Discovery of a stable tripeptide targeting the N-domain of CRF1 receptor.

ABSTRACT: The corticotropin-releasing factor (CRF) and its CRF1 receptor (CRF₁R) play a central role in the maintenance of homeostasis. Malfunctioning of the CRF/CRF₁R unit is associated with several disorders, such as anxiety and depression. Non-peptide CRF₁R-selective antagonists have been shown to exert anxiolytic and antidepressant effects on experimental animals. However, none of them is in clinical use today because of several side effects, thus demonstrating the need for the development of other more suitable CRF₁R antagonists. In an effort to develop novel CRF₁R antagonists we designed, synthesized and chemically characterized two tripeptide analogues of CRF, namely (R)-LMI and (S)-LMI, having their Leu either in R (or D) or in S (or L)

SUBMITTER: Liapakis G 

PROVIDER: S-EPMC7772748 | biostudies-literature | 2020 Sep

REPOSITORIES: biostudies-literature