Dr Paul Reynolds
the strategy with all of them is to inhibit DNA polymerisation, whether that is by inputting a base pair mutation to cause cell death by apoptosis or if it is to do any of the functions listed belo on the tables it basically wants to kill the tumour cells and the tumour cells and undergoing uncontrolled proliferation so it will go to any extent to interfere with proliferation!!
BELOW
| its been put twice one down below ahhh | mechanisms of action | Plant derivatives | mechanisms of action |
|---|---|---|---|
| Anthracyclines | act to inhibit DNA & RNA Polymerisation by binding to DNA. It also acts as an inhibitor of tropoisomerase II which usually helps a cell proliferate | vinca alkaloids | bind tubulin and prevent polymerisation into microtubules |
| Dactinomycin | Interferes with movement of RNA polymerase along genes, preventing transcription. it also has evidence to suggest it acts as an inhibitor of topoisomerase II | Taxanes | microtubule inhibiting agent |
| Bleomycin | Effective in G2 phase and mitosis it is also active against non-dividing cells | camptothecins | bind to and inhibit topoisomerase I |
| Mitomycin | cross links DNA and may degrade DNA through generation of free radicals | Etoposides | inhibits mitochondrial function, tropoisomerase II and nucleoside transport |
| Alkylating agents | example | mechanism of action | cancer uses (not all had a specification) | ||
|---|---|---|---|---|---|
| Nitrogen mustards | cyclophosphamide | Intrastrand crosslinking | |||
| of DNA | |||||
| Ethylenimines | Thiotepa | Intrastrand crosslinking | |||
| of DNA | |||||
| Alkylsulphonates | Busulphan | Intrastrand crosslinking | |||
| of DNA | It is used in chronic | ||||
| granulocytic leukaemia. | |||||
| Hydrazines and Triazines | Temozolomide | Intrastrand crosslinking | |||
| of DNA | |||||
| Nitrosoureas | carmustine | Intrastrand crosslinking | |||
| of DNA | may be used against tumours of | ||||
| the brain and meninges | |||||
| Platinum based compounds | cisplatin | results in local denaturation of the DNA chain BY CAUSING intrastrand cross-linking which inhibits DNA separation |
| Cytotoxic antibiotics | mechanism of action |
|---|---|
| Anthracyclines | It binds to DNA and inhibits both DNA andRNA synthesis the main one is doxorubicin |
| Dactinomycin | interfering with the movement |
| of RNA polymerase along the gene and thus | |
| preventing transcription. it also has an inhibitory affect on topoisomerase II | |
| Bleomycin | effective at stopping proliferation of cells at G2 and mitosis |
| Mitomycin | It cross-links DNA and may also degrade DNA |
| through the generation of free radicals. |
| Antimetabolites | example | mechanism of action |
|---|---|---|
| Antifolates | methotrexate | This inhibits DNA polymerase. |
| Antipyrimidines | 5-FU | inhibits |
| DNA polymerase | ||
| Antipurines | mercaptopurine | inhibits |
| DNA polymerase |
To recognize the clinical context in which particular drugs are used.
To identify the major side effects of these drugs
side effects include the following….