NOTHING IS REAL! EXAM 1 REVIEW Flashcards

1
Q

Antigens are recognized with high affinity by antibodies because

A

the sequences of three hypervariable loops are selected in an immune response to exquisitely complement the 3D shape of the antigen.

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2
Q

kcat is what type of parameter?

A

Kinetic rate constant independent of enzyme or substrate concentration

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3
Q

Change in Km

A

noncompetitive (mixed)

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4
Q

Change in Km and Vmax

A

uncompetitive

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5
Q

change Vmax

A

competitive

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6
Q

The assigned reading “Therapeutic monoclonal antibodies,” describes several types of engineered antibody molecules that have been developed for therapeutics. Which of the names below DOES refer to a type of therapeutic monoclonal antibody?

A

Fab, BiTE, scFv

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7
Q

Twelve domains compose an IgG molecule. Of these domains,

A

all have two or more cysteine residues.

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8
Q

Ig chains

A

4: 2 heavy 2 light

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9
Q

Ig fold (Domain)

A

-sandwich of 2 antiparallel B-sheets
-disulfide bond linkage
-hydrophobic residues
-connected to each other by loops = flexible

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10
Q

Substrate enzyme interactions

A

-hydrophobic to hydrophobic
-H bonding
-coloumbic

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11
Q

KI

A

-dissociation constant
-analogous to KD
-low=more affinity

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12
Q

Cheng-Prusoff

A

relationship btw Ki and IC50

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13
Q

The development of an allosteric drug is attractive because

A

it is possible to consider ACTIVATING an enzyme target in treating a disease.

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14
Q

Darunavir

A

interacts with polypeptide backbone and catalytic asp residues from each subunit of HIV protease

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15
Q

The basis for selectivity of certain NSAIDS, such as celecoxib, for COX-2 over COX-1 is

A

the spatial complementarity between the inhibitor and COX-1 is poor

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16
Q

HIV protease

A

-homodimer
-heme group
-aspartic

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17
Q

Aspirin vs everything else on COX

A

acetylates SERINE residue near active site to block access

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18
Q

Mech-based inhibitors

A

-2-thioxanthines on MPO

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19
Q

TX2 on MPO

A

covalently bonded to heme via thioether bond

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20
Q

NSAIDs

A

block prostaglandin

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21
Q

COX-2 vs COX-1

A

small Valine residue
steric hinderance

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22
Q

Allosteric inhibitor kinetics

A

typically mixed

23
Q

Allosteric inhibition

A

increase Km

24
Q

Cytochrome inhibitor

A

-increase bioavailability/plasma levels of drug
-drug more potent

25
Q

CYP3A4

A

-monoxygenase
-membrane bound
-activity and dosing of drugs

26
Q

cytochrome catalytic activity

A

-insertion of OH from O2
-metabolism of fatty acids
-produce vitamin A and D
-detoxification

27
Q

G is positive

A

NEED energy

28
Q

SLC transporters

A

-large family
-most bio substrates
-NO energy

29
Q

electrochemical transporters

A

-SLC (uni,sym,antiport)

30
Q

SLC2

A

-glucose by uniport

31
Q

SGLT (SLC5)

A

Na+/glucose
-Na+ provides energy to move glucose across gradient
-SYMPORT

32
Q

ATP hydrolysis

A

-P-type (Na/K+ ATPase)
-ABC

33
Q

ABC

A

-energy
-lipids
-P-glycoprotein

34
Q

P-glycoprotein

A

hydrolysis of ATP drives NBDs apart and converts TMDs back

35
Q

The A-form DNA helix

A

often occurs in formation of DNA-RNA hybrid helix.

36
Q

B-DNA

A

-longer
-skinnier
-smaller diameter
-C’2 endo
-bigger pitch and twist

37
Q

B-form major groove

A

wider and shallower
-highly accessible

38
Q

Intercalators

A

-mod DNA locally
-mutagens
-stretch base pairs apart
-TOTO
-small molecules in mostly minor grooves

39
Q

positive supercoiling

A

-left
-overwound
-hard to unwind good for bad condititons

40
Q

topologically strained DNA

A

greater activity for transcription etc

41
Q

TOP 1

A
  1. cuts one strand
  2. controlled rotation
  3. re-ligate
    -NO ENERGY
    -REMOVES supercoiling
42
Q

TOP 2

A
  1. Cuts both strands
  2. Moves other strand through opening in cut strand
  3. re-ligate
    -LK change by 2
    -gyrase (adds negative)
    -NEEDS ENERGY
43
Q

TOP inhibitors

A

-trap complex of enzyme + DNA
-inhibit re-ligation
-topotecan and irinotecan

44
Q

Nucleosome

A

DNA wrapped around histone octamer

45
Q

Energy required to deform DNA

A

from electrostatic interactions between DNA backbone and histone side chains

46
Q

HTH

A

-2 helices w short turn
-second helix binds major groove
-first helix stabilizes

47
Q

Zinc Fingers

A

-a-helix binds
-ALSO recognizes RNA
-4 cys or 2 cys+2his
-tandem

48
Q

bZIP

A

-leucine every 7th a-helix
-dimers
-arg and lys basic region binds major groove
-phosphate baxkbone and H bonding

49
Q

HLH

A

-2 a-helix connected by loop
-4helix dimer
-extension of one a-helix binds major groove

50
Q

CREB domains

A

-DBD (bzip): binding
-Activation domain (Q1 and2): interact with TFs
-protein interaction domain (KID): histone acetyltransferases

51
Q

TBP TATA binding protein

A

B-sheet
-MINOR GROOVE
-bends TATA box
-binding directs assembly of initiation complex

52
Q

Steroid nuclear receptors

A

-bind steroid then bind to DNA to activate transcription
-DBD-hinge-LBD