Early Probe and Drug Discovery in Academia: A Minireview

High-throughput
Anuradha Roy

Abstract

Drug discovery encompasses processes ranging from target selection and validation to the selection of a development candidate. While comprehensive drug discovery work flows are implemented predominantly in the big pharma domain, early discovery focus in academia serves to identify probe molecules that can serve as tools to study targets or pathways. Despite differences in the ultimate goals of the private and academic sectors, the same basic principles define the best practices in early discovery research. A successful early discovery program is built on strong target definition and validation using a diverse set of biochemical and cell-based assays with functional relevance to the biological system being studied. The chemicals identified as hits undergo extensive scaffold optimization and are characterized for their target specificity and off-target effects in in vitro and in animal models. While the active compounds from screening campaigns pass through highly stringent chemical and Absorption, Distribution, Metabolism, and Excretion (ADME) filters for lead identification, the probe discovery involves limited medicinal chemistry optimization. The goal of probe discovery is identification of a compound with sub-µM activity and...Continue Reading

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Citations

Dec 5, 2018·Expert Opinion on Drug Discovery·Anuradha Roy
Jan 16, 2019·Chemistry, an Asian Journal·Zsuzsa SárkányPedro M Martins
Mar 19, 2020·Natural Product Reports·Brice A P WilsonBarry R O'Keefe
Jun 13, 2020·Cancers·Praveensingh B HajeriMasato Yamamoto
Feb 19, 2020·Current Pharmaceutical Design·Eleonore Fröhlich
Jul 2, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Qingxin Li, CongBao Kang
May 1, 2021·Viruses·Yogy SimanjuntakPietro Scaturro
Aug 14, 2020·ACS Combinatorial Science·Alexander T TaguchiNeal W Woodbury
Dec 14, 2019·The Journal of Organic Chemistry·Yoarhy A Amador-SánchezLuis D Miranda

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Methods Mentioned

BETA
two hybrid
Fluorescence
PCR
X-ray
fluorescence-activated cell sorting
thermal shift

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