DRUG DISCOVERY -FINDING A LEAD

Question 1

biological molecules that could serve as drug targets

Answer 1

lipids
proteins
nucleic acids
carbohydrates

Question 2

what is required to find lead compounds and for
drug optimisation

Answer 2

tests

Question 3

initial tests confirming the activity of a compound as a lead compound in vivo, true or false

Answer 3

false, they are done in vitro

Question 4

in vivo

Answer 4

performed or taking place in a living organism

Question 5

in vitro

Answer 5

studies conducted using components of an organism that have been isolated from their usual biological surroundings, such as microorganisms, cells, or biological molecules.

in glass

Question 6

IC50

Answer 6

used in pharmacology and biochemistry to describe the potency of a substance in inhibiting a specific biological or biochemical function by 50%. it simply refers to the half-maximal inhibitory concentration

Question 7

sources of a lead compound

Answer 7

The Natural World
The Synthetic World
The Virtual World

Question 8

lead compound

Answer 8

a molecule that exhibits a desired biological activity and is used as the foundation for the development of new drugs. it is used as the starting point for drug design and development

Question 9

properties of lead compounds

Answer 9

potency, selectivity for the target, and favourable pharmacological properties.

Question 10

what are some methods of identifying lead compounds

Answer 10

FBLD(fragment based lead discovery)
High Throughput screening
Very high throughput screening
NMR screening

Question 11

what are some methods used to determine the molecular structures of lead compounds

Answer 11

Elemental analysis
Molecular weight
Mass spectrometry
Infrared spectroscopy
NMR spectroscopy
X-ray crystallography

Question 12

methods for isolating and purifying lead compounds

Answer 12

Solvent-solvent extraction
Chromatography
Crystallisation
Distillation

Question 13

chromatography

Answer 13

a versatile technique used for separating mixtures based on the differential distribution of components between a stationary phase and a mobile phase.

Question 14

X-ray crystallography

Answer 14

a widely used method for determining the three-dimensional structure of a crystalline material, including organic compounds.

Question 15

HTS

Answer 15

a method used to rapidly test large libraries of compounds for their ability to interact with a target. It allows for the screening of thousands to millions of compounds in a relatively short time

Question 15

VHTS

Answer 15

involves the use of computational methods and virtual screening to predict the potential binding affinity of large databases of compounds with a target protein.

Question 16

FBLD

Answer 16

an approach used in drug discovery to identify small, low-molecular-weight fragments that bind to a target protein. These fragments serve as starting points for developing lead compounds.

Question 17

the aim of structure activity relationships(SAR)

Answer 17

Identify which functional groups are important for binding and/or activity

Question 18

method for testing the SAR of a compound

Answer 18

Alter, remove or mask a functional group
Test the analogue for activity
If in vitro activity drops, it implies group is important for binding activity

Question 19

analogue

Answer 19

a compound that is structurally similar to another compound but may differ in certain key aspects, example it might have a different functional group

Question 20

pharmacophore

Answer 20

a three-dimensional arrangement of chemical features within a molecule that are essential for its biological activity at a receptor or enzyme