1.
Chem Biol Drug Des
; 88(4): 615-9, 2016 10.
Artigo
em Inglês
| MEDLINE
| ID: mdl-27203574
RESUMO
As a unique endogenous opioid ligand, dynorphin A shows paradoxical neuroexcitatory effects at bradykinin receptors, and the effects are known to be amplified by the upregulation of dynorphin A under chronic pain and inflammatory conditions. In our earlier structure-activity relationship studies, the amphipathic dynorphin A fragment, [Des-Arg(7) ]-Dyn A-(4-11), was identified as a pharmacophore for the bradykinin receptors along with key structural features. Here, further modifications of the pharmacophore showed that the position of a Pro residue is also an important feature because of its role in making (or disrupting) a ß-turn or 310 helix structure which is crucial for receptor recognition.