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Medicinal Chemistry Group Dr. Severo Salvadori (center)
The Medicinal Chemistry Group at NIEHS has sought to collaborate with the most experienced scientists worldwide in order to maintain a high level of research at the forefront of scientific research. In terms of synthetic peptide chemistry, the names of Severo Salvadori and Okada Yoshio stand out as giants. Each has a decades-long background of innovative experience and leadership with committed interest in solving the complex picture of how subtle changes in opioid peptides trigger major alterations in their biological actions. Dr. Salvadori was instrumental in our introduction of Dmt into opioid peptide antagonists and agonist that opened the door for new discoveries in this area with Drs. Balboni and Guerrini. Equally, Drs. Okada and Tsuda, along with their dedicated students and technicians, provide an active research program on developing unique opioidmimetic compounds. In collaboration with these two remarkable groups and their colleagues, we have been able to provide the public health sector with potentially new formulations for drugs to treat pain, addictive diseases and other symptoms dealing with neural reward mechanisms.  Dr. Okada Yoshio
Yusuke Sasaki Akihiro Ambo, Tohoku Pharmaceutical University, Sendai, Japan, seek to delineate the bioactivity of opioid analogues in vitro using a variety of classical bioassay techniques. In collaboration with Istvan Tóth and Joanne Blanchfield, University of Queensland, Brisbane, Australia, we embark upon the development of other classes of opioidmimetics aimed at transversing membrane barriers. Tingyou Li, Jilin University, Changchun, Jilin, Republic of China, continues the tradition after postdoctoral studies with Prof. Okada. The interests of Eugenio Vazquez, University of Santiago, Spain, in fluorescent markers expands the applicability of opioids in research and PET scans. Lucia Negri, "Vittorio Erspamer," University La Sapienza, Rome, Italy, and her coworkers provide valuable insights on the functional bioactivity of a multitude of opioids. Several other groups in Europe and the U.S. collaborate with Prof. Salvadori, Drs. Balboni and Guerrini to further define the activity of many of our unusual analogues. In terms of the goals of the Medicinal Chemistry Group in relation to the Mission of the NIEHS, we enlisted the collaboration of Esa Korpi, Helsinki, Finland, and his associates known for their study on the root causes of alcoholism, in addition to H. Scott Swartzwelder, VA Medical Center and Duke University, on the neurophysiology of opioid inhibition of alcoholism. The direct application of our opioid analogues on animal models portends translation to human health. For example, alcoholism is one of the most common and preventable diseases worldwide in which naltrexone is currently used in a treatment regime, although only partially successful due to its side-effects. We hope to make available through patents our potential drugs for use in this important public health issue which affects an untold loss of human lives and billions of man-hours in annual productivity. |
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