ADRENOCORTICOTROPIC HORMONE ANALOGUES AND RELATED METHODS Russian patent published in 2010 - IPC C07K14/695 A61K38/35 

FIELD: medicine.

SUBSTANCE: there is offered adrenocorticotropic hormone (ACTH) analogue consisting of 24 amino acid residues and representing a S-truncated natural human peptide (hACTH 1-24) wherein the sequence Lys¹⁵-Lys¹⁶-Arg¹⁷-Arg¹⁸-Pro¹⁹ is replaced by the sequence Lys¹⁵-Arg¹⁶-Ala¹⁷-Ala¹⁸-Trp¹⁹. A new mutant ACTH-form shows such properties, as (1) reduced corticosteroid secretion by the adrenal membrane with the ACTH analogue added, as compared with modified ACTH; (2) reduced corticosteroid secretion by the adrenal membrane with endogenic ACTH added, and (3) higher MC-2R fixation affinity with lower MC-2R receptor activation as compared with a version of non-modified ACTH fixation.

EFFECT: whole set of properties characterising ACTH analogue under the invention, allows to use it as directly, and in a pharmaceutical composition for treating ACTN-associated conditions, particularly in Cushing disease.

11 cl, 5 dwg, 5 tbl, 5 ex