High Throughput Screening Assays for Drug Discovery
Drug discovery is a highly complex and multidisciplinary process with many branches and possibilities, which typically start with the identification of suitable drug targets. Such targets are biomolecules, most of which are proteins, such as receptors, enzymes or ion channels. In the process of validating a target, it is necessary to determine the relevance of the target to the disease under study and that the adjustment of the target can lead to effective treatment. The initial steps for target validation are usually performed in vitro and in animal models, and the final validation can only be performed in human clinical trials.
Modulators acting on targets can be agonists or antagonists in the case of receptors, activators or inhibitors of enzymes, and openers or blockers of ion channels. Active compounds that demonstrate dose-dependent target modulation are called lead compounds. The phase of lead compound identification starts with the design and development of suitable assay to monitor the target under study. In general, lead compounds continue to be optimized for their efficacy and selectivity, as well as their physicochemical properties, and their pharmacokinetics and safety are evaluated before they become candidates. The late phase of the drug discovery process are human clinical trials.
The Process of Drug Research and Development
High-Throughput Screening (HTS)
High-Throughput Screening (HTS) is a standard method for drug discovery in the pharmaceutical industry and has been widely used in the past decades. HTS is basically a process of screening a large number of active modulators against selected and specific targets. The drug discovery potential of HTS is enormous, when coupled to different types of libraries, including combinatorial chemistry, genomics, protein, and peptide libraries. The screening attrition rate in drug discovery protocols suggests that one marketable drug emerges from approximately one million screened compounds. The primary goal of the HTS assay is to accelerate drug discovery by screening large compound libraries to reduce the costs of drug development.
Product Range
Amerigo Scientific offers high throughput screening (HTS) assays for validated drug targets. The assays are in 96-well or 384-well plate format for tests of inhibition or IC50 measurement of compounds against the specific drug target proteins and enzymes. The validated drug targets include human proteins for anti-cancer and proteins from bacterial, viral and bacterial phage for anti-infection.
HTS Assays for Anticancer Drug Targets
Cancer is one of the biggest threats to human life in the world. The development of novel anticancer drugs is critical for patients with cancer who have no drugs to treat, as well as for reducing the financial burden on patients and prolonging their lives. According to the mechanism of action, anticancer drugs can be divided into angiogenesis inhibitors, DNA intercalators, DNA synthesis inhibitors, transcription regulators, enzyme inhibitors, etc. In clinical use, some of the anticancer agents that target DNA are often used in combination with drugs with other mechanisms of action to improve the survival rate of cancer patients.
Amerigo Scientific offers HTS assays kits for screening potential anticancer compounds that act the following validated targets:
HTS Assays for Antiviral Drug Targets
Viruses are submicroscopic infectious agents with either DNA or RNA as the genetic material and cause a variety of diseases in humans, animals, and plants. A virus must infect a host cell to replicate itself using the components of the host cell and then new viruses are release from the host cell. Virus infection process includes six steps, namely virus attachment, invasion, uncoating, replication, assembly, and release.
Antiviral drugs are one class of medication specifically used to treat viral infections by inhibiting the development of target pathogens rather than destroying them. With emerging new viruses in the current situation, it is increasingly important to develop drugs to treat or prevent them. Antiviral drugs generally target specific regions of the virus and specific phases of the virus life cycle. The modern antiviral drug design aims at identifying viral proteins or their parts. The antivirus targets should not resemble any human proteins to reduce any side-effects and should be common among many strains of viruses.
Amerigo Scientific offers HTS assays kits for screening potential antiviral compounds that act on specific virus proteins or enzymes:
HTS Assays for Antibacterial Drug Targets
Antibacterial drugs are known to either block key biochemical pathways or to interfere with cellular structures, leading to either growth inhibition or bacterial death. Cellular processes interfered by the widely used antibiotics can be grouped into six target categories: bacterial cell wall biosynthesis, bacterial cell membranes, bacterial protein biosynthesis, DNA replication and repair, RNA synthesis, and folate biosynthesis. The distinct cellular constituents as antibacterial targets include enzymes, enzyme substrates, RNA, DNA, membranes, etc. It is estimated that more than validated 40 targets have been developed for antimicrobial drugs on the market.
Amerigo Scientific offers HTS assays kits for screening potential antibacterial compounds that target the following validated targets:
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