Chemotherapy biologics Flashcards
What would it mean if a cancer cell displays oestrogen receptors
Their growth is affected by oestrogen. Oestrogen can promote growth of localised cells and metastasised cells
What is Tamoxifen
a SERM (Selective Oestrogen Receptor Modulator)
What does Tamoxifen do
Blocks oestrogen as a selective oestrogen receptor modulation
When is Tamoxifen used
In oestrogen receptor positive (ER+) breast cancer
What is another positive effect of tamoxifen
Prevents bone loss via mineralisation and prevents osteoporosis
What are alternatives to tamoxifen
Aromatase Inhibitors
Mode of action in aromatase inhibitors
In post-menopausal women, they have high levels of androgens. Aromatase converts androgens to oestrogen. Inhibitors reduce the oestrogen load in females. Therefore PREVENTS PERIPHERAL CONVERSION TO OESTROGENS IN POST MENOPAUSAL WOMEN
When are HER2 receptors expressed
In some breast cancers
What are breast cancer patients tested to see if they have a high number of
HER2 receptors
How do HER2 receptors impact the cancer
Tyrosine Kinase is attached to the HER2 receptors. They become (auto)phosphorylated and this signals to the nucleus to form VEGF (which stimulates vessel growth) and COX2 (inflammatory enzyme) and cyclins (involved in the cell cycle). There is the dysregulation of the cell cycle
What gene is the HER2 receptor due to
oncogene
What does the HER2 receptor affect
Gene transcription and cell cycle
What drug targets the HER2 receptor and what does this due in turn
Trastuzumab
-Prevents dysregulation of cell cycle and production of abnormal cells by targeting HER2
What are Epidermal Growth Factor receptor kinases (erlotinib) used for and why
Certain lug and pancreatic cancers
-Because EGF receptor is found in lung and pancreatic cancer cells
What does the EGF receptor do
Promotes proliferation, invasion, angiogenesis and inhibition of apoptosis
How does Erlotinib act
Targets tyrosine kinase so there is prevention of dysregulation of cell
Which chromosome is associated with Chronic Myeloid Leukemia
Philadelphia Chromosome
What is the role of the Ph (Philadelphia) Chromosome
Produces a protein which has tyrosine kinase activity
How is the Philadelphia chromosome formed
There is translocation of two chromosomes
What does tyrosine kinase lead to
Uncontrolled cell proliferation
What drug is Tyrosine Kinase inhibitors used for
Chronic Myeloid Leukemia
What is PARP
Poly (ADP-ribose) polymerase
What is the role of PARP
Enzyme which repairs DNA
What is the BRCA gene important for
Repairing double strand breaks
What is the PARP enzyme important for
Repairs single strand breaks
What does a PARP inhibitor do and what are its consequences
Inhibit PARP
-LEads to inability of cancer cells to repair double strand breaks, leading to cell death
When is PARP good at repairing DNA and what does this mean in terms of treatment
BRCA gene
-If associated with BRCA gene mutation then PARP inhibitors would be of benefit
When are PARP inhibitors used
IN chemoresistant ovarian cancer
What are many ovarian cancers resistant to
Platinum based therapy
What proteins kill cancer cells
Pro-apoptotic factors
What is the action of proteasome inhibitors
Inhibits intracellular proteasomes which alters the regulation of intracellular proteins
What are proteasome inhibitors
Used in multiple myeloma
What is VEGF
Vascular Endothelial Growth Factor
What is VEGF secreted to promote
Angiogenesis
