Back to basics with receptors and ligands – molecules, mechanisms and medicine

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Nirthanan, Selvanayagam
Griffith University Author(s)
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2019
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Abstract

Drug discovery is a complex, substantially long, technology-driven, labour-intensive and inordinately expensive process involving target discovery and validation, lead identification by high-throughput screening, and lead optimization by medicinal chemistry, preclinical evaluation in animal models, pharmacological screening (ADME screen: administration, distribution, metabolism, elimination) and studies of toxicology, specificity, and drug interactions. While comprehensive drug discovery workflows are predominantly undertaken in the big pharma domain, drug discovery in academia must not be discounted. Research relevant to drug discovery in academia is generally at the fundamental level, with a focus on drug mechanisms and the identification and validation of potential therapeutic targets, often in commercially unattractive, but relevant therapeutic areas particularly for the developing world, including rare disorders, parasitic diseases, and in research into natural products. Investigating natural sources for drug leads include compounds from venomous animals; with illustrious examples of success such as captopril (angiotensin converting enzyme inhibitor for the treatment of hypertension), exenatide (a glucagonlike peptide-1 receptor agonist for the treatment of type 2 diabetes) and ziconotide (an N-type calcium channel blocker for intractable pain)

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Journal of the Ceylon College of Physicians

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50

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2

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© The Author(s) 2020. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.

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Pharmacology and Pharmaceutical Sciences

Clinical Sciences

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Nirthanan, S, Back to basics with receptors and ligands – molecules, mechanisms and medicine, Journal of the Ceylon College of Physicians, 50 (2), pp. 51-51

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