Drug Discovery Paradigms: Phenotypic-Based Drug Discovery. Talevi, A. & Bellera, C. L. In Scotti, M. T. & Bellera, C. L., editors, Drug Target Selection and Validation, of Computer-Aided Drug Discovery and Design, pages 25–40. Springer International Publishing, Cham, 2022. ![Drug Discovery Paradigms: Phenotypic-Based Drug Discovery [link]](https://bibbase.org/img/filetypes/link.svg "link")
Paper doi abstract bibtex A drug discovery and development project typically starts with the identification of novel active scaffolds, i.e., core chemical structures with a desired biological effect. Beyond serendipitous discoveries and findings based on ethnopharmacology/traditional medicine, drug discovery in the modern age has been guided by two fundamental screening philosophies (implemented whether through in silico, in vitro or less often, in vivo approximations). Occasionally, novel chemotypes can be designed de novo by searching for complementary features to a binding site in a predefined drug target. Historically, systematic screening for new active compounds comprised phenotypic screening assays (e.g., against a collection of microorganisms, animal models of disease, or cellular models). Later, the interest of the pharmaceutical companies experienced a substantial shift toward target-focused approximations in which exquisitely selective compounds were sought, usually through high-throughput screening. There, the test compounds were typically confronted with some biological entity, usually a protein, to identify those which could modulate such biomolecule. Nevertheless, as target-focused approximation failed to deliver the expectations, especially when pursuing therapies for complex disorders, renewed interest in phenotypic screening was observed in the pharmaceutical community, supported by a network pharmacology paradigm, high-content screening, small animal models, and organoids and other advanced cell culture platforms.
@incollection{talevi_drug_2022,
address = {Cham},
series = {Computer-{Aided} {Drug} {Discovery} and {Design}},
title = {Drug {Discovery} {Paradigms}: {Phenotypic}-{Based} {Drug} {Discovery}},
isbn = {978-3-030-95895-4},
shorttitle = {Drug {Discovery} {Paradigms}},
url = {https://doi.org/10.1007/978-3-030-95895-4_2},
abstract = {A drug discovery and development project typically starts with the identification of novel active scaffolds, i.e., core chemical structures with a desired biological effect. Beyond serendipitous discoveries and findings based on ethnopharmacology/traditional medicine, drug discovery in the modern age has been guided by two fundamental screening philosophies (implemented whether through in silico, in vitro or less often, in vivo approximations). Occasionally, novel chemotypes can be designed de novo by searching for complementary features to a binding site in a predefined drug target. Historically, systematic screening for new active compounds comprised phenotypic screening assays (e.g., against a collection of microorganisms, animal models of disease, or cellular models). Later, the interest of the pharmaceutical companies experienced a substantial shift toward target-focused approximations in which exquisitely selective compounds were sought, usually through high-throughput screening. There, the test compounds were typically confronted with some biological entity, usually a protein, to identify those which could modulate such biomolecule. Nevertheless, as target-focused approximation failed to deliver the expectations, especially when pursuing therapies for complex disorders, renewed interest in phenotypic screening was observed in the pharmaceutical community, supported by a network pharmacology paradigm, high-content screening, small animal models, and organoids and other advanced cell culture platforms.},
language = {en},
urldate = {2022-05-29},
booktitle = {Drug {Target} {Selection} and {Validation}},
publisher = {Springer International Publishing},
author = {Talevi, Alan and Bellera, Carolina L.},
editor = {Scotti, Marcus T. and Bellera, Carolina L.},
year = {2022},
doi = {10.1007/978-3-030-95895-4_2},
keywords = {Drug discovery, High-content analysis, High-content screening (HCS), High-throughput screening, Hit identification, Phenotypic screening, Target deconvolution, Target-focused approximations},
pages = {25--40},
}
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