THREADGILL LECTURES Flashcards

1
Q

Gives 4 therapeutic applications of PARP-1 inhibition

A

1) potentiation of radiotherapy and cytotoxic chemotherapy of cancer
2) reduction of organ damage following ischaemia/reperfusion injury
3) anti inflammatory
4) anti-retro viral

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2
Q

What is PARP essential for?

A

Repair of nucleotide excision repair
Single stranded break repair
And to some extent double stranded breaks

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3
Q

What is O6-alkylguanineO6-alkyl transferase

A

MGMT- suicide enzyme that repairs alkylation/methylation damage at O6 guanine

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4
Q

Name two MGMT inhibitors

A

O6-benzylguanine

Lomeguatrib- patrin-2

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5
Q

What happens to MGMT after its repaired the DNA

A

Adds ubiquitin the hydrolysed (suicide enzyme)

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6
Q

What is PARP-1 structure made up of

A

Binding domain
Auto modification domain
Catalytic domain

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7
Q

What’s contained on the binding domain of PARP-1?

A

2 (3) zinc fingers needed to insert into DNA

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8
Q

How many KDa is MGMT

A

24 - small and soluble

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9
Q

How many KDa is PARP-1?

A

116KDa

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