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CIVIT 202 > Drug Discovery > Flashcards

Drug Discovery Flashcards

1
Q

Drugs affect:

A

mRNA
proteins
Translation
Transcription

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2
Q

Improving=

A

optimization

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3
Q

Drugs that are too disruptive can

A

affect DNA and cause cancer

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4
Q

From Discovery to approval: stages

A
  1. Drug Discovery
  2. Drug Development
  3. Clinical Trials
  4. Manufacturing
  5. Marketing Application
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5
Q

The process of determining both a target for the treatment of disease and agents that affect the target
-results in identification of a lead compound.

A

Drug Discovery

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6
Q

The lead compound is analyzed for effectiveness, then optimized (an iterative process)

A

Drug Development

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7
Q

A procedure in which repetition of a sequence of operations yields results successively closer to a desired result

A

Iterative process

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8
Q

Evaluations conducted on human subjects, testing for safety and efficacy of the drug.

A

Clinical Trials

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9
Q

The large-scale production of the drug.

A

Manufacturing

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10
Q

The process of requesting approval from regulatory authorities (e.g. FDA)

A

Marketing Application

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11
Q

Drug function by interacting with a target (usually a receptor) in the body.
-Drug/target model is often referred to as this.

A

The drug receptor hypothesis

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12
Q

Receptor = lock

Drug=key

A

lock and key model

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13
Q

Key concept:

A

Most of the time, we have a target receptor and need to find a drug which affects it.

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14
Q

Involves scanning thousands of compounds, looking for a “hit”.

A

Irrational drug development

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15
Q

Seeks to identify drug candidates a priori.

A

Rational drug development

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16
Q

Statement that can be tested/ has data that supports it.

A

Hypothesis

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17
Q

Drug conforms to receptor like a hand that fits into a glove.

A

Induced Fit Model

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18
Q

Specific drug for a specific receptor

-ex. “Magic Bullet”

A

Selectivity

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19
Q

Key Concept #2:

A

Drugs are usually developed to accommodate an unmet medical need.

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20
Q

Pharmaceutical companies need to consider:

A
  • Market potential
  • Patent-ability, capacity for intellectual property
  • Competitive forces and regulatory status
  • Core competencies (ability to succeed)
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21
Q

Central Dogma of Molecular Biology

A

DNA (genes/source) ——->transcription——–>mRNA (transient copy)——–>translation——>Protein (function)

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22
Q

Structure =

A

function

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23
Q

Side effects generally increase as

A

Specificity decreases

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24
Q

Undesired effect of a drug.

A

Side-effect

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25
Q

Drug target: genes

-Most drugs target proteins

A

To understand drug-receptor interactions, it’s usually best to consider what’s going on at a cellular/molecular level

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26
Q

A segment of DNA that codes for a protein

A

gene

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27
Q

Drug target: genes cont…

A

Most disease states have a genetic connection, related to one (or more) proteins produced by genes.
-Humans have differences in their genes, affecting their susceptibility to disease and ability to be treated.

28
Q

Ideal drug development requires knowledge of the genetic basis for a disease

A

High specificity = high efficancy

29
Q

Ex. p53 Protein and Cancer:

A
  • p53 gene is a tumor-suppressor gene
  • Gene encodes the p53 protein, which has the normal fxn. of triggering apoptosis in cells that start to become cancerous.
  • probs with the p53 gene lead to dysfunction in the production of protein and apoptosis is inactivated.
  • tumor progression goes unchecked
30
Q

Methods of target identification:

-There are several commonly employed methods that scientists use to identify a molecular target for a disease.:

A
  1. Radioligand Binding
  2. DNA Microarray
  3. Expressed Sequence Tags (ESTs)
31
Q

A molecule which interacts (binds) to a receptor. Can be endogenous or exogenous

A

Ligand

32
Q

The structure of a disease-related ligand an be modified to incorporate one or more radioactive atoms, making a ______.
-Structure is the same, atom is changed to a radioactive isotope to test and detect.

A

Radioligand

33
Q

Radioligand Binding extra info:

A
  • Radioligand can be exposed to pool of possible receptors
  • Receptors that demonstrate radioactivity were likely bound to the radioligand and may be possible site(s)
  • They detect which receptors the drug interacts with, NOT where on the receptor.
34
Q

Come from within the cell

A

Endogenous

35
Q

Come from outside the cell

-perhaps from a drug

A

Exogenous

36
Q

Unstable molecule which can decay and be monitored.

A

Radioactive Molecule

37
Q

Allows us to directly evaluate genes that are being expressed in cells.

A

DNA microarray

38
Q

DNA microarray

A
  • Looks at DNA instead of protein
  • By comparing expression patterns of healthy vs. diseased cells, we may discover differences, some of which may be involved in disease progression.
39
Q

Is a short nucleotide sequence of DNA (200-500 bps) that codes for a protein.

