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Agonists and Partial Antagonists Acting on the Leptin - Leptin Receptor Interface

机译：作用于瘦素 - 瘦素受体界面的激动剂和部分拮抗剂

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Leptin is a neurohormone regulating energy balance and food intake acting in the hypothalamus [1]. Leptin can also modulate immune response, fertility, and hematopoiesis, acting as a mitogen, metabolic regulator, or pro-angiogenic factor. Both leptin and the leptin receptor (ObR) are overexpressed in breast and colorectal cancer [2]. An ever increasing wealth of evidence suggests that leptin is a novel pharmaceutical target for diseases related to leptin overabundance (cancer) as well as deficit (lipodystrophy or anorexia-related infertility). The full form of ObR is 1,165 amino acids long and contains the extracellular, transmembrane, and intracellular domains. The extracellular domain binds ligand, whereas the intracellular tail recruits and activates signaling substrates. Leptin appears to interact with its receptor at three discontinuous surfaces, at each with two arms [3]. Interfering with these surfaces may decrease or increase the efficiency of downstream ObR signaling in target tissues. Recombinant leptin mutants (all alanine) were suggested to act as true antagonists on STAT3 activation [4,5]. The mutated residues were as follows: in Site I Leu39-Asp40, in Site III Tyr119, and in Site III Ser120-Thr121.
机译：瘦素是一种神经核龙，在下丘脑中的能量平衡和食物摄入量[1]。瘦素还可以调节免疫反应，生育率和血液缺陷，其作为丝裂原，代谢调节剂或促血管生成因子。瘦素和瘦素受体（OBR）都在乳腺癌和结肠直肠癌中过表达[2]。越来越丰富的证据表明，瘦素是与瘦素渗透（癌症）相关的疾病的新药靶标以及缺陷（脂肪育药或厌食症相关的不孕症）。全形式的OBR是1,165个氨基酸长，含有细胞外，跨膜和细胞内域。细胞外结构域结合配体，而细胞内尾部再次投掷并激活信号衬底。瘦素似乎在三个不连续表面下与其受体相互作用，每个臂都有两个臂[3]。干扰这些表面可能会降低或提高目标组织中下游OBR信号传导的效率。建议重组瘦蛋白突变体（所有丙氨酸）作为真实拮抗剂对Stat3活化[4,5]。突变的残基如下：在现场I Leu39-ASP40，在地点III TYR119，在SERI III Ser120-Thr121中。

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