phenotypes of both PrRP-and PrRP-receptor-knockout mice. Lipidized PrRP analogs showed binding affinity and signaling in PrRP receptor-expressing cells similar to natural PrRP. Moreover, these analogs showed high binding affinity also to anorexigenic neuropeptide FF (NPFF)-2 receptor. Acute peripheral administration of myristoylated and palmitoylated PrRP analogs to mice and rats induced strong and long-lasting anorexigenic effects and neuronal activation in the brain areas involved in food intake regulation. Two-week-long subcutaneous administration of palmitoylated PrRP31 and myristoylated PrRP20 lowered food intake, body weight, improved metabolic parameters and attenuated lipogenesis in mice with diet-induced obesity. A strong anorexigenic, body weight-reducing and glucose tolerance-improving effect of palmitoylated-PrRP31 was shown also in diet-induced obese rats after its repeated 2-week-long peripheral administration. Thus, the strong anorexigenic and body weight-reducing effects of palmitoylated PrRP31 and myristoylated PrRP20 make these analogs attractive candidates for antiobesity treatment. Moreover, PrRP receptor might be a new target for obesity therapy.

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Pharmacotherapy for the management of obesity

Cited by 99 publications

References 44 publications

Palmitoylated PrRP analog decreases body weight in DIO rats but not in ZDF rats

Palmitoylated PrRP analog decreases body weight in DIO rats but not in ZDF rats

Artemisinin derivatives prevent obesity by inducing browning of WAT and enhancing BAT function

Prolactin-releasing peptide: a new tool for obesity treatment

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