Goodman and Gilman's The
Pharmacological Basis of Therapeutics
14th Edition
Author(s)Laurence Brunton; Bjorn Knollmann
Print ISBN: 9781264258079
,Question 1
A pharmaceutical research group begins a discovery program by
examining substances used traditionally in medicinal plants and then
isolates individual compounds to determine which constituents have
biological activity. Which historical approach to drug discovery is best
represented by this strategy?
,A. Structure-based drug design
B. Natural-product drug discovery
C. Molecular dynamics simulation
D. De novo computational design
Correct Answer:
B. Natural-product drug discovery
Rationale:
Natural-product drug discovery uses biologically active substances
obtained from natural sources as starting points for identifying
therapeutic compounds. The chapter describes drug discovery as
evolving from human experience with medicinal plants toward
increasingly systematic chemical and computational approaches.
(AccessPharmacy)
A. Structure-based drug design begins with structural information about
a biological target rather than depending primarily on naturally
occurring compounds.
C. Molecular dynamics is a computational method used to study
molecular behavior and interactions; it is not the historical approach
described in the stem.
D. De novo computational design generates candidate structures
computationally and represents a much more modern discovery
strategy.
Question 2
Why can a biologically active natural product be valuable as a starting
point for drug discovery even when the original compound is not
suitable for direct clinical use?
, A. Its biological activity can provide a starting point for chemical
optimization
B. Natural products are automatically safe in humans
C. Natural products do not require pharmacological testing
D. Natural products always possess ideal pharmacokinetic properties
Correct Answer:
A. Its biological activity can provide a starting point for chemical
optimization
Rationale:
A natural product can provide a chemically defined starting structure
whose biological activity can be investigated and optimized through
medicinal chemistry. Biological activity alone does not guarantee
suitability as a drug.
B. Natural origin does not establish safety. Natural compounds can have
substantial toxicity.
C. Natural products still require characterization and pharmacological
evaluation.
D. Bioavailability, metabolism, distribution, and toxicity can all limit a
natural product's usefulness.
Question 3
A research team has identified a cellular protein that appears to
contribute to disease progression. Before investing in extensive
compound screening, investigators want to determine whether altering
this protein is likely to produce a therapeutically useful effect. Which
step is most directly being addressed?
A. Target validation
B. Drug formulation