Drug name: Rapamycin + Gemcitabine


Related CSCTT Targets

Gastric cancer SP cells [ref.1]

Rapamycin

Cas.no PubChem ID
53123-88-9 5284616
Known Target
Serine/threonine-protein kinase mTORP42345
Peptidyl-prolyl cis-trans isomerase FKBP1AP62942
Fibroblast growth factor 2P09038
Structure
...
Introduction
Rapamycin was used as a kind of original antifungal antibiotic, which is produced by Streptomyces hygroscopicus. Now it has been used in the prevention of transplant rejection because of its immunosuppressive effect. It also exhibits activity against several transplantable tumors and slightly activity to inactive against leukemias. The immunosuppressive effect of Rapamycin is exerted by inhibiting the activation and proliferation of T cells. Rapamycin binds to FK-binding protein 12 (FKBP12) and forms the rapamycin-FKBP12 complex, which regulates an enzyme that plays an important role in the progression of the cell cycle. Rapamycin was confirm to be the inhibitor of mTOR.

Gemcitabine

Cas.no PubChem ID
95058-81-4 60750
Known Target
DNA
Ribonucleoside-diphosphate reductase large subunitP23921
Thymidylate synthaseP04818
UMP-CMP kinaseP30085
Structure
...
Introduction
Gemcitabine is a nucleoside analog used as chemotherapy. It is marketed as Gemzar® by Eli Lilly and Company. 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”). Gemcitabine 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.

Reference

  • [1] A c-Met inhibitor increases the chemosensitivity of cancer stem cells to the irinotecan in gastric carcinoma. Yashiro, M., et al. (2013).Br J Cancer. 109(10):2619-28.
    24129235. [ 24129235 ]

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