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Metals are both targets and tools for chemotherapeutic intervention. Metals in Medicine is a dynamic interdisciplinary research field whose major goals are to contribute to an understanding of the role of endogenous and exogenous metals in disease, and to exploit this knowledge for managing or curing fatal illnesses. In 2000, the National Institute of General Medical Sciences (NIGMS) of the National Institutes of Health held a meeting entitled “Metals in Medicine: Targets, Diagnostics, and Therapeutics” (http: / / www.nigms.nih.gov / news / meetings / metals.html) to explore obstacles and opportunities in metalbased and metal-targeted drug development and to foster collaborations between academia and pharmaceutical industry. More recently, the first Gordon Research Conference on “Metals in Medicine“ was organized by N. Farrell, M. J. Clarke, and C. F. Shaw (New London, NH, 2002), another important milestone in promoting this exciting research area. This issue of Current Topics in Medicinal Chemistry was inspired by these events and attempts to be a representative collection of recent advancements in the field. The eight contributions deal with the development of metal-containing pharmaceuticals for the therapy of life-threatening diseases, such as cancer and HIV / AIDS, and new strategies for targeting metalloproteins and metal pools. I thank the authors for their excellent contributions and their patience throughout this project and hope that this special issue will stimulate new developments within a growing community of researchers interested in the various aspects of metals in biology and disease.