Drug Targets Ch 1 Flashcards

1
Q

What type of cells do humans, animals, and plants have?

A

Eukaryotic

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2
Q

Nucleus

A

Contains the genetic blueprint (DNA).

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3
Q

Cytoplasm

A

Fluid content of the cell.

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4
Q

Organelle

A

Structures within the cell.

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5
Q

Mitochondria

A

Produce energy.

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6
Q

Ribosomes

A

Protein factories.

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7
Q

Rough Endoplasmic Reticulum

A

Location of protein synthesis for secretion.

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8
Q

Cell membrane components

A

Fluid mosaic phospholipid bilayer with hydrophobic interior studded with proteins (including glycoproteins that act as carriers or channels).

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9
Q

Phospholipid structure

A

Polar head group and two hydrophobic tails.

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10
Q

Drug target for lipids

A

Cell membrane lipids

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11
Q

Drug targets for protein (4)

A

Receptors
Enzymes
Carrier proteins
Structural proteins

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12
Q

Drug targets for nucleic acids

A

RNA, DNA

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13
Q

Drug targets for carbohydrates

A

Cell surface carbohydrates

Antigens and recognition molecules

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14
Q

Drug targets are usually ____________.

A

macromolecules

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15
Q

Drugs usually bind to _________ _______ , which are usually _________ pockets on the surface of the macromolecule, of target via ______________ _________ and exist in ___________ between bound and unbound states.

A

binding site, hydrophobic, intermolecular interactions, equilibrium

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16
Q

Binding groups

A

Functional groups on the drugs that participate in binding interactions.

17
Q

Binding regions

A

Specific regions within the binding site that are involved in binding interactions.

18
Q

Induced fit

A

Change in shape of binding site and drug producing a pharmacological effect.

19
Q

What is the strongest weak molecular interaction and in what condition is it strongest? What weakens the interaction?

A

Electrostatic/ionic bond (separation between two atoms with opposite formal charges) is strongest (20-40 kJ/mol). Strongest in hydrophobic environment. Weaken by distance.

20
Q

What is the second strongest intermolecular interaction? When is it strongest?

A

Hydrogen bonds (between electron deficient hydrogen and electron rich heteroatom). Strongest when atoms’ orbitals are lined up in 180 degree line.

21
Q

HBD

A

Hydrogen Bond Donor-Electron deficient hydrogen atom (usually bonded to a N or O).

22
Q

HBA

A

Hydrogen Bond Acceptor- electron rich heteroatom (usually N or O).

23
Q

Carboxylate ion, phosphate ion, tertiary amine are (good, moderate, poor) HBD or HBAs?

A

Good HBAs

24
Q

Carboxylic acid, amide oxygen, ketone, ester, ether, and alcohol are (good, moderate, poor) HBD or HBAs?

A

Moderate HBAs

25
Q

Sulfur, fluorine, chlorine, aromatic ring, amide nitrogen, and aromatic amine are (good, moderate, poor) HBD or HBAs?

A

Poor HBAs

26
Q

Primary ammonium ion is a (good, moderate, poor) HBD or HBAs?

A

Good HBD

27
Q

What is the weakest intermolecular interaction? What weakens this force significantly?

A

Van der Waals (transient areas of low and high electron density leading to temporary dipoles in hydrophobic areas). Distance weakens van der Waals.

28
Q

Dipole-dipole interactions.What weakens it?

A

Weak intermolecular interactions (between permanent dipole moments). Incorrect positioning of groups and distance (less significantly than van der Waals but more significantly than ionic bonds) weakens.

29
Q

Ion-dipole interaction: how strong is it and what is the effect of distance on it?

A

Between molecule with formal charge and one with permanent dipole moment. It is stronger than dipole-dipole. Distance weakens the bond, but less than in dipole-dipole.

30
Q

Induced Dipole Interactions (Example)

A

Formal charge of one molecule induces a charge in another (Quaternary ammonium ion and aromatic ring).

31
Q

Desolvation Penalties (enthalpy and entropy)

A

Enthalpy: energy released by binding must be greater than energy released by solvation.
Entropy: hydrophobic forces increase disorder of water

32
Q

Amphotericin B

A

Antifungal agent that builds hyrdophillic tunnels in the cell membrane draining cell.

33
Q

Therapeutic index

A

Ratio of dosage causing toxic effect to dosage causing max therapeutic effect. Higher means safer.

34
Q

Selective toxicity

A

Harmful to only some cell types.

35
Q

Pharmacodynamics

A

Study of how a drug binds to its target molecule.

36
Q

Pharmacokinetics

A

Study of how a drug is absorbed, distributed, and metabolized.