Early Probe and Drug Discovery in Academia: A Minireview
dc.contributor.author | Roy, Anuradha | |
dc.date.accessioned | 2018-06-13T17:27:44Z | |
dc.date.available | 2018-06-13T17:27:44Z | |
dc.date.issued | 2018-02-09 | |
dc.identifier.citation | Roy, A. (2018). Early Probe and Drug Discovery in Academia: A Minireview. High-Throughput, 7(1), 4. http://doi.org/10.3390/ht7010004 | en_US |
dc.identifier.uri | http://hdl.handle.net/1808/26503 | |
dc.description.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 reasonable selectivity in the context of the target being studied. The compounds identified from probe discovery can also serve as starting scaffolds for lead optimization studies. | en_US |
dc.publisher | MDPI | en_US |
dc.rights | Copyright © 2018 by the author. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/). | en_US |
dc.rights.uri | http://creativecommons.org/licenses/by/4.0/ | en_US |
dc.subject | High-throughput screening | en_US |
dc.subject | Assay development | en_US |
dc.subject | Small molecules | en_US |
dc.subject | Drug and probe discovery | en_US |
dc.title | Early Probe and Drug Discovery in Academia: A Minireview | en_US |
dc.type | Article | en_US |
kusw.kuauthor | Roy, Anuradha | |
kusw.kudepartment | High Throughput Screening Laboratory | en_US |
dc.identifier.doi | 10.3390/ht7010004 | en_US |
kusw.oaversion | Scholarly/refereed, publisher version | en_US |
kusw.oapolicy | This item meets KU Open Access policy criteria. | en_US |
dc.rights.accessrights | openAccess | en_US |
Files in this item
This item appears in the following Collection(s)
Except where otherwise noted, this item's license is described as: Copyright © 2018 by the author. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).