last updated 20-11-2024

Rational drug design

Rational drug design

Development of new antitumor drugs is one of the main items in cancer research. Molecular biology helps to understand more of tumor cells and creates new possibilities for rational drug design. The main problem still is that a tumor cell is not really distinguishable from a normal cell, except for the fact, that an abnormal protein is produced and that the cell grows and divides rapidly. And indeed those aspects are important for drug development. In the graphic various theoretically possible sites of intervention in the tumor cell cycle are shown:

 

  • blockade at receptor level

    (a normally present receptor can be blocked for the extensively present growth factors or an abnormal receptor produced by the tumor cell can be blocked)

  • blockade of the signal transduction

    (in this way the signal is not transduced towards the nucleus)

  • blockade at the level of transcription factors binding to DNA

    (a tumor cell might express a modified transcription factor)

  • blockade at the transcription and/or translation level

    (this method is not very specific; it will block all transcription and translation)

  • blockade of the release of abnormal proteins

    (this method could be useful in case the abnormal proteins are growth factors)

In general, the concept for rational drug intervention requires high specificity for the tumor cell.

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