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Neuro 2-Pharmacology week > Drug targets-Konorev > Flashcards

Drug targets-Konorev Flashcards

1
Q

The general name for an enzyme that transfers phosphate groups from ATP to a protein is __

A

Protein kinase

  • Ser-Thr kinases
  • Tyr kinases
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2
Q

The specific DNA sequence a TF binds to is called a ___

A

Response element

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3
Q

___ activates all isoforms of adenylyl cyclas and Src tyrosine kinase

A

Gs

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4
Q

__ inhibits AC but activates tyrosine kinase Src

A

Gi

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5
Q

___ activates PLC

A

Gq

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6
Q

List the steps in the GPCR-cAMP signaling cascade

A

Ligand binds receptor –> Gs activation (active G protein) –> Activate AC –> ATP to cAMP –> Activate PKA –> Activate Phosphorylase kinase –> Activate glycogen phosphorylase

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7
Q

DAG is a lipophilic intermediate that activates ___

A

Protein Kinase C

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8
Q

List the steps in the DAG and IP3 pathway:

A

Ligand binds receptor –> Activate G protein –> Activate PLC –> PIP2 activates DAG and IP3

  • DAG –> PKC
  • IP3 –> Releases Ca –> Ca-CaM complex
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9
Q

The receptors for a group of signaling molecules known as growth factors are often ___

A

Receptor tyrosine kinases

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10
Q

Receptors with RTK transmit the action of a number of ___

A

growth factors

-IGF-1, insulin, EGF, NGF, PDGF

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11
Q

the __ domain of an RTK shows very little similarity between members of the family

the __ domain of an RTK is similar between members of the family

A

ligand-binding

tyrosine kinase

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12
Q

proteins that contain a SRC homology 2 domain (SH2 domain) bind to proteins that have a ___ residue

A

phosphotyrosyl

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13
Q

___ domain binds to the phosphorylated tyrosines

__ domain binds to the proline-rich sequences

A

SH2

SH3

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14
Q

A ras protein is known as a __ GTPase

A

monomeric

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15
Q

list the components of the activation of a monomeric GTPase Ras by growth factors:

GF receptor: ___
Adaptor protein: ___
GEFs: ___
Monomeric GTPase protein: ___

A

RTK

Grb2

SOS

Ras

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16
Q

Point mutations in __ found in 90% of pancreatic adenocarcinomas

Point mutations in __ found in 70% of melanomas

A

Ras

Raf

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17
Q

binding of a NT to this type of receptor directly leads to a change in distribution of ions between extra and IC compartments

A

Ligand-gated ion channel

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18
Q

__ channels are multimeric channels that span the cell membrane and have a binding site for a NT inducing the current, and an ion-conducting pore

A

Ligand-gated

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19
Q

Excitatory NTs open __ channels, depolarize the cell and induce generation of AP in excitable cells

A

cation

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20
Q

Inhibitory NTs open __ channels causing inward flux and hyperpolarization, preventing generation of APs

A

anion

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21
Q

permeability to what ion is increased a result of the activation of a nicotinic receptor?

A

Mostly Na

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22
Q

Nicotinic Ach receptors are generally found where?

A

neuronal and skeletal m. cells

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23
Q

binding of GABA to its cognate receptor ion channel will cause influx of __

A

mostly Cl

24
Q

Transcription factors promote or inhibit the recruitment of ___ to specific genes

What is the defining feature of Transcription factors?

A

RNA polymerase

DNA-binding domain

25
Q

Transcription factors bind to ___regions of DNA that are usually adjacent to the ___ sequence of the regulated gene. The specific DNA sequence they bind to is called the ___

A

Enhancer or promoter

Coding

Response element

26
Q

G-protein binding sites are located where?

A

Cytosol

27
Q

In the DAG and IP3 pathway, what activates these 2?

A

Phosphatidylinositol disphosphate (PIP2)

28
Q

What activates monomeric GTPases?

