After four years of research, Pharmacology Prof. Fraydoon Rastinejad has made a significant breakthrough in his research on nuclear receptors, the University Health System announced Monday. Rastinejad said his discovery “will help pave the way to discovering better drugs that are much more specific and have fewer undesired side affects.”
The subject of Rastinejad’s research is a nuclear hormone receptor called peroxisome proliferator-activated receptor, which plays an important role in the treatment of type two diabetes, among other diseases, Rastinejad explained.
Rastinejad described the receptor as a lock that needs a specifically shaped key to successfully treat diseases. His research intends to help develop drugs that are effective “keys” for their respective diseases. He noted that 201 laboratories worldwide also have been working on the same problem.
“What we’ve done is we’ve made an atom-by-atom description of the three-dimensional structure of this receptor,” Rastinejad said, noting this development will better enable researchers to observe how drugs bind to the receptor and to design medicines that combine more effectively with the receptor. These more-targeted drugs will then provide better treatment for patients.
Assoc. Pharmacology Prof. Ira Schulman said Rastinejad’s research is critical to the understanding not only of PPAR but also of an entire family of related receptors. Shulman emphasized that “the nuclear hormone receptor family is a very important class of drug targets.”
This family “includes the PPAR [which is a] drug target for diabetes, the estrogen receptor for breast cancer and the glucocorticoide receptor,” which is important in the study of most anti-inflammatory drugs, Shulman noted.
To create the 3-D visualization of the receptor, Rastinejad used X-ray crystallography, “which requires that we purify these receptors and grow crystals of these receptors with the drug,” Rastinejad explained, adding that researchers then shoot these crystals with an X-ray beam to create a picture of the receptor.
Pharmacology Prof. Jim Garrison, a former department chair, said Rastinejad’s achievement “compares very well to a lot of major discoveries that change how people think about things — that happens relatively infrequently.”
Shulman, meanwhile, compared Rastinejad’s achievement to the first time the mile was run in under 4 minutes.
“People thought it would never be done,” Shulman said. “Now that barrier has been broken.”
Looking forward, Garrison said the next step of product development resulting from this research is a long way off but emphasized the research’s global implications.
“It’s a piece of information that becomes a template for what people can do all over the world,” he said. As to where its next step will first take root, he noted, “it’s hard to know where it will happen first.”
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