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Pharm - 1st Week > Drug Targets - 8/1 Konorev > Flashcards

Drug Targets - 8/1 Konorev Flashcards

1
Q

What are the GPCR ligands?

A 
Biogenic amines (nt's)
Peptides/proteins
Aminoacids (Glu, GABA)
Lipids
Nucleotides (ATP)
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2
Q

What does the Gi family inhibit?

Activates what?

A

Adenylyl cyclase

Tyr Kinase SRC

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3
Q

Gq activates what?

A

PLC

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4
Q

Starting with PLC, describe the downstream pathways:

A

PLC -> PIP2 -> IP3 -> CaM

PLC -> PIP2 -> DAG -> PKC

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5
Q

Name the diff type of RTKs

A

GFs like IGF, VEGF, EGF, NGF, PDGF

And insulin

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6
Q

Insulin is a type of what?

What special structural features does it have?

A

RTK

2 chains alpha and beta linked by a DSB

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7
Q

Ras is considered what?

A

Monomeric GTPase

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8
Q

SH2 domains bind what?

A

Tyrosines

2 Ty

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9
Q

SH3 domains bind what?

A

Proline-rich sequences

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10
Q

GEFs activate what?

Example of 1

A

Monomeric GTPases

Sos

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11
Q

what inactivate monomeric GTPases?

How?

A

GAPs

GTP hydrolysis

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12
Q

What mutation is found in 70% of melanomas?

A

point mutation in Raf

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13
Q

What mutation is found in 90% of pancreatic adenocarcinomas?

A

Point mutation in Ras

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14
Q

Give the signal transduction starting with a GF down to protein expression

A

GF -> RTK -> G-protein -> Raf -> MEK -> ERK -> to nucleus for transcription -> protein expression

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15
Q

What activates the JAK receptors?

A 
GH (somatotropin)
EPO
Leptin
IFN
IL-2 to 10, 15
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16
Q

JAK inhibitors are used in what disorders?

A

Allergic and autoimmune

17
Q

What are nuclear receptors?

A

Steroid and thyroid hormones
Vit D, Vit A
Lipid mediators (FFA)
Steroid receptor

18
Q

How long is the lag period for nuclear receptors?

A

Hours to days

19
Q

What prevents folding into the active conformation of the receptor in the absence of a hormone?

A

Hsp90

20
Q

What drug is used to treat osteoporosis in menopausal women and breast cancer?

A

Tamoxifen

21
Q

What is a nuclear receptor antagonist drug?

A

Spironolactone

22
Q

What is an analog of endogenous ligands as agonists?

A

Levothyroxine

23
Q

Conductance is induced my membrane potential changes describes what?

A

VG-channels

24
Q

What channels play a role in changing the cell membrane potential?

What else do they do?

A

Ion channels

Change the [ ] of ions in cytosol

25
Q

What channels are multimedia and span the cell membrane and have a binding site for a nt inducing the current and an ion-conducting pore?

A

Ligand-gated

26
Q

What are VG channels controlled by?

Do they bind nts directly?

A

Membrane potential

NO

27
Q

What composes VG-Na channels?

A

Alpha and beta subunits

28
Q

Where are L-type Ca channels located?

What type are they?

A

Cardiac and smooth m.

VG

29
Q

What do excitatory nts do?

Examples?

A

Open cation channels, depolarize the cell and generate AP

ACh
Glutamate

30
Q

What do inhibitory nts do?

Examples?

A

Open anion channel causing hyperpolarization, prevent APs

GABA
Glycine

31
Q

Activation of Nicotinic ACh receptors causes what?

Located where?

What structure?

A

Inward Na+ flux and membrane depolarization

Skeletal m. And neuronal cells

Pentameric (2a, 1b, 1 gamma, 1 delta)

32
Q

The Nicotinic ACh receptor is what?

A

Ligand-gate ion channel

33
Q

Where does ACh bind to the Nicotinic receptor?

A

Alpha subunit

34
Q

GABA receptor activation causes an inward flux in what ion?

Mediates what, where?

A

Cl-

Synaptic inhibition in CNS

35
Q

What structure of GABA receptor?

A

Pentameric

36
Q

Examples of GABA drugs?

A

Halothane
Proposal
Valium

37
Q

What are examples of peptides/proteins?

A

ACTH
Angiotensin
Bradykinin
Opioids

38
Q

What are examples of Lipids?

A

LTKs
Prostacyclin
TxA2

39
Q

What are the Biogenic amines?

A 
ACh
Epi
NE
Dopamine
Serotonin
Histamine

Pharm - 1st Week (4 decks)

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