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ADRENOCORTICOTROPIC HORMONE ANALOGS AND RELATED METHODS

机译:肾上腺皮质激素类似物和相关方法

摘要

ACTH analog compounds of the present invention include compounds comprising an ACTH peptide sequence with one or more structural modifications that can have one or more of the following preferred ACTH analog biological functions: (1) reduction of corticosteroid secretion by adrenal membrane in the presence of the ACTH analog compared to unmodified ACTH, (2) reduction of corticosteroid secretion by adrenal membrane in the presence of endogenous ACTH and (3) increased MC-2R binding affinity with reduced activation of the MC-2R receptor compared to unmodified ACTH binding to the MC-2R melanocortin. The ACTH analog compounds of the present invention are therefore useful for treatment or prevention of diseases and disorders related to ACTH, ACTH receptors or corticosteroid secretion, such as premature labor and Cushing's Disease.
机译:本发明的ACTH类似物化合物包括包含具有一个或多个结构修饰的ACTH肽序列的化合物,该结构可以具有以下优选的ACTH类似物生物学功能中的一种或多种:(1)在存在所述肽时,肾上腺膜减少皮质类固醇分泌。与未经修饰的ACTH相比,ACTH与未经修饰的ACTH相比,(2)在存在内源性ACTH的情况下减少肾上腺皮质皮质类固醇的分泌,以及(3)与未经修饰的ACTH与MC的结合相比,MC-2R的结合亲和力增加,而MC-2R受体的激活减少-2R黑皮质素。因此,本发明的ACTH类似物化合物可用于治疗或预防与ACTH,ACTH受体或皮质类固醇分泌有关的疾病和病症,例如早产和库欣病。

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