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Metals in Medicine: Targets, Diagnostics, and Therapeutics
June 28-29, 2000
Introduction
Factors Motivating Organization of the Meeting
Meeting Objectives
Meeting Organization, Advertising, and Participation
Executive Summary
Metalloenzymes as Targets
Metallopharmaceutical Diagnostics and Radiotherapeutics
Metal Metabolism as a Research Target
Medicinal Inorganic Chemistry
Opportunities
Challenges
General Comments and Recommendations
Detailed Meeting Report
Session 1: Molecular and Cellular Targets of Metal Action
Day 1 Morning Session Discussion
Session 2: Metal-Containing Targets of Drug Action
Session 3: Radiology, Imaging, and Photodynamic Therapy
Day 1 Afternoon Discussion
Session 4: Metal Metabolism
Day 2 Morning Discussion
Session 5: Metallotherapeutics and Disease
Day 2 Afternoon Discussion and Overall Meeting Discussion
Introduction
A meeting, entitled, "Metals in Medicine: Targets, Diagnostics, and Therapeutics", was
held June 28-29, 2000, in the Natcher Conference Center on the NIH campus, in
Bethesda, Maryland. This meeting, sponsored by the National Institute of General
Medical Sciences (NIGMS), the National Cancer Institute (NCI), the National Institute of
Allergy and Infectious Diseases (NIAID), the National Institute of Diabetes and
Digestive and Kidney Diseases (NIDDK), the National Institute of Environmental Health
Sciences (NIEHS), the Center for Scientific Review (CSR), and the NIH Office of
Dietary Supplements generated substantial interest in the scientific community. In
addition to the 25 invited speakers, another 53 people volunteered abstracts for poster
presentations. A total of 352 people registered for the meeting. Actual attendance on-site
was 235. An unknown number viewed the meeting on the Internet or NIH local area
network via the videocast.nih.gov Web site. The broadcast will remain available on that
site for the indefinite future. The meeting Program Booklet, List of Registrants, and this
report have been posted on the NIGMS Metals in Medicine Web page:
http://www.nigms.nih.gov/news/meetings/metals.html.
Factors Motivating Organization of the Meeting

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NIGMS and other NIH components provide significant support for research in
bioinorganic chemistry and metallobiochemistry. Most currently supported research
is focused on metalloprotein structure/function studies and metalloproteins are clearly
important targets for drug development.
Discussions with leaders in the scientific community suggested additional areas of
emerging scientific opportunity (e.g., roles of metals in cellular regulation,
mechanisms of metal trafficking, opportunities to modulate normal and aberrant
metal metabolism).
Discussions also raised the question of why so few inorganic drugs are on the market
and whether this relates to insurmountable obstacles in development of such agents or
limited participation of inorganic chemists in the pharmaceutical industry.
Advances in synthesis and control of inorganic complex reactivity and in
understanding the reactions of metals in vivo, plus the successful development of
metallopharmaceuticals in several diagnostic and therapeutic areas, suggest that
additional research opportunities might exist in this area.
Meeting Objectives
Three general topics were explored:
Current utilization of bioinorganic chemistry and metallobiochemistry basic research
discoveries in the pharmaceutical industry. What is the role of metalloenzyme
structure/function insights in drug discovery and development? What is the role of
inorganic compounds as leads in drug discovery? What is the industry experience?
What is the industry attitude?
Obstacles and opportunities for the development of additional
metallopharmaceuticals. What progress has been made in selectivity? What do we
know about metal toxicity? Is this an insurmountable obstacle or a matter of bad
publicity? What has been learned from the successful development of radiotherapy
and imaging agents? What promising results have been obtained in specific disease
areas? What are the issues surrounding metals as dietary supplements? What types
of research are needed to exploit the unique properties of metals for potential
pharmaceutical benefit?
Opportunities for the development of agents that target metal metabolism and metal-
regulated cellular processes. What new cellular processes are being discovered?
What potential do they have for drug development? What are the roles of essential
elements in the body? What are the causes of metal toxicity? What successes have
been achieved for correcting aberrant metal metabolism and toxic metal exposures?
Meeting Organization, Advertising, and Participation

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Metals in Medicine: Targets, Diagnostics, and Therapeutics June 28-29, 2000 • • • • • • Introduction • Factors Motivating Organization of the Meeting • Meeting Objectives • Meeting Organization, Advertising, and Participation Executive Summary • Metalloenzymes as Targets • Metallopharmaceutical Diagnostics and Radiotherapeutics • Metal Metabolism as a Research Target • Medicinal Inorganic Chemistry Opportunities Challenges General Comments and Recommendations Detailed Meeting Report • Session 1: Molecular and Cellular Targets of Metal Action • Day 1 Morning Session Discussion • Session 2: Metal-Containing Targets of Drug Action • Session 3: Radiology, Imaging, and Photodynamic Therapy • Day 1 Afternoon Discussion • Session 4: Metal Metabolism • Day 2 Morning Discussion • Session 5: Metallotherapeutics and Disease • Day 2 Afternoon Discussion and Overall Meeting Discussion Introduction A meeting, entitled, "Metals in Medicine: Targets, Diagnostics, and Therapeutics", was held June 28-29, 2000, in the Natcher Conference Center on the NIH campus, in Bethesda, Maryland. This meeting, sponsored by the National Institute of General Medical Sciences (NIGMS), the National Cancer Institute (NCI), the National Institute of Allergy and Infectious Diseases (NIAID), the National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK), the National Institute of Environmental Health Sciences (NIEHS), the Center for Scientific Review (C ...
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