Lecture material Flashcards
(27 cards)
When is the earliest you can patent a drug?
Lead discovery, but more reasonable to patent at lead optimization
When is the latest you can patent a drug?
Pre-clinical; before you apply for a clinical trial bc at that point the information is public
What is a lead?
A chemical compound likely to be therapeutically useful
What is a hit?
A compound with desired activity during screening
What is a target?
A protein in the body causing disease. Involved with the progression of disease
What is screening?
Quality/integrity of a hit or a lead. Elimination of harmful or useless compounds
What is MOA?
Mode of action
What is HTS?
High throughput screening which is automated testing for a specific target
What is in vitro testing?
Testing in test tubes, culture, dish
What is in vivo testing?
Testing on/in a living organism
What is in silico testing?
Testing the structure or function of a compound by using 3D technology and simulations
From ancient times until the mid-19th century, ID of new drugs was primarily the result of…
Serendipity (Unplanned, fortunate, discovery)
Ehrlich became the father of modern drug discovery because
A. Discovered chemoreceptors
B. Discovered that chemoreceptors were different between different tissues
C. Treated malaria patients with methylene blue
D. All of the above
E. A and B only
E.
What makes past drug discovery different from modern drug discovery?
A. Process is not structured, more luck based
B. No ethical concerns
C. More radical methods
D. Not target based
E. All of the above
E.
Explain the Wistar rat
A strain of albino rats. An attempt at a standard
Come in:
- diabetic
- tumour formers (Rochester strain)
- Hypersensitive
- Wistar kyoto (ADD model)
- Myelin-deficient rats
When you discuss “in vivo” testing, you must include the models
A. Gender
B. Sex
C. Diet
D. A and B
B.
Gender is only relevant when looking at phenotypes.
When is it ok to study a single sex and not the other?
If disease/condition is only present in one sex (example: menopause)
What makes a good target for drug discovery?
A target on a pathogen that isn’t contained in the human body
A target of interest that is common and reachable
A well-characterized disease/target
Something that can be manipulated without harmful effects on the body
What are the four classes of macromolecules?
Enzymes
GPCRs
Ion channels
Transporters
Sources for leads
Natural products (plants, marine life, fungi)
Synthetic libraries
Bacteria antibiotics
Genomes and genome mining
Metabolic engineering
What are Lipinski’s rule of 5 (Ro5)?
rotatable bonds <10
Molecular weight <500 DA
logP < 5 (solubility)
H bond donors <5
H bond acceptors <10
(the following was added by Daniel Veber et al.)
Polar surface area <140 A^2
What does a high logP value mean in Ro5?
The molecule is more hydrophobic
What compounds are acceptions to the Ro5?
Antibiotics
Antifungals
Vitamins
What is Ro3?
Molecular weight <300 DA
LogP < 3
H bond donors <= 3
H bond acceptors <=3
Rotatable bonds <=3
