Seid Hadžić

Medical University of Vienna

Author Statistics

Papers

Citation

H-Index

i-10 index

Research Trends

Author Order

Document Type

Co-Authors

Stuart M. Brierley

South Australian Health and Medical Research Institute

Edin Muratspahić

University of Washington

Richard J. Clark

Next Energy Technologies (United States)

Leopold Duerrauer

University of Queensland

Christian W. Gruber

Medical University of Vienna

Nataša Tomašević

Medical University of Vienna

Spyridon Sideromenos

Medical University of Vienna

Johannes Koehbach

ARC Centre of Excellence for Innovations in Peptide and Protein Science

Gudrun Schober

South Australian Health and Medical Research Institute

Joel Castro

South Australian Health and Medical Research Institute

Cooperative Institutions

Medical University of Vienna

University of Queensland

Australian Research Council

Brisbane School of Theology

South Australian Health and Medical Research Institute

University of Adelaide

Flinders University

Adelaide Institute for Sleep Health

ARC Centre of Excellence for Innovations in Peptide and Protein Science

Royal Adelaide Hospital

Author Statistics

Papers

Citation

H-Index

i-10 index

Research Field

Design of a Stable Cyclic Peptide Analgesic Derived from Sunflower Seeds that Targets the κ-Opioid Receptor for the Treatment of Chronic Abdominal Pain

Journal of Medicinal Chemistry (2021)

Edin Muratspahić Nataša Tomašević Johannes Koehbach Leopold Duerrauer Seid Hadžić

The rising opioid crisis has become a worldwide societal and public health burden, resulting from the abuse of prescription opioids. Targeting the κ-opioid receptor (KOR) in the periphery has emerged as a powerful approach to develop novel pain medications without central side effects. Inspired by the traditional use of sunflower (Helianthus annuus) preparations for analgesic purposes, we developed novel stabilized KOR ligands (termed as helianorphins) by incorporating different dynorphin A sequence fragments into a cyclic sunflower peptide scaffold. As a result, helianorphin-19 selectively bound to and fully activated the KOR with nanomolar potency. Importantly, helianorphin-19 exhibited strong KOR-specific peripheral analgesic activity in a mouse model of chronic visceral pain, without inducing unwanted central effects on motor coordination/sedation. Our study provides a proof of principle that cyclic peptides from plants may be used as templates to develop potent and stable peptide analgesics applicable via enteric administration by targeting the peripheral KOR for the treatment of chronic abdominal pain.

Dynorphin

10.1021/acs.jmedchem.1c00158

Cite

Citations (25)