Drug name: DZNeP + Gemcitabine

Cas.no	PubChem ID
102052-95-9	73087

Known Target
Histone-lysine N-methyltransferase EZH2	Q15910
Structure
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Introduction
3-Deazaneplanocin A (DZNep) is an S-Adenosylhomocysteine Hydrolase inhibitor and histone methyltransferase EZH2 inhibitor. It switches on repressed tumor suppressor genes and induces apoptosis by inhibiting the expression of EZH2. Studies have shown that it acts as an anti-cancer drug with effectiveness against a variety of different tumour types.

Cas.no	PubChem ID
95058-81-4	60750

Known Target
DNA
Ribonucleoside-diphosphate reductase large subunit	P23921
Thymidylate synthase	P04818
UMP-CMP kinase	P30085
Structure
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Introduction
Gemcitabine is a nucleoside analog used as chemotherapy. As with fluorouracil and other analogues of pyrimidines, the drug replaces one of the building blocks of nucleic acids, in this case cytidine, during DNA replication. The process arrests tumor growth, as new nucleosides cannot be attached to the “faulty” nucleoside, resulting in apoptosis (cellular “suicide”). It is used in various carcinomas: non-small cell lung cancer, pancreatic cancer, bladder cancer and breast cancer. It is being investigated for use in oesophageal cancer, and is used experimentally in lymphomas and various other tumor types.

• [1] Molecular mechanisms involved in the synergistic interaction of the EZH2 inhibitor 3-deazaneplanocin A with gemcitabine in pancreatic cancer cells. Avan, A., et al. (2012).Mol Cancer Ther.11(8):1735-46.
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