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Generally, the "target" is the naturally existing cellular or molecular structure involved in the pathology of interest where the drug-in-development is meant to act. [9] However, the distinction between a "new" and "established" target can be made without a full understanding of just what a "target" is.
The term "biological target" is frequently used in pharmaceutical research to describe the native protein in the body whose activity is modified by a drug resulting in a specific effect, which may be a desirable therapeutic effect or an unwanted adverse effect. In this context, the biological target is often referred to as a drug target.
An example target identification by chromatographic co-elution (TICC) workflow. Drug-spiked lysate is fractionated using ion exchange chromatography. Fractions are collected every minute, then analyzed for both drug and protein content using LC-MS/MS. Drug and protein elution profiles are constructed and correlated. Target identification is ...
This approach is known as "reverse pharmacology" or "target based drug discovery" (TDD). [5] However recent statistical analysis reveals that a disproportionate number of first-in-class drugs with novel mechanisms of action come from phenotypic screening [6] which has led to a resurgence of interest in this method. [1] [7] [8]
Forward and reverse pharmacology approaches in drug discovery. In the field of drug discovery, reverse pharmacology [1] [2] [3] also known as target-based drug discovery (TDD), [4] a hypothesis is first made that modulation of the activity of a specific protein target thought to be disease modifying will have beneficial therapeutic effects.
By identifying the pharmacophore of the drug molecule, the profiling method of pattern recognition can be carried out where a new target is identified. [15] This provides an insight at a possible mechanism of action since it is known what certain functional components of the drug are responsible for when interacting with a certain area on a ...
Target validation (TV) → Assay development → High-throughput screening (HTS) → Hit to lead (H2L) → Lead optimization (LO) → Preclinical development → Clinical development The hit to lead stage starts with confirmation and evaluation of the initial screening hits and is followed by synthesis of analogs (hit expansion).
Druggability is a term used in drug discovery to describe a biological target (such as a protein) that is known to or is predicted to bind with high affinity to a drug. Furthermore, by definition, the binding of the drug to a druggable target must alter the function of the target with a therapeutic benefit to the patient.