In this review, we would like to introduce the term molecular biomarkers as a broad term to refer to all biomarkers that are measurable by methods based on the biomarker's molecular properties. This definition would comprise a wide range of biomarkers from small to large molecules, from nucleic acids to proteins. We present an overview of the different classifications and uses of biomarkers, especially in the context of drug development. We also offer a summary of the different platforms being employed in the search for novel molecular biomarkers such as genomics, proteomics, and other “-omics” technologies. A case study on the application of biomarkers in the development of new drugs for the treatment of diabetes is also presented. This includes an overview of the development of a specific biomarker, adiponectin, from its discovery using genomics methods and its subsequent re-identification using differential mass spectroscopy. An evolution of methods for the detection of adiponectin from a Western blot, to an ELISA, to an antibody-free mass spectrometry method is also illustrated.
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