Stress-protective effect of the KKRR synthetic peptide corresponding to the 15–18 sequence of human adrenocorticotropic hormone

The activity of the KKRR synthetic peptide corresponding to the 15-18 sequence of human adrenocorticotropic hormone (ACTH) and its analogues: KKKK, RRRR, RRKK, kKRR, KkRR, KKrR, and KKRr (amino acid residues of the D configuration are designated by small letters), was studied in vivo on rats under c...

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Bibliographic Details
Published inRussian journal of bioorganic chemistry Vol. 35; no. 1; pp. 19 - 23
Main Authors Sadovnikov, V. B., Sazhin, A. I., Zolotarev, Yu. A., Navolotskaya, E. V.
Format Journal Article
LanguageEnglish
Published Dordrecht SP MAIK Nauka/Interperiodica 2009
Subjects
Biochemistry
Biomedical and Life Sciences
Biomedicine
Bioorganic Chemistry
Life Sciences
Organic Chemistry
stress
peptides
adrenocorticotropic hormone (ACTH)
receptors
adrenal cortex
adenylate cyclase
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Summary:The activity of the KKRR synthetic peptide corresponding to the 15-18 sequence of human adrenocorticotropic hormone (ACTH) and its analogues: KKKK, RRRR, RRKK, kKRR, KkRR, KKrR, and KKRr (amino acid residues of the D configuration are designated by small letters), was studied in vivo on rats under cold and heat shock. Intranasal administration of the KKRR peptide at doses of 2–10 μg/animal 1 day before the shock was found to prevent a dramatic increase in the level of corticosterone in rat adrenal glands and blood plasma caused by the temperature effect. Amino acid substitutions in the KKRR peptide were shown to result in abrupt decrease in its activity. The peptide analogues exhibit a low stress-protective activity and had a low affinity for the ACTH receptor.
ISSN:1068-1620
1608-330X
DOI:10.1134/S1068162009010038