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Grant: Collaborative Research and Development Grants

University of Ontario Institute of Technology

$28,000.00

Development of non-covalent chemical probes for mu, delta and kappa opioid receptors

FY 2016-17

Summary
Despite the fact that codeine has been isolated over 150 years ago little is known about its interaction with opioid receptors. The aim of the project is to deepen a fundamental understanding of the ligand-opioid receptor interaction. Our efforts will focus on the systematic synthesis of codeine dimers as non-covalent chemical probes for opioid receptors. Analysis of novel non-covalently bound dimers to the opioid receptor will lead to a better understanding of ligand-receptor interaction and new structure-function relationships will emerge from this study. The generation of new scientific knowledge will enhance our understanding of the structural requirements that govern this ligand-receptor function, and this new knowledge may shed light in comprehending other novel ligand-receptor pairs. The results of this project may eventually lead to the development of a new class of safe drugs by Purdue Pharma. Therefore, Canadians will benefit immensely from the availability of safe non-addictive painkillers. In addition to pain management, opioid receptors are widely involved in various physiological and pathophysiological activities, including the regulation of cell proliferation, emotional response, epileptic seizures, immune function, feeding, obesity, respiratory and cardiovascular control as well as some neurodegenerative disorders including Alzheimer's and Parkinson's diseases. Therefore, this study will have a broad impact from pharmacological point of view.
Program
Collaborative Research and Development Grants
Location
Ontario, Canada
Recipient Type
Academia
Type
Grant
Source
NSERC's Awards Data

As published

Application id
500505-2016
Name nom
Bolshan, Yuri
Department département
Science, Faculty of
Organization id
19222
Institution établissement
University of Ontario Institute of Technology
Province en
Ontario
Province fr
Ontario
Country en
CANADA
Country fr
CANADA
Fiscal year exercice financier
2016
Competition year année de concours
2016
Award amount
28000
Program id
CRDPJ
Program name en
Collaborative Research and Development Grants
Program name fr
Subventions de recherche et développement coopérative
Group en
Research partnerships programs
Group fr
Programmes de partenariat
Committee code
96
Committee name en
RPP Internal Decision Cttee
Committee name fr
Cté de décision interne - PPR
Area of application code
504
Area of application group en
Manufacturing processes and products
Area of application group fr
Procédés et produits industriels
Area of application en
Human pharmaceuticals
Area of application fr
Produits pharmaceutiques administrables à l'homme
Research subject code
3700
Research subject group en
Organic chemistry
Research subject group fr
Chimie organique
Research subject en
Organic chemistry
Research subject fr
Chimie organique
Partie
1
Nb partie
2
Application title
Development of non-covalent chemical probes for mu, delta and kappa opioid receptors
Keyword
NSERC
Application summary
Despite the fact that codeine has been isolated over 150 years ago little is known about its interaction with opioid receptors. The aim of the project is to deepen a fundamental understanding of the ligand-opioid receptor interaction. Our efforts will focus on the systematic synthesis of codeine dimers as non-covalent chemical probes for opioid receptors. Analysis of novel non-covalently bound dimers to the opioid receptor will lead to a better understanding of ligand-receptor interaction and new structure-function relationships will emerge from this study. The generation of new scientific knowledge will enhance our understanding of the structural requirements that govern this ligand-receptor function, and this new knowledge may shed light in comprehending other novel ligand-receptor pairs. The results of this project may eventually lead to the development of a new class of safe drugs by Purdue Pharma. Therefore, Canadians will benefit immensely from the availability of safe non-addictive painkillers. In addition to pain management, opioid receptors are widely involved in various physiological and pathophysiological activities, including the regulation of cell proliferation, emotional response, epileptic seizures, immune function, feeding, obesity, respiratory and cardiovascular control as well as some neurodegenerative disorders including Alzheimer's and Parkinson's diseases. Therefore, this study will have a broad impact from pharmacological point of view.