Grant: Project Grant
Research Institute of the McGill University Health Centre
$841,500.00
Understanding the allosteric and functional selectivity regulation of the Prostaglandin F2 receptor.
FY 2018-19
Summary
Our research focuses on a class of membrane receptor for hormones know as prostaglandins that are involved in normal delivery, but that also play a role in premature birth. Pharmacological therapies targeting these receptors to prevent premature birth would greatly reduce the personal and socio-economical burden associated with this problem, for which no safe drugs exist. Our research has unveiled the properties of a new class of drugs that act in an unconventional way on these receptors to selectively affect the response of the natural hormone prostaglandin and regulate uterine contraction. We propose to characterize the functional domains of these receptors, known as "allosteric" sites, which are targeted by our newly discovered compounds, to iteratively generate more selective and efficacious drugs. Complications related to preterm birth contribute to 40% of all neonatal deaths and have continued increasing in the last 30 years. Our research should thus have great impact on managing preterm delivery in Canadian women, which is the primary cause of neonatal mortality.
Department
Program
Project Grant
Location
Quebec, Canada
Type
Grant
Source
CIHR Funding Decisions Database
As published
Id
389406
Name
Laporte Stéphane A
Region
Québec
Country
Canada
Orgtype
Institution Paid; Research Institution
Instname2
Human Development, Child and Youth Health
Theme2
Biomedical
Prcname2
Pharmacology & Toxicology
Projecttitle
Understanding the allosteric and functional selectivity regulation of the Prostaglandin F2 receptor.
Programtype2
Operating Grants
Orgnameinp2
Research Institute of the McGill University Health Centre
Cihramount2
$841,500
Cihrequipment2
$0
Programname2
Project Grant
Keyworddelim
Bret/Fret; Crispr/Cas9; Gpcr; Molecular Pharmacology; Myometrial Cells; Pre-Term Birth; Prostaglandin F2 Alpha Receptor; Small Molecules Therapeutics; Structure Function; Tocolytics
Abstract
Our research focuses on a class of membrane receptor for hormones know as prostaglandins that are involved in normal delivery, but that also play a role in premature birth. Pharmacological therapies targeting these receptors to prevent premature birth would greatly reduce the personal and socio-economical burden associated with this problem, for which no safe drugs exist. Our research has unveiled the properties of a new class of drugs that act in an unconventional way on these receptors to selectively affect the response of the natural hormone prostaglandin and regulate uterine contraction. We propose to characterize the functional domains of these receptors, known as "allosteric" sites, which are targeted by our newly discovered compounds, to iteratively generate more selective and efficacious drugs. Complications related to preterm birth contribute to 40% of all neonatal deaths and have continued increasing in the last 30 years. Our research should thus have great impact on managing preterm delivery in Canadian women, which is the primary cause of neonatal mortality.
Competitiondate
201809
Approvedterm2
5 yrs 0 mth
Pinamesdelim
Laporte, Stéphane A
Approvedterm
5 ans 0 mois
Cihrcontribution2
~ $841,500~ $0~
