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Mysterious Bitter Receptor, Hope for the Treatment of Asthma

2021-01-07
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Although scientists have made progress in controlling asthma and chronic obstructive pulmonary disease (COPD), improper control of the symptoms of both respiratory diseases can lead to severe shortness of breath, hospitalization and even death. Dr. Stephen Liggert, associate dean of research at the University of South Florida, Mossani, said that only about 50% of asthma patients and a lower proportion of COPD patients can adequately control lung inflammation and airway contraction with currently available drugs. But just recently, Dr. Ligit’s laboratory discovered that several subtypes of bitter taste receptors (TAS2Rs)-G protein-coupled receptors are expressed on human smooth muscle airway muscle cells deep in the lung.

Mysterious bitter taste receptor, hope for the treatment of asthma

In asthma and chronic obstructive pulmonary disease, tightening the smooth muscles around the bronchi shrinks the airway and reduces airflow. Dr. Ligit’s laboratory found that these taste receptors open the airway when activated. Now they are looking for new drugs to open airway constriction by targeting smooth muscle TAS2Rs to treat asthma and other obstructive lung diseases.

COPD
Dr. Stephen Liggett

Dr. Liggett and colleagues have identified 18 new compounds that activate the bitter receptor TAS2R5 subtype to promote the expansion of human airway smooth muscle cells. The interdisciplinary research team found that 1,10 phenanthroline 5,6-dione (T5-8 for short) is the most promising of several lead compounds (drug candidates). The efficacy of T5-8 is 1000 times that of other tested compounds, and it has significant effectiveness in human airway smooth muscle cells grown in the laboratory.
Researchers have developed screening techniques to determine the potency and effectiveness of 18 compounds. A biochemical test evaluated the extent to which these new agonists activate TAS2R5 in airway smooth muscle cells isolated from the lungs of non-asthmatic human donors. Then, the researchers used the technique of magnetic twist cytometry to verify the effect on airway smooth muscle relaxation.
Dr. Ligit said that the biggest challenge now is that there is no 3-D crystal structure of TAS2R5, so I don’t know how the agonist T5-1 fits this mysterious bitter receptor. By combining strengths in receptors, pharmacology, physiology, and drug development, Dr. Lijit’s team said they could make breakthroughs.
T5-8 is superior to all other selected bronchodilator agonists, exhibiting a maximum relaxation response (50%) that is significantly greater than that of salbutamol (27%). Albuterol belongs to the only class of direct bronchodilators (beta-2 agonists) that can be used to treat wheezing and shortness of breath caused by asthma and COPD. However, this drug and its derivatives are usually used in emergency inhalers and are not suitable for all patients. Overuse has led to an increase in hospitalization rates. This shows that having two different types of drugs to open the airways in different ways will be an important step in helping patients to optimally control their symptoms.
Inhalation preparations are unique in terms of technology development and review and approval. It is necessary to comprehensively consider the product’s prescription technology, quality control, drug delivery device, industrial production, and clinical application. Medicilon is familiar with the development process of various inhalation preparations, especially in the field of inhalation powder inhalation (DPI), atomized inhalation and nasal spray (Nasal Spray) preparations. It has very rich research and development experience and is equipped with professional equipment, such as COPLEY’s new generation of medicinal impactor (NGI), COPLEY’s BRS2100 breathing simulator, Germany’s Sinpatec laser particle size analyzer, etc., can meet the quality research and in vitro evaluation of various inhalation preparations. Medicilon has a complete preclinical research platform for inhaled drug delivery, including pharmacokinetic tests and efficacy tests of inhaled drugs; at the same time, it can complete the safety evaluation of a complete set of drugs, such as tissue distribution test, acute toxicity test, repeated administration toxicity test , Irritation test, allergy test and safety pharmacology test, etc. Medicilon will continue to pay attention to the progress of this research, hoping to help the research and development of inhaled drugs.
About Medicilon

Medicilon (stock code: 688202) was established in 2004 and is headquartered in Shanghai. It is committed to providing a full range of preclinical new drug research services for global pharmaceutical companies, research institutions and scientific researchers. Medicilon’s one-stop integrated service helps customers accelerate the development of new drugs with strong project management and more efficient and cost-effective R&D services. The services cover the entire process of preclinical new drug research in medicine, including drug discovery, pharmaceutical research and clinical trials. Pre-research. Medicilon grows together with high-quality customers at home and abroad, and provides new drug research and development services to more than 700 customers around the world. Medicilon will continue to base itself on a global perspective, gather Chinese innovation, and contribute to human health!

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