Structure-activity relationships of non-opioid [des-Arg7]-dynorphin A analogues for bradykinin receptors

Yeon Sun Lee, David Rankin, Sara M. Hall, Cyf Ramos-Colon, Jose Juan Ortiz, Robert Kupp, Frank Porreca, Josephine Lai, Victor J. Hruby

Research output: Contribution to journalArticlepeer-review

8 Scopus citations

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-Arg7]-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-Arg7]-Dyn A analogs and confirmed that all of the [des-Arg7]-Dyn A analogues showed good binding affinities at the BRs.

Original languageEnglish (US)
Pages (from-to)4976-4979
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume24
Issue number21
DOIs
StatePublished - Nov 1 2014

Keywords

  • Bradykinin receptors
  • Chronic pain
  • Non-opioid dynorphin A
  • Structure-activity relationship
  • pH sensitivity

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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