Category Archives: Drug Discovery

Why has cancer drug discovery changed so much?

Cancer drug discovery has undergone a remarkable series of changes over the last 15 years. So what has changed so much?

First, the molecular targets of contemporary cancer drug discovery projects are very different. Current targets reflect our increasing understanding of the genetic and epigenetic changes that are responsible for the initiation and malignant progression of cancer through the dysregulation of cell biochemistry and signaling networks.

Second, the integrated application of a range of powerful drug discovery technologies has had

a major impact .

Third, many new treatments have emerged over the last 15 years based on this paradigm that are firmly established in the clinic. The present volume brings together many of the important aspects of the discovery and design of new cancer drugs, emphasizing small molecules.

Integrated small-molecule drug discovery and development

The successful discovery and development of small-molecule cancer drugs are highly dependent upon the creative interplay between many disciplines: these include genetics, genomics, and bioinformatics; cell and molecular biology; structural biology; tumor biology; pharmacology; pharmacokinetics and metabolism; medicinal chemistry; and experimental medicine. The application of a wide range of powerful technologies has had a major impact.


New molecular targets: the druggable cancer genome and epigenome

The selection of the best possible molecular targets is clearly crucial to the success of a drug discovery and development project. A number of factors influence the choice of target, including, in particular, (1) the involvement of the target in the initiation and progression of cancer, and (2) the technical feasibility or “druggability” of the target. With the mapping of the human genome sequence, the concept of the “druggable genome” has become popular and useful.



Modern Cancer Drug Discovery: Integrating Targets, Technologies, and Treatments for Personalized Medicine. Cancer Drug Design and Discovery (Second Edition). 2014; 3-53.