Drug Targets Screening Based on SPR Technology

The site of binding of a drug to a biomolecule in the body is the drug target. The targets of drug action involve receptors, enzymes, ion channels, transporters, the immune system, genes and so on. The selection of targets is the starting point for drug development. How to find the more promising and promising target among the many targets is the focus of the new drug development process.

• Enzymes as targets

Enzymes are specific proteins produced by cells in the body that are catalytically active and highly specific. As enzymes are involved in the pathogenesis of some diseases, they catalyse the production of pathological response mediators or regulatory factors. Enzymes are therefore an important class of drug targets. Drugs that target enzymes can inhibit, induce, activate or revive them. Most of the drugs commonly used today are enzyme inhibitors. In addition, some drugs are enzymes themselves, such as pepsin and trypsin. Other drugs are substrates of enzymes and need to be converted to act.

• Ion channels as targets

Ion channels are composed of subunits formed by peptide chains that travel back and forth across the membrane several times. The main ion channels are Ca²⁺, K⁺, Na⁺ and Cl^- channels, whose function is to regulate the distribution of inorganic ions inside and outside the cell membrane. The opening or closing of channels affects the transport of inorganic ions inside and outside the cell and can rapidly alter cellular function, causing neural excitation, cardiovascular contraction or glandular secretion. Some drugs modulate ion channels by activating receptors. In addition, some ion channels are the direct targets of drugs, which open or close them by altering their conformation.

• Genes as targets

In recent years, as genetic research has intensified, genes associated with certain diseases have been found one after another. Nucleic acid drugs are drugs that act at the nucleic acid level, with the main action being to interfere with or block the synthesis of nucleic acids in bacteria, viruses and tumour cells, ultimately achieving effective killing or inhibition of bacteria, viruses and tumour cells. The main mechanisms of action of drugs that target nucleic acids include affecting, interfering with or blocking the synthesis of DNA/RNA.

Many single-target drugs have been developed to date, but there is no doubt that the efficacy of single-target drugs for complex diseases is limited. In complex diseases, the pathogenesis is often dependent on a series of biochemical events and several biological receptors. The efficacy and safety of multi-targeted drugs is better than that of single-targeted drugs and therefore the development of multi-targeted drugs is a hot emerging field at the moment. The images below illustrate how multi-targeted drugs are designed.

Fig.1 The conceptual diagram of ideas for the development of multi-target drugs. (Makhoba, X, H, et al., 2020)

Surface plasmon resonance (SPR) in the process of drug targets screening

In the early stages of drug development, the starting point for both single and multi-target drug therapies is to find and screen for the desired target. The screening of targets involves the exploration of disease mechanisms and drug action mechanisms. In this process, molecular interaction analysis is essential. The difference is that target screening for multi-targeted drugs is more complex and time-consuming than for single-targeted drugs. Molecular interaction analysis is involved in the target screening and validation process and therefore the selection of an efficient molecular interaction platform for target screening is very important throughout the drug development process. At Creative Proteomics, we offer SPR that can provide you with high quality molecular interaction analysis services. A broad conceptual diagram of the SPR technology platform involved in target screening is shown below. As you can see in the diagram, the SPR technology platform provides an efficient molecular interaction analysis service for target discovery, screening and validation.

Fig.2 BIAchip™ in the process of drug targets screening

Compared to other target screening methods, our technology platform has the following distinct advantages.

• The most fundamental basis and criteria for target screening is based on the effect of molecular interactions. Our SPR technology platform can provide high throughput molecular interaction analysis during your target screening process, allowing you to improve screening efficiency and reduce time wastage when faced with a large number of targets to be screened.
• It is well known that there are many different types of targets and the high flexibility and scalability of SPR technology allows for the analysis of interactions between various types of biomolecules. From Creative Proteomics you can get any customised service you want, with short lead times and customer satisfaction guaranteed.
• The accuracy of results is at an unprecedented level, providing you with the assurance that you can subsequently achieve peace of mind. In addition, the high sensitivity of the SPR technology platform ensures low detection limits, so you don't have to worry about no signal or false negatives when analyzing small molecular weight samples.

With so many significant advantages for molecular interaction analysis during target screening, why not try our SPR technology platform? Once you have placed your order, Creative Proteomics will arrange for you to receive a tailor-made service from our experts in target screening field. All services are available on a 24/7/365 basis. If you have any questions or suggestions about our SPR services, please feel free to contact us right now.

For research use only. Not intended for any clinical use.