EGFR signalling And Cancer Flashcards

1
Q

What do ERbB receptors undergo?

A

Autophosphorylation

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2
Q

EGFR signal transduction

A
GRB2
SOS
RAS
RAF
MEK
MAPK
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3
Q

3 ways EGFR enters cells

A

Clathrin dep endocytosis
Clathrin indep endocytosis
Secretase cleavage

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4
Q

3 ways EGFR signalling is enhanced

A

Increase in amount of ligand available for binding
Cross talk between receptors
Heterodimerisation with other members of HER family

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5
Q

How many RTKs in mammals?

A

58

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6
Q

How many subfamilies of RTKs?

A

20

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7
Q

Regions of RTK

A

Variable extra cellular region

Well conserved TK region

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8
Q

RTK mutation in cancer -percentage

A

30%

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9
Q

EGFR main biological function

A

Epithelial development

Neuronal differentiation

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10
Q

cKit main biological function

A

Haematopoiesis

Mast cell development

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11
Q

HGFR role

A

Placenta, liver and muscle development

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12
Q

RET role

A

Kidney and neuronal differentiation

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13
Q

How many percent of human cancers have overexpressed EGFR?

A

50%

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14
Q

5 results of overexpressed EGFR in cancer

A
Dedifferentiation
Angiogenesis
Metastasis
Cell proliferation
Survival and protection from apoptosis
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15
Q

Which antibody blocks ligand binding to EGFR?

A

Cetuximab

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16
Q

2 antibodies blocking dimerisation of ErbB2

A

Pertuzumab

Trastuzumab

17
Q

What are the majority of TKI?

A

ATP mimetic

18
Q

2 EGFR specific TKI;

A

Gefitinib

Erlotinib

19
Q

A EGFR/ERbB2 inhibitor

A

Lapatinib

20
Q

Direct action of mAB cancer therapy 2

A

Block cell cycle progression, antiangiogenic, internalising receptors

Conjugation with toxins

21
Q

Indirect action of mAB cancer therapy

A

Immune system cytotoxicity

Ab dep cellular cytotoxicity

22
Q

What does imatinib do?

A

Small molecule inactivating kinase activity of BCR-abl and multi targeted inhibitor of KIT and PDGFA, PDGFB