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COMPOUNDS, COMPOSITIONS, METHODS, AND USES FOR TREATING LEPTIN RESISTANCE, OBESITY, DIABETES MELLITUS AND METABOLIC SYNDROME
COMPOUNDS, COMPOSITIONS, METHODS, AND USES FOR TREATING LEPTIN RESISTANCE, OBESITY, DIABETES MELLITUS AND METABOLIC SYNDROME
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机译:用于治疗瘦蛋白抗性,肥胖,糖尿病和代谢综合征的化合物,组合物,方法和用途
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摘要
Novel leptin and leptin-fusion protein-small molecule drug conjugates are disclosed, where conjugation takes place through the use of cleavable and non-cleavable linkers. The small molecules chemically linked to the protein carrier are imported into the specific leptin-responsive target tissue or cell through receptor-mediated endocytosis and released from the carrier protein through enzymatic cleavage of the linker-drug moiety or through lysosomal degradation of the carrier protein. Free drug then act to modify leptin receptor-triggered biochemical pathways that are altered in conditions of leptin-resistance. Drug will correct altered pathway allowing resensitization of receptor signaling. This can greatly aid in the resolution of pathologies either initiated at the onset of leptin resistance or exacerbated by it.
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