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Foundations Exam 1 > McPhail > Flashcards

McPhail Flashcards

(75 cards)

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1
Q

What was important about the discovery of the ability to synthesize salicylic acid?

A

It showed that we can get a large amount of a product without using all of our natural resources

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2
Q

Potential therapeutic target

A

genomic sequence specific to disease

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3
Q

target validation

A

assays/tests

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4
Q

Hits

A

Compound that was effective in the assay

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5
Q

Hit validation with follow up assays

A

Different assays to make sure the hit actually works and wasn’t just in the right conditions

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6
Q

Clinical candidate

A

Shows potential but hasn’t been tested

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7
Q

Drug discovery process

A

Elucidation and selection of a potential therapeutic target, target validation, screening assay development, high throughput screening, hits, hit validation with follow up assay, lead compound, lead optimization, clinical candidate, pre-clinical and clinical studies, approval, new chemical entity as a therapeutic candidate

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8
Q

Lead profiling

A

Testing how good a lead compound is

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9
Q

What is the difference between hit and lead?

A

A hit worked for that particular assay, but a lead works for several.

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10
Q

What is the mission of the FDA?

A

To promote and protect public health by guiding safe and effective drug products to the market in a timely manner

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11
Q

What are phase IV clinical trials?

A

Post-market surveillance

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12
Q

What are the four functions of the FDA?

A

(1) To monitor and protect public health by guiding safe and effective drug products to the market in a timely manner (2) To monitor products for continued safety after they’re on the market (3) To regulate biologicals, medical devices, veterinary drugs, food products, and animal feed (4) To monitor the safety of cosmetics, other medical and consumer products, and devices which emit radiation

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13
Q

What FDA centers monitor human pharmaceuticals?

A

Center for Drug Evaluation and Research, Center for Biologics Evaluation and Research, and the Office of Regulatory Affairs

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14
Q

What does the Center for Drug Evaluation and Research do?

A

Evaluates and monitors prescription, generic, and OTC drugs.

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15
Q

What does the Center for Biologics Evaluation and Research do?

A

Regulates biologics not reviewed by the CDER (many are reviewed by both)

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16
Q

What does the Office of Regulatory Affairs do?

A

Monitors sites and facilities for drug manufacture

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17
Q

What is preclinical testing and what is its purpose?

A

In vitro and in vivo laboratory animal experiments to evaluate toxicity, pharmacology, and ADME

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18
Q

What is the purpose of an Investigational New Drug application?

A

It allows a drug candidate to become an investigational drug and proceed to human trials after approved

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19
Q

How many drugs that enter phase I will make it to FDA approval?

A

16%

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20
Q

Describe Phase 1 clinical trials

A

20-100 healthy volunteers with gradually increasing doses over the course of a year. The goal is to assess safety and obtain general pharmacokinetic data

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21
Q

Describe Phase 2 clinical trials

A

100-500 patients with the targeted disease/condition. Dosage and route of administration are varied over two years. The goal is to evaluate effectiveness and further check on safety

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22
Q

Describe Phase 3 clinical trials

A

1000-5000 patients that may have some comorbid conditions and is typically a longer study. The goal is to confirm efficacy (that it’s better than the existing options) and safety.

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23
Q

What populations are left out of clinical trials?

A

Pediatric, Geriatric, and Pregnant/Nursing mothers

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24
Q

How long does it take a new drug application o be reviewed?

