Selected category: Drug Discovery

Several outbreaks of the Zika virus have been reported around the world since its discovery in 1947, but a commercially available treatment for the disease is still not available, and scientists continue to search for the best antiviral agent. Professor Martin Würtele and his colleagues in the Department of Science and Technology at the Federal University of São Paulo recently published a study identifying several natural substances that showed potent antiviral activity against the Zika virus protease.

Opioid addiction, alongside addiction to other substances, is a significant public health, social and economic challenge in the US. In 2017, the opioid epidemic was declared a public health emergency by the Department of Health and Human Services, with one of its aims to improve access to treatment and recovery services. Despite this, over 100,000 US lives were lost to opioid overdoses in the year to April 2021. Increasingly, outpatient centers such as Ideal Option are providing medication-assisted treatment (MAT) – combining approved medications with counseling and support therapy – to offer a ‘whole-patient’ approach to treatment of, and sustained recovery from, these addictions.

Mitosis plays an essential role in growth and cellular replacement, and is often dysregulated in cancers, making the process of therapeutic interest. Researchers at the University of North Carolina at Chapel Hill (UNC Chapel Hill) are developing novel cell imaging tools to help them classify key components of mitosis and identify new therapeutic targets.

The race has been on since the start of the pandemic to develop vaccines and drugs to fight against the SARS-CoV-2 virus. Vaccine development has proven successful, with vaccine roll-out underway in many countries, but the need remains to identify drugs that can treat the disease for those who have not been vaccinated, or for those where the vaccine is not effective enough to prevent disease. Researchers at the Fraunhofer Institute for Translational Medicine and Pharmacology (ITMP) in Hamburg, Germany, have been using high throughput drug approaches to screen compound libraries for candidate antiviral drugs.

Carbonic anhydrases (CAs) catalyze the reaction between water and carbon dioxide to regulate pH and fluid balance in vivo. Deviations in CA activity have been shown to correlate with bone, lung and liver diseases, as well as obesity, type II diabetes and even epilepsy. Professor Areej Abuhammad and her team at the University of Jordan are interested in developing novel therapies to counteract imbalances in CA activity, using protein crystallography to investigate a wide range of potential inhibitors.

Laboratory automation is increasingly common in life sciences research, helping to tackle some of the challenges that come with manual workflows, including inefficient operation, limited throughput and challenges of reproducibility. However, most automated platforms still require human operators to set up reagents, transfer plates between machines, and clean down afterwards. Dr Koichi Takahashi and his colleagues at the RIKEN Center for Biosystems Dynamics Research in Japan are developing a new type of laboratory automation workflow system that combines humanoid and other types of robots, creating a prototype for the lab of the future.

3D cell culture is an area of great interest in the drug development industry, as 3D models give a more accurate representation of how cells act in response to compounds in vivo. Merck’s Cellular Pharmacology Department specializes in the use of spheroid cell cultures to test various conditions and compounds of interest, and identify candidate drugs. Automation plays a vital role in this process, enabling high throughput screening of cell-based assays.

Recent viral outbreaks have alerted the world to the serious consequences of viral disease, yet the development of new antiviral drugs is challenging because of problems such as resistance or lack of molecular targets. Researchers at Zhejiang University’s College of Pharmaceutical Sciences are seeking to identify new antiviral drugs by combining insights from traditional Chinese medicine with modern high throughput technologies to discover novel lead compounds.

Damage to the brain or spinal cord can be life changing for affected individuals, and it was historically thought that these injuries would not heal and could not be repaired. However, since the discovery of neurite growth inhibitors by Professor Martin E. Schwab at the University of Zurich, clinical researchers have been exploring new therapeutic approaches to treat cerebral stroke and spinal cord injury. The Wyss Zurich/University of Zurich CeNeReg project and NovaGo Therapeutics Inc. – co-founded by Professor Schwab – are at the forefront of this exciting field, and are dedicated to the development of human antibody therapeutics to stimulate nerve repair and regeneration.

Drug discovery is a lengthy and expensive process, particularly in the early candidate identification stages, where screening of large numbers of compounds is required. Researchers at the University of Central Florida are using artificial intelligence (AI) to aid candidate selection for antimalarial drugs, making this selection process more efficient and cost effective, as well as increasing the likelihood of success.

The VirPath laboratory is focused on the study of influenza and other respiratory viruses to identify new antiviral molecules and develop innovative vaccines. Digital dispensing and luminescence-based assays play an important role in the evaluation of viral growth in different experimental models.

Detecting adverse off-target effects is crucial to ensure the safety of potential therapeutics, but limited throughput and ethical considerations have traditionally forced pharmaceutical companies to perform safety pharmacology studies at a late stage of the drug development process. Human stem cell-based cellular models and automated screening processes are revolutionizing drug safety studies, enabling much earlier testing, with companies such as Ncardia at the forefront of this workflow transformation.

Small molecule drug discovery involves a range of functional assays that have traditionally relied on manual cell counting techniques to monitor proliferation, migration and invasion. Automated cell counting is enabling the EB House Austria to save time and free up personnel, as well as designing time-course experiments that were previously unachievable.

The successful treatment of inflammatory diseases may lie with controlling the production of particular proteins, driving efforts to identify translational repressors for drug targeting. Scientists at the Moulder Center for Drug Discovery Research have developed luminescencebased biosensors for protein detection, supporting multiplex studies and timecourse assays for identifying and characterizing novel compounds.

Developing therapies to treat rare diseases is often hindered by the limited availability of primary patient samples. Without these precious samples, it is difficult to understand the fundamental biology of these conditions or screen compound libraries for drug candidates. A group at the University of Parma is using a ‘chemogenomics’ approach to overcome this challenge, working on a nanoliter scale to identify new treatments for aggressive pediatric leukemias.

The HP D300 Digital Dispenser is enabling researchers at the Columbia Genome Center’s High-Throughput Screening Facility to quickly and simply create dose-response curves for combinations of up to nine compounds, allowing rapid generation of EC 50 data for faster experimental progress.

Automation brings more than simply speed to the laboratory. Modern software is taking the headache out of serial dilution and normalization calculations, supporting assay development and delivering reliable results for international healthcare company Merck.

Chinese medicine combines herbal remedies with acupuncture, massage, exercise and diet to provide alternative therapies for a wide range of conditions. Despite drawing on over 2,500 years of traditional knowledge, little is known about the mode of action of these herbal medicines. Researchers at Zhejiang University’s College of Pharmaceutical Sciences are looking to address this, using modern laboratory techniques to identify the numerous active pharmaceutical ingredients and synergistic effects that contribute to their efficacy.

Biomolecular interaction analysis plays an important role in the pharmaceutical industry. SensiQ Technologies has optimized surface plasmon resonance technology for drug discovery applications, developing an automated system that can provide rapid affinity data for prompt identification of candidate fragment activities.

Dart NeuroScience specializes in the development of novel therapeutics targeting neurological disorders, with an emphasis on impairment of cognitive functions such as memory.