Term
| DNA Methylation Inhibitors (2) |
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Definition
Azacytidine
Decitabine
Inhibit DNA methylation at cytosine residues by blocking DNA methyltransferases
Treatment of Myelodysplastic syndrome (MDS) |
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Term
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Definition
| Acetylates E-amino groups of lysine residues on histone which reduces histone basicity and expose DNA to transcription factors leading to gene expression |
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Term
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Definition
| Removes acetyl groups from histone E-N-acetylated lysine and restore positive charge and block transcription |
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Term
| Histone Deacetylase inhibitors (2) |
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Definition
1. Vorinostat (SAHA)
Treats Cutaneous T-cell lymphoma (CTCL)
2. Romidepsin
A depsipeptide HDAC inhibitor |
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Term
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Definition
Epidermal growth factor receptor
A type of receptor tyrosine kinase
4 Members: ErbB1 (HER1), ErbB2 (Her2/neu), B3 and B4 |
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Term
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Definition
| A EGFR that is overexpressed in 30% of breast cancers and increased expression of gene correlates with poor prognosis |
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Term
| This antibody targets HER2/neu receptor |
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Definition
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Term
| These 2 antibodies target ErbB1 receptor |
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Definition
1) Cetuximab
2) Panitumumab |
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Term
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Definition
| RTK Inhibitor of ErbB1 receptor overexpressed in LUNG CANCERS |
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Term
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Definition
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Term
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Definition
| dual RTK inhibitor that inhibits both ErbB1 and HER2/neu |
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Term
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Definition
RTK inhibitor associated with PDGF and VEGF and Raf kinase
Treats RENAL CELL CARCINOMA |
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Term
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Definition
RTK inhibitor for treatment of
1) Gastrointestinal stromal tumor (GIST)
2) Renal cell carcinoma
Also inhibit kit kinase |
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Term
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Definition
Vascular endothelial growth factor
Another RTK (Other than EGFR)
Inhibition stops angiogenesis
2 Drugs: Pazopanib (for renal cell carcinoma) and Bevacizumab (Avastin) |
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Term
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Definition
| VEGF receptor inibitor of all 3 isoforms |
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Term
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Definition
| targets VEGF for treatment of glioblastoma |
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Term
| 2 Types of Non-receptor tyrosine kinase inhibitors |
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Definition
1) Abl kinase inhibitors
2) Serine/threonine kinase mTOR inhibitors |
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Term
| Chronic myelogenous leukemia pathophysiology |
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Definition
Due to abnormal chromosome Philadelphia chromosome leading to Constitutively active Abl protein
3 Treatments:
Imatinib (Gleevec)
Nilotinib
Dasatinib |
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Term
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Definition
| First FDA-approved drug targeted to specific molecular defect in a cancer to treat chronic myelogenous leukemia from Philadelphia chromosome |
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Term
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Definition
| Second generation Abl tyrosine kinase inhibitor |
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Term
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Definition
| Second generation Abl kinase inhibitor for resistance to imatinib |
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Term
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Definition
mammalian target of rapamycin
A serine/threonine protein kinase
3 inhibitors:
1) Sirolimus (rapamycin)
2) Temsirolimus
3) Everolimus |
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Term
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Definition
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Term
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Definition
| inhibitor of mTOR approved for treatment of ADVANCED RENAL CELL CARCINOMA |
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Term
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Definition
| mTOR inhibitor for renal cell carcinoma after failure with sunitinib |
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