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Jun 24, 2016

UNCW Chemists Work With Pharmaceutical Company To Help Develop Potential Medicines

Sponsored Content provided by Daniel G. Baden - Executive Principal, Marine Biotechnology in North Carolina (MARBIONC)

University researchers are finding new ways to collaborate with the pharmaceutical industry through a program meant to rapidly advance biomedical science. UNC Wilmington is now part of Eli Lilly’s unique Open Innovation Drug Discovery (OIDD) program, which streamlines the process of identifying potentially useful new substances.
Among the most exciting scientific work being done is discovering chemical compounds that affect biological processes, and ultimately might prove valuable in medicine. Here at UNCW, biologists and chemists on our faculty are finding hundreds of these substances in the marine organisms they study, as well as creating them “from scratch” in the lab. A major challenge, though, is determining which of them are “biologically active,” which means they might have possibilities as pharmaceuticals.
Lilly’s OIDD helps the process in many ways, starting with a computer algorithm that can evaluate hundreds or thousands of compounds based on data about their molecular structure.
Jeremy Morgan, Ph.D., is an organic chemist who works in the Department of Chemistry and Biochemistry on UNCW’s main campus. He and his colleagues choose research projects with an academic focus, with the primary goal of training students in laboratory skills. “But we often come up with new organic compounds that may be useful,” he explained. Organic, in this context, means “containing carbon” in their molecules, not necessarily produced by biological processes. But biochemists, many of them working in labs on our CREST Research Campus, are isolating many chemicals that do come from living organisms.
Regardless of the source – whether synthesized in laboratory glassware or naturally created by exotic marine algae – UNCW researchers have developed a “library” of literally hundreds of unique compounds, never identified anywhere else. An important objective, Morgan said, “is to determine if they have some unique biological effect.” A new molecule might just fit a receptor on the surface of a human cell, for example, or on a bacterium or other form of life. Or one of these unique compounds might interact with DNA in ways that could be useful in fighting certain cancers.
This is vitally important for medical research. Drug companies are always looking for compounds that will fit into particular receptors, and thus help control certain diseases.
Morgan, along with chemistry faculty members Sridhar Varadarajan and Tom Coombs, set out to create a database of these unique compounds so they could be evaluated for “bioactivity.” Steven Fontana on the Center for Marine Science staff at CREST Research Park took the lead in setting it up, working with a cross-departmental team including Ron Vetter, Ph.D., the dean of our graduate school. They hired an undergraduate chemistry major, Nicole Palmer, to do the actual work of coding the database. She used specialized software that creates graphic renderings of the structure of any molecule, and enters that structural data in a computer-readable format.
Meanwhile, Stephen Eitelman, Ph.D., business development consultant at MARBIONC, was seeking an avenue to get this library of compounds tested. The result: Our acceptance as a partner with Eli Lilly in the OIDD program.
“They have a well-designed system to submit compounds” for analysis, Morgan said. “We upload the structural information” and Lilly’s algorithm screens them for potential further study.
From a marketing perspective, one of OIDD’s virtues is that the testing is “blind,” preserving what might, some day, amount to valuable trade secrets. Unique compounds, and the chemical processes to produce them, can be patented, and UNCW has obtained some patents of this kind. So during this initial computerized review, Lilly’s own researchers don’t have any access to the data we submit about our unique compounds. The screening is all done with anonymous, bar-coded numbers. Only “if we get a hit,” as Morgan put it, if something looks promising for potential development, “do we get to the point of negotiating” with the drug company.
Options include selling a molecule outright, or entering into a range of licensing or partnership deals.
All that is in the future for us because our work with OIDD is fairly new. Even so, “We’ve submitted about 80 compounds that they’re interested in,” Morgan said, out of a total of around 500. That expression of interest leads to the next step, which is Lilly’s scientists actually working with the compounds in their laboratories. Often we’re able to send them samples that we have accumulated in our own labs. But sometimes we run out. That means, as in that old snack-food commercial, “We’ll make more.”
That’s where another aspect of OIDD comes into play. Lilly has a system by which it can synthesize a molecule based on detailed information about its structure. “I can draw a molecule we don’t have on hand,” Morgan explained, “and decide whether to synthesize it here, or let them make it themselves.” What Lilly calls an “automated synthesis laboratory” allows its partners to create compounds “remotely and securely.”
That step, of course, comes after we have reached agreement about how we’ll share that essential data – and possibly valuable intellectual property.
The substances we and other research institutions are submitting to OIDD are being evaluated for possible use in treating Alzheimer’s disease, diabetes, cardiovascular disorders, chronic pain, infectious diseases caused by both bacteria and viruses, neurological diseases and cancers. The program has a particular focus on so-called “neglected and tropical diseases.” In short: This work is connected to every important avenue of medical research.
After our first round of submissions about six months ago, “We have some data back,” Morgan said, based on those computerized assays. These have told us, for example, if a compound affects a particular receptor, or interacts with certain proteins, or affects a whole cell, which might mean it could kill a cancerous cell. Even if Lilly isn’t interested in a compound, and that’s true of a majority of what we submit, it still returns the assay data to us. Then our faculty and student researchers can use it for scholarly publications, applying for research grants, and other important academic purposes.
This relationship has proved to be highly fruitful already, and it’s still in its infancy. Morgan, Eitelman and Palmer have been cited for “Outstanding Continuous Contribution to Compound Screening” as a result of their work with OIDD.
“The idea that we could directly work with a well-known pharmaceutical company to develop a drug is pretty exciting,” Morgan commented.
UNCW CREST Research Park is a front-runner in marine biotech research and development. Researchers are exploring the potential of natural products derived from the sea to treat or cure human diseases and meet other important needs.
Discover why rising biotechnology and life sciences groups from all over the country are moving to UNCW CREST Research Park. UNCW CREST Research Park offers top-notch commercial laboratories available for lease at affordable rates, flexible terms, and innovative product development opportunities that are unmatched by any other park. Connect with CREST at [email protected] today.

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