Classical pharmacology

Forward (classical) and reverse pharmacology approaches in drug discovery

In the field of drug discovery, classical pharmacology,[1] also known as forward pharmacology,[2][3][4] or phenotypic drug discovery (PDD),[5] relies on phenotypic screening (screening in intact cells or whole organisms) of chemical libraries of synthetic small molecules, natural products or extracts to identify substances that have a desirable therapeutic effect. Using the techniques of medicinal chemistry, the potency, selectivity, and other properties of these screening hits are optimized to produce candidate drugs.

  1. ^ Takenaka T (September 2001). "Classical vs reverse pharmacology in drug discovery". BJU Int. 88 Suppl 2: 7–10, discussion 49–50. doi:10.1111/j.1464-410X.2001.00112.x. PMID 11589663. S2CID 30711746.
  2. ^ Lazo JS (April 2008). "Rear-view mirrors and crystal balls: a brief reflection on drug discovery". Mol. Interv. 8 (2): 60–3. doi:10.1124/mi.8.2.1. PMID 18403648.
  3. ^ Bachmann KA, Hacker MP, Messer W (2009). Pharmacology principles and practice. Amsterdam: Elsevier/Academic Press. p. 576. ISBN 978-0-12-369521-5.
  4. ^ Vogt A, Lazo JS (August 2005). "Chemical complementation: a definitive phenotypic strategy for identifying small molecule inhibitors of elusive cellular targets". Pharmacol. Ther. 107 (2): 212–21. doi:10.1016/j.pharmthera.2005.03.002. PMID 15925410.
  5. ^ Lee JA, Uhlik MT, Moxham CM, Tomandl D, Sall DJ (May 2012). "Modern phenotypic drug discovery is a viable, neoclassic pharma strategy". J. Med. Chem. 55 (10): 4527–38. doi:10.1021/jm201649s. PMID 22409666.