My research is concerned with the design, synthesis, and biological evaluation of ligands for their use as tools and potential analgesic agents at opioid receptors. We are particularly interested in mechanisms for the association of such ligands with opioid receptors. Of particular interest is the role of heteromerization of GPCRs in signaling.
(For a comprehensive list of recent publications, refer to PubMed, a service provided by the National Library of Medicine.)
- Akgün E, Lunzer MM, Tian D, Ansonoff M, Pintar J, Bruce D, Hawkinson JE, Wilcox GL, Portoghese PS. FBNTI, a DOR-aelective antagonist that allosterically activates MOR within a MOR-DOR heteromer. Biochemistry. 2021 May 11;60(18):1413-1419.
- Shueb SS, Erb SJ, Lunzer MM, Speltz R, Harding-Rose C, Akgün E, Simone DA, Portoghese PS. Targeting MOR-mGluR5 heteromers reduces bone cancer pain by activating MOR and inhibiting mGluR5. Neuropharmacology. 2019 Dec 1;160:107690.
- Cataldo G, Lunzer MM, Olson JK, Akgün E, Belcher JD, Vercellotti GM, Portoghese PS, Simone DA. The bivalent ligand MCC22 potently attenuates nociception in a murine model of sickle cell disease. Neuropharmacology. 2019 Nov 1;158:107598.
- Peterson CD, Kitto KF, Akgün E, Lunzer MM, Riedl MS, Vulchanova L, Wilcox GL, Portoghese PS, Fairbanks CA. Bivalent ligand that activates mu opioid receptor and antagonizes mGluR5 receptor reduces neuropathic pain in mice. Pain. 2017;158(12):2431-2441.
- Portoghese PS, Akgün E, Lunzer MM. Heteromer induction: An approach to unique pharmacology? ACS Chem Neurosci. 2017;8(3):426-428.
- Goudie-DeAngelis EM, Abdelhamid RE, Nunez MG, Kissel CL, Kovács KJ, Portoghese PS, Larson AA. Modulation of musculoskeletal hyperalgesia by brown adipose tissue activity in mice. Pain. 2016;157(11):2561-2570.
- Akgün E, Javed MI, Lunzer MM, Powers MD, Sham YY, Watanabe Y, Portoghese PS. Inhibition of Inflammatory and Neuropathic Pain by Targeting a Mu Opioid Receptor/Chemokine Receptor5 Heteromer (MOR-CCR5). J Med Chem. 2015;58(21):8647-57.
- Smeester BA, Lunzer MM, Akgün E, Beitz AJ, Portoghese PS. Targeting putative mu opioid/metabotropic glutamate receptor-5 heteromers produces potent antinociception in a chronic murine bone cancer model. Eur J Pharmacol. 2014;743:48-52.
- Le Naour M, Lunzer MM, Powers MD, Kalyuzhny AE, Benneyworth MA, Thomas MJ, Portoghese PS. Putative kappa opioid heteromers as targets for developing analgesics free of adverse effects. J Med Chem. 2014;57(15):6383-92.