Goodman and Gilman's The
Pharmacological Basis of Therapeutics
14th Edition
Author(s)Laurence Brunton; Bjorn Knollmann
Print ISBN: 9781264258079
,Question 1
Which historical approach most directly contributed to the early
identification of pharmacologically active substances?
A. Automated molecular docking
B. Traditional use of medicinal plants
C. DNA-encoded compound libraries
D. High-throughput receptor screening
,Correct Answer:
B. Traditional use of medicinal plants
Rationale:
Traditional medicinal practices provided empirical observations that
certain plants or plant-derived substances could alter biological
function, creating starting points for later isolation and
characterization of active compounds. This represents an effect-driven
approach rather than one based on a predefined molecular target. A.
Molecular docking is a modern computational approach that depends
on structural information. C. DNA-encoded libraries are modern
technologies for identifying binding compounds from very large
chemical collections. D. High-throughput screening emerged much
later and uses automated testing of large numbers of compounds.
Question 2
A researcher identifies a biologically active compound after
unexpectedly observing that a chemical being investigated for one
purpose produces a useful effect in a different disease model. Which
drug-discovery concept best describes this situation?
A. Structure-based drug design
B. Serendipitous discovery
C. Fragment-based drug discovery
D. Rational dose optimization
Correct Answer:
B. Serendipitous discovery
, Rationale:
Serendipitous discovery occurs when an important pharmacological
effect is recognized unexpectedly rather than emerging from a strictly
predefined target-driven design strategy. A. Structure-based drug
design begins with information about a biological target and uses
structural information to guide ligand development. C. Fragment-
based drug discovery starts with small chemical fragments that bind
weakly and develops them into stronger ligands. D. Dose optimization
concerns selection of an appropriate dose after a candidate already
exists and does not describe how the compound was discovered.
Question 3
A pharmaceutical company wants to evaluate tens of thousands of
compounds rapidly against a purified enzyme target. Which approach
is most appropriate?
A. High-throughput screening
B. Phase I clinical testing
C. Postmarketing surveillance
D. Therapeutic drug monitoring
Correct Answer:
A. High-throughput screening
Rationale:
High-throughput screening (HTS) uses automated systems to evaluate
large numbers of compounds for activity against a biological target
efficiently. The approach can identify initial “hits” for further
investigation. B. Phase I testing evaluates an investigational drug in