Biological target
A biological target is anything within a living organism to which some other entity (like an endogenous
Mechanism
The external stimulus (i.e., the drug or ligand) physically binds to ("hits") the biological target.[1][2] The interaction between the substance and the target may be:
- noncovalent – A relatively weak interaction between the stimulus and the target where no chemical bond is formed between the two interacting partners and hence the interaction is completely reversible.[citation needed]
- reversible covalent – A chemical reaction occurs between the stimulus and target in which the stimulus becomes chemically bonded to the target, but the reverse reaction also readily occurs in which the bond can be broken.[citation needed]
- irreversible covalent – The stimulus is permanently bound to the target through irreversible chemical bond formation.[citation needed]
Depending on the nature of the stimulus, the following can occur:[3]
- There is no direct change in the biological target, but the binding of the substance prevents other ion channel blockade.
- A conformational change in the target is induced by the stimulus which results in a change in target function. This change in function can mimic the effect of the endogenous substance in which case the effect is referred to as receptor agonism (or channel or enzyme activation) or be the opposite of the endogenous substance which in the case of receptors is referred to as inverse agonism.
Drug targets
The term "biological target" is frequently used in
- proteins
- G protein-coupled receptors (target of 50% of drugs)[7]
- enzymes (especially protein kinases, proteases, esterases, and phosphatases)
- ion channels
- nuclear hormone receptors
- structural proteins such as tubulin
- membrane transport proteins
- nucleic acids
Drug target identification
Identifying the biological origin of a disease, and the potential targets for intervention, is the first step in the discovery of a medicine using the
Databases
Databases containing biological targets information:
Conservation ecology
These biological targets are conserved across species, making pharmaceutical pollution of the environment a danger to species who possess the same targets.
See also
References
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- ISBN 978-0-7020-3471-8.
- ISBN 978-0-7020-3471-8.
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Novelty of target and MoA [Mechanism of Action] is the second major potential advantage of PDD [Phenotypic Drug Discovery]. In addition to identifying novel targets, PDD can contribute to improvements over existing therapies by identifying novel physiology for a known target, exploring 'undrugged' targets that belong to well known drug target classes or discovering novel MoAs, including new ways of interfering with difficult-to-drug targets.
- S2CID 13577563.
- PMID 21077692.
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- ^ PMID 18754513.
- .
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- PMID 17936335.