A

Expressed Sequence Tags (ESTs)

40
Q

ESTs info:

A
  • Using computational databases and algorithms, ESTs can be compared to a large number of proteins, an in silico approach.
  • To accomplish this, the computer attemtps to predict the final 3D shape of a resultant protein based on the nucleotide sequence of the DNA
  • Takes the DNA sequence and determines what 1, 2, and 3 shapes will be thus what final 3D shape will be.
41
Q

Catalysis

A

A modification and especially increase in the rate of a chemical reaction induced by material unchanged chemically at the end of the reaction

42
Q

Target Validation:
-Once a molecular target for potential frug development has been identified (using one of the search approaches), it needs to be validated (confirmed that it isn’t a false positive)

A
  • Combines in vitro, in vivio, and in silico methods to ask:
  • What is the fxn of the target?
  • Which disease pathway does the target regulate?
  • How imporant is the disease pathway (is there a bottleneck)?
  • What is the expected therapeutic index if a drug were to interact with the target? (beneficial or toxic? effects on homeostasis) Receptors are natively in our bodies.
43
Q

Key Concept #3:

A

Proteins constitute the major type of target with which drugs interact to elicit a beneficial effect.

44
Q

Are proteins which catalyze biochemical reactions; drug interaction can modulate their activity

A

Enzymes

45
Q

Are located on the interior of a cell; drugs wishing to interact with these must first pass the lipid bilayer

A

Intracellular Receptors

46
Q

Are embedded in the cell membrane; drug interaction often induces signaling cascades

A

Cell surface receptors

47
Q

In an advantageous drug/target interaction, binding:

A
  • Is specific
  • Occurs at particular sites in the target molecule
  • Is reversible
48
Q

A drug when binding activates a biochemical rxn is known as an ______.

A

agonist

49
Q

A drug is a _____ when binding inhibits a biochemical rxn.

A

antagoinst

50
Q

Key Concept #4:

A

The 3D shape of a drug is directly related to its ability to interact with the target (and elicit an effect)

51
Q

Drug shape = function

A

-drug/target interactions occur through a combo of noncovalent, electrostatic interactions, including
H-bonding (strong dipole-dipole interaction)
Van der waals forces (polar and nonpolar)
-As noncovalent interactions, these binding events are reversible. (few drugs react covalently)

52
Q

Are biological molecules which speed up the rate of a biochemical rxn, a process known as catalysis.

  • most are proteins
  • have variety of functions
  • Are not consumed in the rxn; lower energy barrier btwn reactants and products
A

enzymes

53
Q

Enzymes function by bringing reactants in the correct:

A
  1. Proximity (close range)

2. Orientation (collide in correct way)

54
Q

The part of an enzyme that brings reactants together (through binding) is called the_____.

A

Active Site

55
Q

Key Concept #5

A

Many drugs function as an inhibitor of an enzyme active site

56
Q

Bind to the enzyme site, preventing its use by the normal reactants.

A

Competitive Inhibitors

57
Q

Bind to a different region of the enzyme, changing the shape of the enzyme and preventing its ability to catalyze reactions.

A

Noncompetitive Inhibitors

58
Q

Key Concept #6:

A

Disruption of cellular communication leads to uncoordinated (unregulated) processes
-Cell surface receptors function to relay chemical communication signals through signal transduction.

59
Q

Are an incredibly important class of drug targets

  • More than 30% of current drugs target this class
  • Are cell surface proteins which initiate and relay chemical signals to the interior of the cell (usually includes a signal cascade)
  • Drug’s message crosses cell membrane, drug does not.
A

G-Protein coupled receptors (GPCRs)

60
Q

Facilitate passage of polar ions across a cell membrane

-variants include ligand gated (small molecules ) and voltage gated (nerve transmission)

A

Ion channel receptors

61
Q

Are located on the outside surface of cells and initiate signal cascades from hormones and growth receptors through phosphorylation events

  • amplify and activate proteins
  • allow rapid response to external stimuli
A

Tyrosine Kinases

62
Q

Are located within cells and regulate transcription messages from genes
-often regulate transcription, translation, expression, etc…

A

Intracellular Receptors

63
Q

An important aspect of drug discovery process is being able to efficiently evaluate the ability of the drug to affect the target:

A

-To simplify the complexity of using living systems, one or more biochemical assays usually need to be developed

64
Q

an ideal assay provides a method to quantitatively monitor the effects of a drug vs. time using:

A
  • a non-living system which mimics the target
  • a way to measure a biological or physiological effect (endpoint) which is relevant to the target being studied
  • a mechanism to easily visualize the results (emission of light, fluorescence, etc…)
65
Q

Biochemical Assays cont…: Development

A

-how to get things on a small scale
(1 molecule = 10^-9 nm)
-allow high through-put screening

66
Q

Functions of enzymes:

A
  1. remove or add hydrogen atoms in oxidation or reduction rxns.
  2. transfer fxnal groups
  3. hydrolyze various fxnal groups
  4. add water, ammonia, or carbon dioxide across double bonds or remove elements to produce double bonds
  5. convert between different isomers
  6. form a bond between molecules

CIVIT 202 (1 decks)

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