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    • 2. 发明授权
    • Mammalian melanocortin receptors and uses
    • 哺乳动物黑皮质素受体和用途
    • US06278038B1
    • 2001-08-21
    • US09097231
    • 1998-06-12
    • Roger D. ConeWenbiao ChenMalcolm J. Low
    • Roger D. ConeWenbiao ChenMalcolm J. Low
    • A01K6700
    • C12Q1/6897A01K2217/075A61K38/00C07K7/56C07K14/4711C07K14/723C12Q1/6876C12Q2600/136C12Q2600/158G01N33/74G01N2333/68G01N2333/695G01N2333/72G01N2333/726G01N2500/00
    • This invention provides methods and reagents for developing naturally-occurring and synthetic agonists and antagonists specific for a mammalian melanocortin receptor, and the use of such agonists and antagonists for treatment and alleviation of dysfunction and disease. The invention specifically provides reagents and methods for developing naturally-occurring and synthetic agonists and antagonists specific for a mammalian melanocortin receptor termed MC5-R. The naturally-occurring and synthetic agonists and antagonists specific for the MC5-R receptor are provided by the invention for the treatment, control, amelioration and alleviation of diseases, and dysfunctional and abnormal states related to thermoregulatory disorders, as well as other diseases relating to exocrine gland disorders, including lacrimal gland dysfunction and sebaceous gland disorders including acne and other skin problems. Also provided by the invention are nucleic acids, constructs, vectors and methods for producing an animal bearing a genetically-disrupted endogenous MC5-R melanocortin receptor, in both the heterozygous and homozygous condition, preferably a rodent and most preferably a mouse. Rodents bearing genetically disrupted MC5-R genes homozygously, termed “gene knockout”rodents in the art, are also advantageously provided.
    • 本发明提供用于开发天然存在的和合成的哺乳动物黑皮质素受体特异的激动剂和拮抗剂的方法和试剂,以及这些激动剂和拮抗剂用于治疗和减轻功能障碍和疾病的用途。 本发明特别提供了用于开发天然存在的和合成的激动剂和特异于哺乳动物黑皮质素受体MC5-R的拮抗剂的试剂和方法。 本发明提供了针对MC5-R受体特异性的天然存在和合成的激动剂和拮抗剂,用于治疗,控制,改善和缓解疾病,以及与体温调节性疾病有关的功能障碍和异常状态以及与 外分泌腺疾病,包括泪腺功能障碍和皮脂腺疾病,包括痤疮和其他皮肤问题。 本发明还提供了在杂合和纯合条件下产生具有遗传破坏的内源性MC5-R黑皮质素受体的动物的核酸,构建体,载体和方法,优选啮齿动物,最优选小鼠。 也有利地提供了在本领域中遗传上破坏的基因破坏的MC5-R基因,称为“基因敲除”啮齿动物。