Small molecules and their roles in effective pre-clinical target validation

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Clegg, Michael and Tomkinson, Nicholas C. O. and Prinjah, Rab K. and Humphreys, Philip G. (2017) Small molecules and their roles in effective pre-clinical target validation. Future Medicinal Chemistry, 9 (14). pp. 1579-1582. ISSN 1756-8919 (https://doi.org/10.4155/fmc-2017-0121)

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Abstract

As demonstrated in multiple historical analyses, there are two main causes of clinical attrition; firstly drugs are not efficacious, and secondly they cause unacceptable toxicity, both of which can be the result of poor pre-clinical target validation. Target validation, one of the early stages of a drug discovery program, is the process of (in) validating a drug target to ensure it is significant to the intended disease, and unlikely to drive undesired toxicity. Target validation is vital in preventing late stage failures in the clinic and, if done effectively, can save pharmaceutical companies a great deal of time and money. As such, target validation is treated extremely seriously, as demonstrated by the formation of public - private partnerships, such as Open Targets, aimed to provide evidence of biological validity and the possible likelihood of pharmacological intervention. Central to the variety of molecular tools available for use in target validation are high quality small molecules called chemical probes.

ORCID iDs

Clegg, Michael, Tomkinson, Nicholas C. O. ORCID logoORCID: https://orcid.org/0000-0002-5509-0133, Prinjah, Rab K. and Humphreys, Philip G.;
  • Item type:Article
    ID code:61170
    Dates:
    Date
    Event
    22 December 2017
    Published
    19 May 2017
    Accepted
    12 May 2017
    Submitted
    Notes:© 2017 Future Science Ltd Clegg, M. A., Tomkinson, N. C., Prinjha, R. K., & Humphreys, P. G. (2017). Small Molecules and Their Role in Effective Preclinical Target Validation. Future Medicinal Chemistry, 9(14), 1579–1582. https://doi.org/10.4155/fmc-2017-0121
    Subjects:Science > Chemistry
    Medicine > Pharmacy and materia medica
    Department:Faculty of Science > Pure and Applied Chemistry
    Depositing user: Pure Administrator
    Date deposited:29 Jun 2017 11:16
    Last modified:11 Nov 2024 11:43
    Related URLs:
    URI:https://strathprints.strath.ac.uk/id/eprint/61170
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