Literature DB >> 28139906

Heteromer Induction: An Approach to Unique Pharmacology?

Philip S Portoghese1, Eyup Akgün1, Mary M Lunzer1.   

Abstract

It is proposed that two types of opioid receptor heteromers exist: a) those that are constitutive and b) those that are induced by bivalent ligands. Mu opioid agonists interact with constitutive MOR-DOR heteromer to mediate tolerance and dependence. Bivalent ligand, MDAN21, is devoid of these adverse effects by virtue of its DOR antagonist pharmacophore. We propose that bivalent ligands MMG22 and MCC22 induce colocalized receptors to form heteromers (MOR-mGluR5 and MOR-CCR5, respectively) that do not occur naturally, thereby promoting unique pharmacology. Heteromer induction with bivalent ligands offers a general approach to unique pharmacology that complements traditional SAR.

Entities:  

Keywords:  DOR; MOR; heterodimer; opiod receptor

Mesh：

Substances：

Year:  2017        PMID： 28139906     DOI： 10.1021/acschemneuro.7b00002

Source DB:  PubMed          Journal:  ACS Chem Neurosci        ISSN： 1948-7193            Impact factor:   4.418


  11 in total

1.  The bivalent ligand MCC22 potently attenuates hyperalgesia in a mouse model of cisplatin-evoked neuropathic pain without tolerance or reward.

Authors:  Giuseppe Cataldo; Samuel J Erb; Mary M Lunzer; Nhungoc Luong; Eyup Akgün; Philip S Portoghese; Julie K Olson; Donald A Simone
Journal:  Neuropharmacology       Date:  2019-04-07       Impact factor: 5.250

2.  CCR5 mediates HIV-1 Tat-induced neuroinflammation and influences morphine tolerance, dependence, and reward.

Authors:  Maciej Gonek; Virginia D McLane; David L Stevens; Kumiko Lippold; Hamid I Akbarali; Pamela E Knapp; William L Dewey; Kurt F Hauser; Jason J Paris
Journal:  Brain Behav Immun       Date:  2017-11-13       Impact factor: 7.217

3.  Developing a Biased Unmatched Bivalent Ligand (BUmBL) Design Strategy to Target the GPCR Homodimer Allosteric Signaling (cAMP over β-Arrestin 2 Recruitment) Within the Melanocortin Receptors.

Authors:  Cody J Lensing; Katie T Freeman; Sathya M Schnell; Robert C Speth; Adam T Zarth; Carrie Haskell-Luevano
Journal:  J Med Chem       Date:  2018-05-09       Impact factor: 7.446

4.  Targeting MOR-mGluR5 heteromers reduces bone cancer pain by activating MOR and inhibiting mGluR5.

Authors:  Sarah S Shueb; Samuel J Erb; Mary M Lunzer; Rebecca Speltz; Catherine Harding-Rose; Eyup Akgün; Donald A Simone; Philip S Portoghese
Journal:  Neuropharmacology       Date:  2019-07-01       Impact factor: 5.250

5.  Synthesis and Pharmacology of a Novel μ-δ Opioid Receptor Heteromer-Selective Agonist Based on the Carfentanyl Template.

Authors:  Abdelfattah Faouzi; Rajendra Uprety; Ivone Gomes; Nicolas Massaly; Attila I Keresztes; Valerie Le Rouzic; Achla Gupta; Tiffany Zhang; Hye Jean Yoon; Michael Ansonoff; Abdullah Allaoa; Ying Xian Pan; John Pintar; Jose A Morón; John M Streicher; Lakshmi A Devi; Susruta Majumdar
Journal:  J Med Chem       Date:  2020-11-10       Impact factor: 7.446

6.  Activation of µ-δ opioid receptor heteromers inhibits neuropathic pain behavior in rodents.

Authors:  Vinod Tiwari; Shao-Qiu He; Qian Huang; Lingli Liang; Fei Yang; Zhiyong Chen; Vineeta Tiwari; Wakako Fujita; Lakshmi A Devi; Xinzhong Dong; Yun Guan; Srinivasa N Raja
Journal:  Pain       Date:  2020-04       Impact factor: 7.926

7.  The size matters? A computational tool to design bivalent ligands.

Authors:  Laura Pérez-Benito; Andrew Henry; Minos-Timotheos Matsoukas; Laura Lopez; Daniel Pulido; Miriam Royo; Arnau Cordomí; Gary Tresadern; Leonardo Pardo
Journal:  Bioinformatics       Date:  2018-11-15       Impact factor: 6.937

8.  Comprehensive molecular pharmacology screening reveals potential new receptor interactions for clinically relevant opioids.

Authors:  Keith M Olson; David I Duron; Daniel Womer; Ryan Fell; John M Streicher
Journal:  PLoS One       Date:  2019-06-06       Impact factor: 3.240

9.  The Balance of MU-Opioid, Dopamine D2 and Adenosine A2A Heteroreceptor Complexes in the Ventral Striatal-Pallidal GABA Antireward Neurons May Have a Significant Role in Morphine and Cocaine Use Disorders.

Authors:  Dasiel O Borroto-Escuela; Karolina Wydra; Ramon Fores-Pons; Lakshmi Vasudevan; Wilber Romero-Fernandez; Małgorzata Frankowska; Luca Ferraro; Sarah Beggiato; Minerva Crespo-Ramirez; Alicia Rivera; Luisa L Rocha; Miguel Perez de la Mora; Christophe Stove; Małgorzata Filip; Kjell Fuxe
Journal:  Front Pharmacol       Date:  2021-03-15       Impact factor: 5.810

10.  Influence of functional gene polymorphisms on human behaviour: the case of CCR5.

Authors:  Paul R Albert
Journal:  J Psychiatry Neurosci       Date:  2021-12-16       Impact factor: 6.186
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