Grant: Project Grant
Université de Sherbrooke
$696,150.00
High affinity inhibitors of PACE4 with therapeutic implications for prostate cancer
FY 2018-19
Summary
Prostate cancer is the most important cancer in men. Recurrence is a major problem that kills over 4000 Canadian men per year. While anti-androgen therapies extend life, prostate cancer cells adapt and become resistant. Novel, non-androgen targeted therapies are urgently needed. In this context we discovered that PACE4 play an important role in prostate cancer progression in an androgen-independent manner. Then we developed compound C23, a PACE4 inhibitor, that significantly reduces tumor progression in animal models that harbor human prostate cancer tumors. Our objective is to bring this compound to clinical trials. However, several steps need to be taken first. First and foremost, we must modify this compound into a form that has the best chance of being clinically relevant, in regards to its delivery and patient usage. To do this we will combine medicinal chemistry and targeting strategies with testing in prostate cancer animal models. Additionally, we will devise a precision medicine approach to select the patients that can benefit the most from C23 therapy. We will explore if existing drug therapies can be combined with C23, to develop the most effective treatment possible. A better understanding of these parameters will maximize a therapeutic response that can be better transferred into a clinic setting.
Department
Program
Project Grant
Recipient
Location
Quebec, Canada
Recipient Type
Academia
Type
Grant
Source
CIHR Funding Decisions Database
As published
Id
401636
Name
Day Robert
Region
Québec
Country
Canada
Orgtype
Institution Paid; Research Institution
Instname2
Cancer Research
Theme2
Biomedical
Prcname2
Pharmaceutical Sciences
Projecttitle
High affinity inhibitors of PACE4 with therapeutic implications for prostate cancer
Programtype2
Operating Grants
Orgnameinp2
Université de Sherbrooke
Cihramount2
$696,150
Cihrequipment2
$0
Programname2
Project Grant
Keyworddelim
C23; Cancer Animal Models; Drug Delivery; Enzyme Inhibitor; Imaging; Medicinal Chemistry; Pace4; Prodrugs; Structure Activity; Theranostics
Abstract
Prostate cancer is the most important cancer in men. Recurrence is a major problem that kills over 4000 Canadian men per year. While anti-androgen therapies extend life, prostate cancer cells adapt and become resistant. Novel, non-androgen targeted therapies are urgently needed. In this context we discovered that PACE4 play an important role in prostate cancer progression in an androgen-independent manner. Then we developed compound C23, a PACE4 inhibitor, that significantly reduces tumor progression in animal models that harbor human prostate cancer tumors. Our objective is to bring this compound to clinical trials. However, several steps need to be taken first. First and foremost, we must modify this compound into a form that has the best chance of being clinically relevant, in regards to its delivery and patient usage. To do this we will combine medicinal chemistry and targeting strategies with testing in prostate cancer animal models. Additionally, we will devise a precision medicine approach to select the patients that can benefit the most from C23 therapy. We will explore if existing drug therapies can be combined with C23, to develop the most effective treatment possible. A better understanding of these parameters will maximize a therapeutic response that can be better transferred into a clinic setting.
Competitiondate
201903
Approvedterm2
5 yrs 0 mth
Pinamesdelim
Day, Robert
Approvedterm
5 ans 0 mois
Cihrcontribution2
~ $696,150~ $0~