Goodman and Gilman's The
Pharmacological Basis of Therapeutics
14th Edition
Author(s)Laurence Brunton; Bjorn Knollmann
Print ISBN: 9781264258079
,Question 1
A researcher isolates a biologically active compound from a medicinal
plant but initially has no information about its molecular target. Which
approach best characterizes the discovery strategy represented by this
finding?
A. Structure-based drug design
B. Phenotypic drug discovery
,C. Target-guided virtual screening
D. Fragment-based computational screening
Correct Answer:
B. Phenotypic drug discovery
Rationale:
A phenotypic discovery strategy begins with an observed biological
effect and works backward toward identifying the responsible
compound and, eventually, its molecular target. This approach is
historically important in natural-product drug discovery, where
biological activity could be recognized before the underlying
mechanism was understood.
• A is incorrect: Structure-based drug design generally requires
structural knowledge of a molecular target to guide compound
design or optimization.
• C is incorrect: Target-guided virtual screening requires a defined
molecular target before compounds are computationally
evaluated.
• D is incorrect: Fragment-based computational approaches
typically begin with small chemical fragments and a molecular
target rather than an unidentified biological effect.
Question 2
Why have medicinal plants historically served as useful starting points
for drug discovery?
, A. Plant compounds are uniformly safe at therapeutic concentrations
B. Plants contain diverse molecules capable of altering biological
processes
C. Plant-derived compounds usually have predictable pharmacokinetics
D. Plant extracts automatically satisfy modern drug-approval
requirements
Correct Answer:
B. Plants contain diverse molecules capable of altering biological
processes
Rationale:
Plants produce numerous chemically diverse compounds, including
molecules involved in defense and ecological interactions. Some of
these compounds exert biologically significant effects in humans and
can provide starting points for drug discovery.
• A is incorrect: Natural origin does not guarantee safety; some
plant-derived compounds are highly toxic.
• C is incorrect: Pharmacokinetic behavior must be experimentally
determined and cannot be assumed from natural origin.
• D is incorrect: A plant extract or natural product requires
appropriate scientific and regulatory evaluation before it can
become an approved medicine.
Question 3
A chemist modifies several functional groups on a natural product while
preserving the structural region believed to interact with its biological