METHOD FOR DETERMINING FUNCTIONAL ACTIVITY PROFILE OF RECEPTOR PEPTIDES-AGONISTS ACTIVATED BY PROTEASE TYPE 1 UNDER EXPERIMENTAL CONDITIONS IMITATING ISCHEMIC Russian patent published in 2021 - IPC C07K2/00 

FIELD: biochemistry.

SUBSTANCE: invention relates to the field of biochemistry, namely to a method for determining the profile of the functional activity of peptides-analogues of the N-terminal fragment of receptors activated by proteases of type 1, based on the dependence of their effects on the activity of β-arrestin-2. The method includes determining the profile of the functional activity of peptides-analogues of the N-terminal fragment of receptors activated by type 1 proteases under experimental conditions mimicking ischemic, in vitro and / or in vivo at least 4 experimental groups, of which at least two subgroups are formed which include at least groups 1 and 2 with normal β-arrestin-2 activity and at least groups 3 and 4 with suppressed β-arrestin-2 activity, wherein at least groups 1 and 3 are exposed to ischemic conditions only, and groups 2 and 4 are exposed to both ischemic conditions and the test peptide, then the profile of the activity of the peptide is determined by comparing the severity of ischemic lesions between the groups, and if the test peptide alleviates the consequences of experimental ischemia in the group without suppressing the activity of β-arrestin-2 compared with the group without inhibition of β-arrestin-2 activity and without the action of the peptide, and this effect not expressed or less pronounced in the group with suppressed β-arrestin-2 activity compared with the group with suppressed β-arrestin-2 activity and without peptide action, it is concluded that the peptide exhibits an activated protein C activity profile if the peptide aggravates the severity of the experimental ischemia in the group without inhibition of β-arrestin-2 activity compared with the group without inhibition of β-arrestin-2 activity and without peptide action, and this effect is more pronounced in the group with inhibited β-arrestin-2 activity compared to the group with inhibited β-arrestin-2 activity -arrestin-2 and without the action of the peptide, it is concluded that the peptide exhibits the functional activity of thrombin.

EFFECT: invention provides the creation of a test system that allows determining the functional activity of peptides in a short period of time using a minimum number of experimental groups, reagents and biomaterials, characterized by ease of interpretation of the results.

15 cl, 5 dwg, 6 ex