Grant: Project Grant
University of Toronto
$1,116,900.00
Stage-specific treatment of human non-alcoholic fatty liver disease: elucidating the precise mechanisms of actions of glucagon-like peptide-1 receptor agonists and novel anti-fibrosis molecules
EF 2022-23
Résumé
Non-alcoholic Fatty Liver Disease (NAFLD) is present in 30% of Canadians, reaching >70% in those with diabetes and obesity. Many progress from reversible stages of liver fat accumulation to inflammation (non-alcoholic steatohepatitis-NASH) and fibrosis; to irreversible stages of cirrhosis and cancer. No medicines are yet approved for NAFLD but the most promising are long-acting glucagon-like peptide-1 receptor agonists (GLP-1-RA) which reduced NASH activity in most patients but did not reduce fibrosis, the primary determinant of long-term survival. There is thus great need for anti-fibrosis drugs, which we've just identified to be YAP/TAZ NUAK inhibitors (NUAK-i). The major problems with previous studies are: 1) inability to dissect the different components of this complex disease including mitochondria dysfunction, toxic fat accumulation, inflammation and fibrosis; and elucidate the specific mechanisms each drug actually works on each disease component; and 2) directly test drugs on the different stages of human NAFLD livers whereby each stage likely requires specific drug combinations, recognizing that mouse models may not completely mimic human NAFLD nor accurately predict clinical response to treatment. We surmounted these problems by: 1) developing thin liver slices assays that independently assess fat accumulation (Aim 1), mitochondria function & survival (Aim 2), and fibrosis (Aim 3); and 2) obtaining fresh liver samples from patients undergoing bariatric surgery that span the reversible stages of NAFLD (normal, steatosis, NASH) and various stages of fibrosis. This provides a unique opportunity to test our hypothesis that GLP-1RA and NUAK-i can block or reverse each disease component of NAFLD. This work will: 1) unequivocally show the specific cellular events matched to disease genes and NAFLD stage rescued by GLP-1-RAs and NUAK-i; and 2) provide a precision medicine approach to treat each NAFLD stage with insights directly translatable to clinical trials.
Programme
Project Grant
Bénéficiaire
Emplacement
Ontario, Canada
Type de bénéficiaire
Academia
Type
Grant
Source
CIHR Funding Decisions Database
Tel que publié
Id
468757
Name
Gaisano Herbert Y
Region
Ontario
Country
Canada
Orgtype
Institution Paid; Research Institution
Instname2
Nutrition, Metabolism and Diabetes
Theme2
Biomedical
Prcname2
Hematology, Digestive Disease & Kidney
Projecttitle
Stage-specific treatment of human non-alcoholic fatty liver disease: elucidating the precise mechanisms of actions of glucagon-like peptide-1 receptor agonists and novel anti-fibrosis molecules
Programtype2
Operating Grants
Orgnameinp2
University of Toronto
Cihramount2
$1,116,900
Cihrequipment2
$0
Programname2
Project Grant
Keyworddelim
Anti-Fibrosis Drug; Glucagon-Like Peptide 1; Non-Alcoholic Fatty Liver Disease
Abstract
Non-alcoholic Fatty Liver Disease (NAFLD) is present in 30% of Canadians, reaching >70% in those with diabetes and obesity. Many progress from reversible stages of liver fat accumulation to inflammation (non-alcoholic steatohepatitis-NASH) and fibrosis; to irreversible stages of cirrhosis and cancer. No medicines are yet approved for NAFLD but the most promising are long-acting glucagon-like peptide-1 receptor agonists (GLP-1-RA) which reduced NASH activity in most patients but did not reduce fibrosis, the primary determinant of long-term survival. There is thus great need for anti-fibrosis drugs, which we've just identified to be YAP/TAZ NUAK inhibitors (NUAK-i). The major problems with previous studies are: 1) inability to dissect the different components of this complex disease including mitochondria dysfunction, toxic fat accumulation, inflammation and fibrosis; and elucidate the specific mechanisms each drug actually works on each disease component; and 2) directly test drugs on the different stages of human NAFLD livers whereby each stage likely requires specific drug combinations, recognizing that mouse models may not completely mimic human NAFLD nor accurately predict clinical response to treatment. We surmounted these problems by: 1) developing thin liver slices assays that independently assess fat accumulation (Aim 1), mitochondria function & survival (Aim 2), and fibrosis (Aim 3); and 2) obtaining fresh liver samples from patients undergoing bariatric surgery that span the reversible stages of NAFLD (normal, steatosis, NASH) and various stages of fibrosis. This provides a unique opportunity to test our hypothesis that GLP-1RA and NUAK-i can block or reverse each disease component of NAFLD. This work will: 1) unequivocally show the specific cellular events matched to disease genes and NAFLD stage rescued by GLP-1-RAs and NUAK-i; and 2) provide a precision medicine approach to treat each NAFLD stage with insights directly translatable to clinical trials.
Competitiondate
202209
Approvedterm2
5 yrs 0 mth
Pinamesdelim
Gaisano, Herbert Y; Yuen, Darren A
Approvedterm
5 ans 0 mois
Cihrcontribution2
~ $1,116,900~ $0~