Reference
Lee, Yeon Sun, et al. “Structure-Activity Relationships of Non-Opioid [des-Arg(7)]-Dynorphin A Analogues for Bradykinin Receptors”. Bioorg Med Chem Lett, vol. 24, no. 21, Jan. 2014, pp. 4976-9, https://doi.org/10.1016/j.bmcl.2014.09.033.
Abstract
In our earlier studies, bradykinin receptors (BRs) were identified as a potential target for the neuroexcitatory effects of dynorphin A (Dyn A) in the central nervous system (CNS), and [des-Arg(7)]-Dyn A-(4-11) (6) was discovered as a lead ligand to modulate Dyn A-(2-13) induced neuroexcitatory effects in the CNS as an antagonist. In an effort to gain insights into key structural features of the Dyn A for the BRs, we pursued further structure-activity relationships (SAR) study on the [des-Arg(7)]-Dyn A analogs and confirmed that all of the [des-Arg(7)]-Dyn A analogues showed good binding affinities at the BRs.