The Stony Brook University scientists tied to the Institute of Chemical Biology and Drug Discovery (ICB & DD) discovered that Fatty Acid Binding Proteins (FABPs) are pharmacological targets of the body’s endocannabinoid system licensed to Artelo Biosciences, Inc. Fatty Acid Binding Proteins (FABPs) were identified as potential pharmacological targets for the treatment of cancer, inflammation, and pain six years ago, thanks to a promising technology licensed. The Food and Drug Administration has approved these first compounds for use in human clinical studies.
Artelo is investigating the unique properties of endocannabinoids, which efficiently block pain but are not associated with addiction. The discovery that FABPs are endocannabinoid transporters marked the start of the study in 2009. Using computational biology for both virtual screening and real tests, lead compounds that bind to FABPs and work as analgesics for a range of pain kinds were found. Three new chemical compounds, known as Stony Brook FABP Inhibitors or SB-FIs, were discovered by the AEA research and are covered by patents at Stony Brook University. Artelo will look into these compounds as part of its medication development plan. This licensing arrangement opens up new business opportunities for Artelo and is in line with the company’s strategic aim.
What are Endocannabinoids?
The body naturally produces compounds called endocannabinoids, which resemble marijuana and may serve as the foundation for novel therapeutics for the treatment of pain, inflammation, and cancer.
Cannabinoid-based therapies: A new horizon
The endocannabinoid anadamide (AEA), a neurotransmitter produced in the brain that binds to THC receptors, has been found to be transported within cells by fatty acid-binding proteins. Studies on animals have shown that increased endocannabinoids can have positive pharmacological effects on stress, pain, and inflammation. They can also lessen the side effects of stopping a medicine. AEA is elevated through the inhibition of FABP transporters. Elevated amounts of AEA would result from potential medications working in this way. Similar to modern antidepressants, which block serotonin transport, these medications would work by inhibiting the same mechanism.
More About Ongoing Cannabinoid Research
Artelo made an announcement stating that the FDA’s initial approval of ART26.12, an FABP5 (5 denotes a specific protein) selective chemical, allows the business to begin the drug’s first phase 1 single ascending dose study in humans. According to the company, ART26.12 will cure chemotherapy-induced peripheral neuropathy, hence meeting a vital demand for cancer patients. It is anticipated that phase 1 clinical trials will begin in other countries in the first half of 2025.
The first drug in the class of FABP5 inhibitors being developed is ART26.12. An exclusive license to use all FABP inhibitors’ intellectual property for endocannabinoid system regulation was granted to Artelo in 2018.
In cooperation with the Institute of Chemical Biology and Drug Discovery, Iwao Ojima, a distinguished professor of chemistry at Stony Brook University, Martin Kaczocha, an associate professor of anesthesiology, and Dale Deutsch, an emeritus professor of biochemistry and cell biology, started the research on FABPs. The endocannabinoid anandamide (AEA), a neurotransmitter produced in the brain that interacts with cannabinoid receptors, has been discovered as a potential pharmacological target for the intracellular transporter FABP5. Increased endocannabinoids can lessen the effects of drug withdrawal and help with stress, pain, and inflammation. The research team showed that blocking FABP transporters increases AEA levels, which lays the groundwork for developing drugs to do the same.
Members of the FABP Stony Brook research group needed to be experts in a variety of fields, including biochemistry, chemistry, computational biology, computer science, X-ray crystallography, and medicine, in order to create innovative FABP inhibitors. Deutsch, Martin Kaczocha from the Dept. of Anesthesiology, Robert Rizzo from the Dept. of Applied Mathematics and Statistics, Huilin Li, who was previously employed by the Department of Biochemistry and Cell Biology, and Distinguished Professor Iwao Ojima, who is also the Director of the ICB & DD, are the members of the team. The Stony Brook team and Artelo’s team worked together to create compounds with high FABP5 potency and selectivity. As a result, the first medication in a prospective pipeline of pain and inflammatory treatments—ART26.12—began to be commercialized. Ojima and Kaczocha analyzed compound candidates under a contract with Artelo, which led to the development of the main candidate, SB-FI-1621, also known as ART26.12.
Conclusion
Sean Boykevisch, head of Intellectual Property Partners at Stony Brook’s Technology Transfer Office, called the discovery of this first clinical-stage medication that targets the FABP pathway “an important and exciting milestone.” “A real bench-to-bedside programme with the aim of better patient experiences and outcomes was produced by the Stony Brook team’s basic and translational research and their subsequent collaboration with Artelo.”
Gregory D. Gorgas, president and CEO of Artelo Biosciences, stated, “We look forward to sharing the initial clinical results with ART26.12 next year.” Being the pioneer in FABP inhibition research, researchers are dedicated to expanding on the distinctive lipid-modulating mechanism of the FABP inhibitor platform to treat disorders that have few, if any, safe and effective pharmacological treatments.
Story Source: Reference Article 1 | Reference Article 2
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Deotima is a consulting scientific content writing intern at CBIRT. Currently she's pursuing Master's in Bioinformatics at Maulana Abul Kalam Azad University of Technology. As an emerging scientific writer, she is eager to apply her expertise in making intricate scientific concepts comprehensible to individuals from diverse backgrounds. Deotima harbors a particular passion for Structural Bioinformatics and Molecular Dynamics.
