Scolaro Laura, Cassone Marco, Kolaczynski Jerzy W, Otvos Laszlo, Surmacz Eva
a Temple University, Philadelphia, PA 19122, USA.
b UMDNJ-Robert Wood Johnson Medical School, NJ, USA.
Expert Rev Endocrinol Metab. 2010 Nov;5(6):875-889. doi: 10.1586/eem.10.61.
Leptin, a pluripotent adipokine, has been discovered as a hormone controlling energy balance in hypothalamic neuroendocrine centers. In addition, recent studies provided ample evidence that leptin can be produced by cells other than adipocytes, and that the hormone can regulate many physiological processes other than energy balance and appetite. In this context, it is not surprising that both leptin excess as well as leptin insufficiency have been implicated in various pathologies. Consequently, despite initially disappointing results with recombinant leptin as the drug for obesity management, new leptin receptor modifiers have been developed and emerged as potential treatment modalities for numerous metabolic, immunological and neoplastic diseases. The major focus of this paper is a systematic review of current experimental leptin-based therapies, including pharmacological advantages and limitations of each prodrug category.
瘦素是一种多能脂肪因子，已被发现是一种在下丘脑神经内分泌中心控制能量平衡的激素。此外，最近的研究提供了充分的证据表明，瘦素可由脂肪细胞以外的细胞产生，且该激素可调节能量平衡和食欲以外的许多生理过程。在这种情况下，瘦素过多和瘦素不足均与各种病理状况有关也就不足为奇了。因此，尽管最初将重组瘦素作为肥胖管理药物的结果令人失望，但新的瘦素受体修饰剂已被开发出来，并成为众多代谢、免疫和肿瘤疾病的潜在治疗方式。本文的主要重点是对当前基于瘦素的实验性疗法进行系统综述，包括每种前药类别的药理学优势和局限性。
