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Grant: CIHR Fellowship

Université du Québec à Trois-Rivières

$135,000.00

Vectorization of New Anticancer Agents to Target Prostate Cancer Cells via their Conjugation to Testosterone: Design, Synthesis and Biological Evaluation

FY 2011-12

Summary
In Canada, prostate cancer is ranked first amongst the new cancer cases diagnosed and it is the third most common cancer exhibiting the highest mortality rate and therefore it is of major public health problem. In this context, new treatments are in constant demand to reduce the mortality and morbidity outcomes of that disease. To that end, the research team supervised by Drs. Bérubé and Asselin is developing a new therapeutical approach based on the use testosterone, a male hormone, to transport anticancer drugs selectively to prostate cancer cells. The antiandrogens (antitestosterone) are members of the anticancer drugs normally used in clinic to slow down the progression of prostate cancer at early stages. However, in advanced stages of the disease the tumours become resistant to the treatments resulting in untimely death. Adjuvant drugs can be added to the chemotherapy of prostate cancer, however, their effects are often of limited efficacy and duration. To date, Drs. Bérubé and Asselin have conducted studies using molecular models that show how and where to conjugate anticancer drugs to testosterone, which afterward can effectively target and kill hormone-dependent prostate cancer cells. The aim of our research program is to use new chemical methods to prepare new compounds designated as "testosterone-drug" and study their pharmacological properties on prostate cancer cells. Our project will focus on four main objectives involving: i) design of the new molecules using molecular modeling, ii) preparation and characterization of the new compounds, iii) study of their antiproliferative effects on prostate cancer cells versus normal cells, and finally iv) study of the molecular mechanisms involved in prostate cancer cell death. Our endeavour should lead to new medications both more effective and less toxic for patients suffering from prostate cancer.
Program
CIHR Fellowship
Location
Quebec, Canada
Recipient Type
Academia
Type
Grant
Source
CIHR Funding Decisions Database

As published

Id
242452
Name
Fortin Sébastien
Region
Québec
Country
Canada
Orgtype
Institution Paid; Research Institution
Instname2
Cancer Research
Theme2
Biomedical
Prcname2
Fellowships - Post-PhD
Projecttitle
Vectorization of New Anticancer Agents to Target Prostate Cancer Cells via their Conjugation to Testosterone: Design, Synthesis and Biological Evaluation
Programtype2
Fellowship Programs
Orgnameinp2
Université du Québec à Trois-Rivières
Cihramount2
$135,000
Cihrequipment2
$0
Programname2
CIHR Fellowship
Keyworddelim
Alkylating Agents; Antiandrogens; Anticancer Agents; Cancer Chemotherapy; Conjugation Testosterone-Drugs; Medicinal Chemistry; Molecular Cell Biology; Molecular Modeling; Molecular Pharmacology; Vectorization Cancer Therapy
Abstract
In Canada, prostate cancer is ranked first amongst the new cancer cases diagnosed and it is the third most common cancer exhibiting the highest mortality rate and therefore it is of major public health problem. In this context, new treatments are in constant demand to reduce the mortality and morbidity outcomes of that disease. To that end, the research team supervised by Drs. Bérubé and Asselin is developing a new therapeutical approach based on the use testosterone, a male hormone, to transport anticancer drugs selectively to prostate cancer cells. The antiandrogens (antitestosterone) are members of the anticancer drugs normally used in clinic to slow down the progression of prostate cancer at early stages. However, in advanced stages of the disease the tumours become resistant to the treatments resulting in untimely death. Adjuvant drugs can be added to the chemotherapy of prostate cancer, however, their effects are often of limited efficacy and duration. To date, Drs. Bérubé and Asselin have conducted studies using molecular models that show how and where to conjugate anticancer drugs to testosterone, which afterward can effectively target and kill hormone-dependent prostate cancer cells. The aim of our research program is to use new chemical methods to prepare new compounds designated as "testosterone-drug" and study their pharmacological properties on prostate cancer cells. Our project will focus on four main objectives involving: i) design of the new molecules using molecular modeling, ii) preparation and characterization of the new compounds, iii) study of their antiproliferative effects on prostate cancer cells versus normal cells, and finally iv) study of the molecular mechanisms involved in prostate cancer cell death. Our endeavour should lead to new medications both more effective and less toxic for patients suffering from prostate cancer.
Competitiondate
201110
Approvedterm2
3 yrs 0 mth
Pinamesdelim
Fortin, Sébastien
Approvedterm
3 ans 0 mois
Cihrcontribution2
~ $135,000~ $0~