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Cisplatin's Effect on Humans

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Submitted By dodgypie
Words 284
Pages 2
Drug/small molecule:
Cisplastin

Chemical scaffold/structure:

Target ? Is target used as a Biomarker ? In what tumour type?:
Solid tumours. It’s primary target is DNA.

Proposed mech. of action:
It has a cytotoxic mode of action, it’s primary target is DNA. However it is not fully understood how it works and gaps remain.
It inhibits DNA synthesis, suppresses RNA transcription and induces apoptosis.

Cisplatin binds to DNA which inhiobits replication and transcription of DNA leading to programmed cell death, apoptosis.
Cisplatin coordinates to DNA mainly through certain nitrogen atoms of the DNA base pairs; these nitrogen atoms (specifically, the N7 atoms of purines) are free to coordinate to cisplatin because they do not form hydrogen bonds with any other DNA bases
Cisplatin-DNA complexes are known as abbucts. Most important one is where two chlorine ligands of cisplatin are replaced by purine nitrogen atoms on adjacent bases on the same strand of DNA. Purine bases most commonly found here us guanines, however abbucts involving one guanine and one adenine are also found. The formation of these adducts causes the purines to become destacked and the DNA helix to become kinked. which activate several signal transduction pathways, including those involving ATR, p53, p73, and MAPK
Damaged DNA elicits DNA repair mechanisms, one of which is apoptosis when repair proves too difficult
Effects of drug in cells and animal models?:

Any non-specific or ‘off-target’ effects?:
Loss of fertility, loss of appetite, numbness or tingling, loss of rate. In high doses can prove

Approved or in trials?
Approved, discovered in the 1960s. Used in combination therapies?
Can be used with etoposide in luing cancer
In your opinion is it a ‘good’ or ‘bad’ drug?

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