Although there is significant improvement in managing asthma and chronic obstructive pulmonary disease (COPD) diseases, there is still a strong need in controlling symptoms to prevent hospitalizations or even death.
"Only about 50 percent of asthmatics, and an even lower percentage of people with COPD, achieve adequate control of lung inflammation and airway constriction with currently available medications," said Stephen Liggett, MD, vice dean for research at the University of South Florida Morsani College of Medicine and a USF Health professor of medicine, molecular pharmacology and physiology, and biomedical engineering. "So, we're clearly missing something from our drug armamentarium to help all these patients."
Now, research has found a way to target certain receptors with a promising bronchodilator.
"The two key questions we asked were: 'Is it possible to find a more potent agonist that activates this receptor?' and 'Is it feasible to deliver by inhalation given the potencies that we find?'" said Dr. Liggett, the paper's senior author. "T5-8 was the bronchodilator agonist that worked best. There were a few others that were very good as well, so we now have multiple potential new drugs to carry out the next steps."
Findings were in ACS Pharmacology and Translational Science.
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"The biggest challenge we faced was not having a 3-D crystal structure of TAS2R5, so we had no idea exactly how agonist T5-1 fit into this mysterious bitter taste receptor," Dr. Liggett said. "By merging our strength in receptors, pharmacology, physiology, and drug development, our team was able to make the breakthrough."
"Having two distinct classes of drugs that work in different ways to open the airways would be an important step to help patients optimally control their symptoms."
"This study yielded a drug discovery that successfully meets most of the criteria needed to advance the compound toward its first trial as a potential first-in-class bronchodilator targeting airway receptor TAS2R5."
Source: Science Daily
