Publication

Miniaturized technologies for high-throughput drug screening enzymatic assays and diagnostics - A review

Paul Joseph Dyson, Sarah Alexandra Pais Pereira
2020
Journal paper

Abstract

Drug discovery is a complex, multistep process, in which many challenges need to be overcome at each stage, from the discovery of a biomolecular target to the ensuring of the efficacy and safety of a compound in humans. Today's analytical methods allow tens of thousands of drug candidates to be screened for their ability to inhibit specific enzymes and the miniaturization of these approaches is highly desirable, accelerating the drug discovery process and reducing the associated costs. Herein, it is reviewed the miniaturized techniques currently used to evaluate enzymatic activity and inhibition giving special attention to microplate formats, microarrays, nanoarrays, and microfluidic technologies. It is, also, highlighted some of the characteristics and their abilities for potential uses are compared and discussed. In addition, the challenges of their applications in diagnosis, analysis, and therapy, which should help to improve the quality of healthcare globally are also pointed out. (C) 2020 Elsevier B.V. All rights reserved.

Official source

https://infoscience.epfl.ch/record/278230?ln=en

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Ontological neighbourhood

Health sciences

Pharmacology: Drug discovery

Related concepts (21)

Drug discovery

In the fields of medicine, biotechnology and pharmacology, drug discovery is the process by which new candidate medications are discovered. Historically, drugs were discovered by identifying the active ingredient from traditional remedies or by serendipitous discovery, as with penicillin. More recently, chemical libraries of synthetic small molecules, natural products or extracts were screened in intact cells or whole organisms to identify substances that had a desirable therapeutic effect in a process known as classical pharmacology.

Drug design

Drug design, often referred to as rational drug design or simply rational design, is the inventive process of finding new medications based on the knowledge of a biological target. The drug is most commonly an organic small molecule that activates or inhibits the function of a biomolecule such as a protein, which in turn results in a therapeutic benefit to the patient. In the most basic sense, drug design involves the design of molecules that are complementary in shape and charge to the biomolecular target with which they interact and therefore will bind to it.

Fragment-based lead discovery

Fragment-based lead discovery (FBLD) also known as fragment-based drug discovery (FBDD) is a method used for finding lead compounds as part of the drug discovery process. Fragments are small organic molecules which are small in size and low in molecular weight. It is based on identifying small chemical fragments, which may bind only weakly to the biological target, and then growing them or combining them to produce a lead with a higher affinity. FBLD can be compared with high-throughput screening (HTS).

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