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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.
However, in some cases, off-target activity can be taken advantage of for therapeutic purposes. An example of this is the repurposing of the antimineralocorticoid and diuretic spironolactone , which was found to produce feminization and gynecomastia as side effects, for use as an antiandrogen in the treatment of androgen-dependent conditions ...
Targeted covalent inhibitors (TCIs) or Targeted covalent drugs are rationally designed inhibitors that bind and then bond to their target proteins.These inhibitors possess a bond-forming functional group of low chemical reactivity that, following binding to the target protein, is positioned to react rapidly with a proximate nucleophilic residue at the target site to form a bond.
The phrase "drug design" is similar to ligand design (i.e., design of a molecule that will bind tightly to its target). [6] Although design techniques for prediction of binding affinity are reasonably successful, there are many other properties, such as bioavailability, metabolic half-life, and side effects, that first must be optimized before a ligand can become a safe and effictive drug.
The interaction between the drug and this site results in a modification of the target that may include inhibition or potentiation. [15] Most of the pharmacogenetic interactions that involve drug targets are within the field of oncology and include targeted therapeutics designed to address somatic mutations (see also Cancer Pharmacogenomics ).
When two drugs affect each other, it is a drug–drug interaction (DDI). The risk of a DDI increases with the number of drugs used. [1] A large share of elderly people regularly use five or more medications or supplements, with a significant risk of side-effects from drug–drug interactions. [2] Drug interactions can be of three kinds ...
Target validation normally requires the determination that the target is expressed in the disease-relevant cells/tissues, [6] it can be directly modulated by a drug or drug-like molecule with adequate potency in biochemical assay, [7] and that target modulation in cell and/or animal models ameliorates the relevant disease phenotype. [8]
However, the modalities can be combined; antibody-drug conjugates combine biologic and cytotoxic mechanisms into one targeted therapy. Another form of targeted therapy involves the use of nanoengineered enzymes to bind to a tumor cell such that the body's natural cell degradation process can digest the cell, effectively eliminating it from the ...
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