Alex Makriyannis is the George Behrakis Chair of Pharmaceutical Biotechnology at Northeastern University, Boston, MA, and is the Founder and Director of the Center for Drug Discovery. He is a highly successful medicinal chemist and is well recognized nationally and internationally for his important contributions in endocannabinoid research. This relatively newly characterized biochemical system, where he played an important role in its discovery, regulates many physiological functions including pain, neuroprotection, addiction, immunomodulation and cognition. Over the past four decades, his laboratory has designed and synthesized some of the key pharmacological endocannabinoid probes that are widely used and serve as leads for the development of new medications. He has also made important contributions aimed at understanding the molecular basis of cannabinoid activity. He has been a creative pioneer in the field of chemical biology where he combined the use of medicinal chemistry, biochemistry, molecular biology and biophysics, his work is recognized for its high level of originality. Some of his compounds are in advanced preclinical trials for the treatment of metabolic disorders and liver function, neuropathic pain, addiction and neurodegenerative diseases.