AI Article Synopsis
- Urotensin-II (UT-II) plays a role in regulating cardiovascular health and disease, prompting research into its receptor, GPR-14.
- A cyclic hexapeptide library based on the UT-II sequence led to the discovery of a new synthetic sequence (WK[Xaa]) that effectively activates the receptor, unlike the previously used WK[Y] sequence.
- Compound 1, identified in the study, exhibited strong agonistic activity with an EC(50) of 6.94 nM, while structural analysis revealed it lacked a typical secondary structure, paving the way for further exploration of UT-II's active conformation and new ligand discovery for GPR-14.
Article Abstract
Urotensin-II (UT-II) is thought to be involved in the regulation of cardiovascular homeostasis and pathology. A head-to-tail cyclic hexapeptide library based on UT-II sequence was designed, synthesized, and evaluated by the activity on the UT-II receptor (GPR-14). A new synthetic sequence, WK[Xaa] (Xaa: amino acid with aromatic side chain), was identified as a characteristic minimum fragment activating hUT-II receptor instead of the WK[Y] sequence. Compound 1 showed an agonistic activity with an EC(50) value of 6.94 nM. The conformational investigation suggested that 1 did not have typical secondary structure in the message sequence. Structural analyses may enable us to investigate the active conformation of UT-II and lead to the identification of new ligands for GPR-14.
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| http://dx.doi.org/10.1016/j.bmc.2009.07.058 | DOI Listing |
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