L14 - rational treatment of cancer Flashcards

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1
Q

What are some examples of rational cancer treatment strategies?

A

Induce differentiation, discourage proliferative signalling, promote apop signalling, exploit checkpoint vulnerability, identify relevant population for specific strategy

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2
Q

How are gene expression arrays uses to stratify cancers?

A

Analyse g.e. in particular cancers and identify expression/downreg of particular genes associated with low survival - target these genes

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3
Q

What is one way of targetting acute pro-myelocytic leukaemia?

A

Exploit differentiation by treating with all trans retinoic acid or arsenic trioxide. Recruits ubiq ligase to destroy the fusion protein (normally it would force differentiation)

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4
Q

Why are tumour suppressor genes difficult to target?

A

They are not normally present - LOH

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5
Q

What is druggability?

A

Whether or not the target protein has a defined structure that specifically binds low molecular weight chemical entities

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6
Q

The structure a drug binds to is usually a cavity with what properties?

A

Vulnerable to low MW compounds that inhibit function of the cavity and disrupts catalytic activity
Provides lots of points of contact for drug - more potent and more specificity

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7
Q

What is an undruggable target?

A

TF oncogenes e.g. c-myc and fos

DNA binding cleft is similar between TF therefor not sufficiently specific

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8
Q

What are the pros and cons of kinases are cancer drug targets?

A
PROS
- many are oncogenes 
- 518 in genome 
- very druggable (ATP sub binding cleft)
CONS
- many have same common ancestor - not sufficient variation that allows dev of specific inhibitors
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9
Q

How can we exploit checkpoint vulnerability?

A

Normal cells stop cc and initiate DNA repair when DNA is damaged. Cancer cells lack this machinery so they can’t repair the damage - this puts the cell at risk of mitotic catastrophes after a few rounds of replication

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