Week 3: Signal transduction II, RECEPTOR TYROSINE KINASES Flashcards Preview

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Flashcards in Week 3: Signal transduction II, RECEPTOR TYROSINE KINASES Deck (18):
1

T/F: This was the worst lecture that's been given in UMD's 30 year history

True

2

What does BCR-ABL signaling mimic?

growth factor activation

3

What does a mutation in the BCR-ABL pathway cause?

CML

4

Where in the vicinity of the cell is the tyrosine kinase domain located and what is it bound to?

found intracellularly, bound to a ligand binding domain

5

When do receptors typically signal intracellularly?

When they dimerize and are activated by a ligand, but heterodimers with various partners are common

6

What do SH2 domains do?

recognize phospho-tyrosine and connect the RTK phosphorylation events to various "second messengers"

7

How does the signal manifest in terms of cell biology?

modulation of transcription factors

8

What does HIF-alpha sense? What does it do?

low oxygen state; translocates to nucleus and induces hypoxia-inducible genes (VEGF and PDGF)

9

What helps to degrade HIF protein?

Prolyl hydroxylase, vitamin C, alpha-ketoglutarate, O2 via E3 ligase activity

10

How do you block VEGF signaling?

Antibodies to it's receptor, TKIs to block intracellular signaling (inhibition of tyrosine kinase), rapalogues to block Akt/mTOR pathway

11

What are some drugs that are FDA approved to inhibit VEGF-axis?

sorafenib, sunitinib, IFN/bevacizumab, pazaopanib, axitinib

12

What are side effects of VEGFR inhibitors?

cause hypertension, hypothyroidism, loss of hair pigmentation, can cause GI perforation, paricardial effusion, myelosuppression, hepatic toxicity

13

What is unique about HER2?

doesn't contain a binding domain, helps drive proliferation when it dimerizes with EGFR

14

What is trastuzumab used to treat?

antibody to the extracellular domain of Her2 protein

15

What is lapatinib? What does it do?

TKI against HER2, blocks both the EGFR and Her-2

16

What are gefitinib and erlotinib used for?

blocks EGFR or ALK signaling when they are mutated in lung cancers

17

What are side effects of TKIs?

fluid retention, myelosuppression, diarrhea, stomatitis, bowel perforsation

18

What mutation of lung cancers have the highest response rates to TKIs?

ALK mutation in lungs