Pharmacological activity of a Bv8 analogue modified in position 24.

ABSTRACT:

Background and purpose

The amphibian peptide Bv8 induces potent nociceptive sensitization in rodents. Its mammalian homologue, prokineticin 2 (PROK2), is strongly up-regulated in inflamed tissues and is a major determinant in triggering inflammatory pain. Bv8 and PROK2 activate two closely related GPCRs, PK(1) and PK(2) , in a relatively non-selective fashion. To characterize better the roles of the two receptors in hyperalgesia and to obtain ligands whose binding affinity and efficacy differed for the two receptors, we modified the Bv8 molecule in regions essential for receptor recognition and activation.

Experimental approach

We modified the Bv8 molecule by substituting Trp in position 24 with Ala (A-24) and compared it with Bv8 for binding and activating PK(1) and PK(2) r

SUBMITTER: Lattanzi R 

PROVIDER: S-EPMC3417421 | biostudies-literature | 2012 Jun

REPOSITORIES: biostudies-literature