What is target-centered drug design?

• A. Uses a validated biochemical or molecular target to search for hits.
• B. Relies on modifying natural ligands.
• C. Relies on random screening.
• D. Disregards knowledge of the target.

Answer: (A)

Target-centered drug design starts with a clearly defined, validated biological target implicated in disease and aims to modulate that target with small molecules. Because the target and its role are known, researchers search for compounds that bind to or inhibit (or activate) the target, then use structure-guided design and medicinal chemistry to optimize potency, selectivity, and pharmacokinetic properties. This approach relies on evidence that engaging the target will produce the desired therapeutic effect, often using structural data or computational tools to refine interactions and validate target engagement with biological assays. It contrasts with methods that don’t leverage a known target, such as random screening or simply modifying natural ligands without ensuring the target’s relevance to the disease.