What is High-Throughput Screening in Drug Discovery

What is the term High-Throughput Screening in Drug Discovery?

High-throughput screening (HTS) is the most sophisticated method that utilizes automation, robotics, and artificial intelligence to rapidly screen millions of compounds or samples at a given time. This technique is mainly used in pharma and biotech companies for compound identification and helps accelerate the drug discovery procedure.

What role does high-throughput screening play in drug discovery?

HTS helps accelerate the identification of test targets against a vast library of compounds. This approach enables drug companies in their goal of achieving fast and efficient drug discovery and development.

How does high-throughput screening work in drug discovery?

High-throughput screening has revolutionized the pharma sector by automating and optimizing the screening process. With the help of automation, robotic-assisted sample handling, compatible assay designs, and data analytics and interpretation, the HTS method allows researchers to rapidly identify compounds and generate insightful data on various compound interactions, toxicity, and efficacy. Researchers leverage this large pool of compounds to identify promising leads with the desired therapeutic potential.

What are the steps involved in high-throughput screening?

The major steps involved in HTS are:

• Assay development
• Library preparation
• Dry run
• Primary screening
• Data analysis
• Secondary screening
• Preliminary SAR
• Preclinical evaluation
• Clinical trials

What are the advantages of using high-throughput screening over traditional screening methods?

Efficiency: HTS allows for the screening of millions of compounds/antibodies in a short period simultaneously, accelerating the screening process and hence increases the efficiency.
Broad screening capability: HTS can screen 10,000 to 100,000 per day/week, compared to traditional methods of screening 20-50 compounds per week, enabling comprehensive analysis of compound libraries.
Quality data: HTS provides accuracy with precision which ensures that the hits identified are truly active against the intended target. This increases the confidence in the identified hits, facilitating potent target identification.
Cost efficiency: The setup cost will always be there but once installed it has greater utility than the traditional methods.
Minimally labor-intensive: HTS relies on automated software and data processing with robotic-assisted sample handling, thus reducing the need for human interventions.

How has high-throughput screening impacted drug discovery?

High-throughput drug screening has impacted drug discovery in any way, such as:

High-throughput screening (HTS) has enabled increased speed, efficiency, and productivity of the drug discovery process allowing researchers to screen a substantially higher number of compounds than traditional methods.

The precision and targeted approach of HTS enables comprehensive ways of locating the targets and identifying and screening large numbers of molecules in a short period.

Furthermore, HTS can be applied to a wide range of biological targets, like enzymes, ion channels, receptors, and cellular pathways. This versatility allows researchers to probe diverse therapeutic targets implicated in various diseases, leading to the discovery of novel drug candidates for previously unexplored targets.

The flexibility of generating large, statistically significant datasets with HTS facilitates the identification of true hits with greater confidence and reduces the risk of false positives, allowing researchers to emphasize the most promising compounds for further optimization.

HTS has greatly impacted drug discovery as it has become a valuable tool in optimizing and automating complex and lengthy processes.

High throughput screening (HTS) is an inseparable part of the scientific toolkit and is being widely used for the discovery of new chemotypes and integration of small-molecule discovery by both biomedical researchers and academics.

What are some examples of successful drugs discovered through high-throughput screening for cancer treatment?

• Nutlins and benzodiazepinediones as p53-MDM2 inhibitors.
• Antineoplastic agents like histone deacetylase inhibitor trichostatin A, thiram, disulfiram (DSF), and monensin.
• Various novel drugs for anti-infective agents were discovered through high-throughput screening.
• Drugs aimed at cancer genome targets like Herceptin, Gleevec, and Iressa.