|Title||Structure-activity relationships of non-opioid [des-Arg(7)]-dynorphin A analogues for bradykinin receptors.|
|Publication Type||Journal Article|
|Year of Publication||2014|
|Authors||Lee YSun, Rankin D, Hall SM, Ramos-Colon C, Ortiz JJuan, Kupp R, Porreca F, Lai J, Hruby VJ|
|Journal||Bioorg Med Chem Lett|
|Date Published||2014 Nov 01|
|Keywords||Animals, Brain, Dynorphins, Neurotransmitter Agents, Rats, Receptors, Bradykinin, Structure-Activity Relationship|
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.
|Alternate Journal||Bioorg. Med. Chem. Lett.|
|PubMed Central ID||PMC4250343|
|Grant List||P01 DA006284 / DA / NIDA NIH HHS / United States |
R01 DA013449 / DA / NIDA NIH HHS / United States
NIDA P01DA006284 / / PHS HHS / United States
R01DA013449 / DA / NIDA NIH HHS / United States
Structure-activity relationships of non-opioid [des-Arg(7)]-dynorphin A analogues for bradykinin receptors.
Faculty Member Reference:
Yeon Sun Lee, Ph.D.
Frank Porreca, Ph.D.