A

6 months - several years

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25
What are the three phases of drug design?
Discovery, Optimization and Development
26
Describe the discovery phase of drug design
Identification of a pharmacologically active compound (lead compound)
27
Describe the optimization phase of drug design
Modification of the structure of the lead compound to accentuate desired characteristics (selectivity, potency, absorption, metabolism, low toxicity, duration of action, ADME)
28
Describe the development phase of drug design
Developing the formulation taking into account different salt forms, solubility characteristics, binders, fillers, dosage form, ease/cost of preparations, taste/smell, etc
29
What constitutes a drug in the drug development process?
The entire formulation
30
What are two questions that assess how good a drug is going to be?
(1) How well does it access its target? (2) How well does it bind to its target?
31
What are the biochemical classes of targets for drugs? (8)
Enzymes (47%), G-Protein Coupled Receptors (30%), Nuclear Hormone Receptors and Transporters (8%), Ion Channels (7%), Other receptors (4%), miscellaneous (2%), DNA (1%), Integral Membrane Proteins (1%)
32
What are the four general types of bioassays?
Assays using whole organisms, mammalian cell cultures, purified enzymes or receptors, and engineered microorganisms.
33
What are the mechanism dependent types of biological assays?
Assays using purified enzymes or receptors and assays using engineered microorganisms.
34
What are the mechanism independent types of biological assays?
Assays using whole organisms or assays using mammalian cell cultures.
35
What are the cell based types of biological assays?
Assays using mammalian cell cultures or engineered microorganisms.
36
What is high throughput screening?
Automated screening of chemical compounds/mixtures/extracts in relevant bioassays.
37
What constitutes a natural product compound?
If it's purified from plants, microbes, or animals
38
What are the two types of synthetic compounds?
Combinatorial libraries and virtual libraries
39
What is a combinatorial library?
A collection of synthetic compounds made from combinatorial chemistry
40
What is a virtual library?
Any synthetic or natural product compounds modeled on a computer
41
What are the two types of natural products?
Crude extracts and pure compounds
42
What is the benefit of a pure compound?
It offers a great range of structural diversity
43
Define convulation
Separation of the active principle from the inactive components
44
Define dereplication
rapid identification of previously identified bioactive compounds
45
Do synthetic or natural products have greater structural diversity?
Natural products
46
What does 'in silico' mean?
Exclusively by computer
47
What are the four places you can look for compounds?
Natural products, synthetic compound collections, combinatorial libraries, and virtual libraries.
48
Are natural products easy to make synthetically? Why or why not?
No because they're very structurally complex
49
What makes synthetic products easy to manufacture compared to natural products?
They're a lot less complex.
50
What elements do synthetic compounds tend to contain?
Nitrogen, Fluorine, Chlorine
51
How do monomers relate to dimers, trimer, tetramers, pentamers, etc? How is the number of compounds affected?
Monomers are building blocks, dimers are two monomers, trimers are three monomers, tetramers are made of four monomers, pentamers are made of five monomers. For n monomers, there are n^2 dimers, n^3 trimers, n^4 tetramers, and n^5 pentamers.
52
What differences are there if the monomer has two distinct functional groups (like amino acids)?
The products are directional , so XY and YX aren't the same.
53
What is the rigid lock and key model?
Receptors bind molecules and molecules have specific regions (functional groups) important for binding and pharmacological activity
54
What is the induced fit model?
Binding of a substrate to the enzyme induces structural changes in the enzyme so that important amino acid side chains are brought into the correct spatial arrangement for catalysis.
55
What are they six types of chemical bonds covered?
Covalent, ionic, hydrogen, ion-dipole, dipole-dipole, and hydrophobic (van der waals)
56
What dictates the extent of protonation?
The pKa for the individual molecule and the pH of the environment.
57
Define eutomer
The stereoisomer with the highest receptor affinity or activity
58
Define distomer
The stereoisomer with lower receptor affinity or activity
59
Define racemic mixture
A mixture with equal quantities of R and S enantiomers
60
Define enantiomer
Stereoisomers with equal and opposite optical rotations
61
Define diastereomer
Stereoisomers that aren't exact mirror images of one another
62
Define pharmacophore
The three-dimensional arrangement of the essential functional groups necessary to cause a biological response. If the change causes a different biological response, it's a different pharmacophore
63
Define structure - activity relationships
The identification of key portions of the molecule that are important for the imparting optimal biological activity by systematic modification of the structure
64
What are the four approaches to systematically modifying the structure?
Homologation (extending the chain), chain branching, ring transformations, and replacing functional groups with bioisosteres
65
What is the classical definition of isostere?
Molecules or ions with the same number of atoms and/or the same number and arrangement of valance electrons
66
What is the isostere definition extended to biological systems?
Groups of atoms that have chemical and physical similarities producing broadly similar biological properties
67
What are the four categories of classical bioisosteres?
Univalent, Bivalent, Trivalent, and Tetravalent.
68
For ring equivalents, what order can you replace atoms?
Carbon, sulfur, oxygen, nitrogen
69
Define non-classical bioisosteres
Molecules or ions that share similar shapes, volumes, electronic distributions and physiochemical properties that together produce similar biological effects, but their structures do not follow an easily definable set of rules as for classical isosteres
70
What's the difference between isostere and bioisosteres?
They have to retain activity to be bioisosteres
71
What is log P?
Log P is a measure of the lipophilicity of a molecule
72
What is the log P equation?
Log P = log (conc. of drug in octanol / conc. of drug in water)
73
What log P values represent water soluble and insoluble?
A log P value greater than 0.5 are water insoluble, and a value less than 0.5 are water soluble
74
What type of drugs do lipinski's rule of five apply to?
Oral drugs
75
What are lipinski's rule of five?
(1) a molecular weight of under 500 (2) fewer than 10 hydrogen bond acceptors (3) fewer than 5 hydrogen bond donors (4) a C log P value of less than 5

Foundations Exam 1 (2 decks)

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