Drug Design & Development

Permanent URI for this collection

http://dspace.alquds.edu:4000/handle/20.500.12213/4755

Overview

The aim of this group is to investigate issues related to acces to health care services. Issue of human rights in health, financial socio-cultural barriers to care, stiga and health care access, quality of life, health coverage and access.

Our Team

    • Rafik Karaman

    Ph.D

    • Jehad Abbadi

    Ph.D.

    Mohannad Qurei

    Ph.D

    Mustafa Khamis

    Ph.D

    Browse

    Browsing Drug Design & Development by Subject "Enzyme models"

    Now showing 1 - 2 of 2
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      Anti-cancer Prodrugs-Three Decades of Design
      (2015-07-31) Horani, Waad; Thawabteh, Ameen; Scrano, Laura; A. Bufo, Sabino; Mecca, Gennaro; Karaman, Rafik
      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.
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      Prodrugs targeting the central nervous system (cns)
      (2015-08-07) Salameh, Falasteen; Karaman, Donia; Karaman, Rafik
      The classical approach for delivery of drugs into the central nervous system (CNS) is associated with adverse effects and it has many limitations. Therefore, extensive efforts have been done in searching and developing novel methods for achieving such delivery. This minireview discusses the design and synthesis of selected targeting prodrugs for the treatment of conditions related to impairment in the CNS such as Parkinson‘s and Alzheimer‘s diseases. Such approaches include targeting prodrugs which are designed to interact with unique cellular conditions at the target site, especially the availability of certain enzymes and transporters at these sites. In addition, part of this mini-review is devoted to prodrugs design based on enzyme models that have been invoked to understand how enzymes catalyzebiotransformation. In this approach, the prodrugs design isdone using quantum molecular orbital and molecular mechanics methods. The equations obtained from correlations of experimental and calculated rate values for some intramolecular processes are used to predict parameters for other intramolecular processes that can be utilized as prodrugs linkers. In this approach, there is no need for enzymes to catalyze the conversion of the prodrug to its active parent drug and the conversion rate of the prodrug is dependent only on those factors playing dominant role in the rate-limiting step of the process.