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

Résumé

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.

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Concepts associés (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.
Conception de médicament
La conception de médicament, plus précisément conception de substance pharmacologiquement active plus connue sous sa dénomination anglaise Drug design est l'ensemble des processus nécessaires à l'élaboration d'un médicament. Dans l'industrie pharmaceutique, ces processus peuvent-être subdivisés et répartis en quatre phases ou étapes : La phase de recherche La phase de développement La phase clinique La phase de mise sur le marché Remarque : Les phases de recherche et développement sont communément dénommées R&D.
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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