A

GEFs

29
Q

What inactivates monomeric GTPases by accelerating GTP hydrolysis?

A

GAPs

30
Q

Point mutations in __ are found in 90% of pancreatic adenocarcinomas

A

Ras

31
Q

Point mutations in ___ are found in 70% of melanomas

A

Raf

32
Q

What are examples of the types of drugs that inhibit GF signaling in carcinogenesis?

A

Monoclonal antibodies to GF receptors and their ligands

Multikinase inhibitors

33
Q

JAK is found in which part of the cell?

A

Cytosol

34
Q

Recombinant ligans (HGH, EPO, IFN, and IL-2), receptor antagonists such as pegvisomant (a GH antagonist), and drugs used in allergic and autoimmune disorders target the __ pathway

A

JAK-STAT

35
Q

List some ligands that target nuclear nuclear receptors:

A

Steroids, thyroid hormones, Vit A and D, lipid mediators such as free FAs and their products

36
Q

In the mechanism of a steroid hormone action, binding of a hormone ligand (steroid) causes dissociation of what?

A

hsp90

Binding of steroid causes dissociation of the hsp90 stabilizer and permits conversion to the active configuration

37
Q

___ channel conductance is induced by membrane potential changes and Na, Ca, and K channels are targets of drug action

A

Voltage-gated

38
Q

__ channels are multimeric channels that span the cell membrane and have a binding site for a NT inducing the current, and an ion-conducting pore

A

Ligand-gated

39
Q

__ do not bind NTs directly but are controlled by membrane potential

A

Voltage-gated

40
Q

Local anesthetics (lidocaine), antiarrhythmic drugs (quinidine), and drugs used for tx of epilepsy (phenytoine) act to inhibit __

A

Voltage-gated Na channels

41
Q

__ channels are located on cardiac and smooth muscle cells

A

L-type voltage-gated Ca channels

42
Q

__ are receptors for NTs that have an ion-conducting pore

A

Direct ligand-gated ion channels

43
Q

___ open cation channels, depolarize the cell and induce generation of AP in excitable cells

A

Excitatory NTs

44
Q

List examples of Excitatory NTs

A

Ach and glutamate

45
Q

___ open anion channels causing inward anion flux and hyperpolarization, preventing generation of APs

A

Inhibitory NTs

46
Q

List examples of inhibitory NTs

A

Gaba and glycine

47
Q

Activation of a nicotinic Ach receptor induces inward ___ fluxes and membrane depolarization

A

Na

48
Q

Antagonist drugs used as neuromuscular blockers (Tubocurarine) and partial agonist drugs used for smoking cessation (Verenicline) are examples of this pentameric receptor:

A

Nicotinic Ach receptor

49
Q

GABA-A receptors are anionic channels that cause inward __ influx and hyperpolarization. GABA mediates synaptic inhibition in CNS via these channels

A

Cl

50
Q

This type of receptor is a target for:

  • inhalation general anesthesia drugs (halothane)
  • IV general anesthesia drugs (propofol)
  • ethanol
  • hypnotic and anti-anxiety benzodiazepine drugs (valium)
A

GABA-A

51
Q

Volatile anesthetics and ethanol target the ___ subunit of the GABA-A receptor

Neurosteroids and propofol target the __ subunit of the GABA-A receptor

A

Alpha

Beta

52
Q

Cardiac glycosides target the ___

A

Na pump

53
Q

Thiazide diuretics (chlorothiazide) target the __

A

Na/Cl co-transporter

54
Q

Loop diuretics target the ___

A

Na/K/Cl co-transporter

55
Q

Adrenergic drugs (reserpine) target ___

A

VMAT

56
Q

Adrenomimetic drugs (ephedrine, amphetamines) target __

A

NE transporter

57
Q

Antidepressants (paroxetine) target )))

A

SERT (serotonin/Na symporter)

Neuro 2-Pharmacology week (7 decks)

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