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Pharmacy

Dr. Rafik Karaman: Anti-cancer Prodrugs-Three Decades of Design

Field of Research: Anti Cancer Drugs

Name of author) (s): Horani W., Thawabteh A., Scrano L., Bufo S.A., Mecca G., Karaman R.

Title of published work: “Anti-cancer Prodrugs-Three Decades of Design”

Name of Journal: World Journal of Pharmacy & Pharmaceutical Sciences

Year: 2015

Volume:  4 (7)

Pages: 1751-1779

Publisher: WJPPS

Abstract:

The conventional old treatment method for cancer therapy is associated with severe side effects along with several limitations. Therefore, searching and developing new methods for cancer became crucial. This mini review was devoted on the design and synthesis of prodrugs for cancer treatment. The methods discussed include targeted prodrugs which are depending on the presence of unique cellular conditions at the desired target, especially the availability of certain enzymes and transporters at these target sites, antibody directed enzyme prodrug therapy (ADEPT), gene-directed enzyme prodrug therapy (GDEPT) which is considered one of the important strategies for the treatment of cancer and prodrugs based on enzyme models that have been advocated to understand enzyme catalysis. In this approach, a design of prodrugs is accomplished using computational calculations based on molecular orbital and molecular mechanics methods. Correlations between experimental and calculated rate values for some intramolecular processes provided a tool to predict thermodynamic and kinetic parameters for intramolecular processes that can be utilized as prodrugs linkers. This approach does not require any enzyme to catalyze the prodrug interconversion. The interconversion rate is solely dependent on the factors govern the limiting step of the intramolecular process.

Keywords:

Prodrugs, Targeted prodrugs, ADEPT, GDEPT, Cancer, Intramolecular process, Enzyme models.

Contact author (s):

Name: Rafik Karaman, PhD.

Address: Al Quds University, Faculty of Pharmacy

E-mail: This email address is being protected from spambots. You need JavaScript enabled to view it.

 

 

 

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