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- NCIT_C173660 IAO_0000115 "A drug-dendrimer conjugate composed of a B-cell lymphoma 2 (Bcl-2)/Bcl-XL inhibitor AZD4320 that is chemically conjugated to a proprietary 5-generation pegylated poly-lysine dendrimer via a hydrolytically labile linker, with potential pro-apoptotic and antineoplastic activities. Upon administration of AZD0466, AZD4320 is released through hydrolytic cleavage of the linker. AZD4320 is a Bcl2-homology domain 3 (BH3) mimetic that specifically binds to and inhibits the activity of the anti-apoptotic proteins Bcl-2 and Bcl-XL. This restores apoptotic processes and inhibits cell proliferation in Bcl-2/Bcl-XL-dependent tumor cells. Bcl-2 and Bcl-XL, proteins belonging to the Bcl-2 family that are overexpressed in many cancers, play an important role in the negative regulation of apoptosis. Their expression in tumors is associated with increased drug resistance and cancer cell survival. The conjugation of AZD 4320 to the dendrimer construct may allow extended release of the agent, which may improve efficacy and lower toxicity." @default.
- NCIT_C173660 NCIT_A32 NCIT_C1909 @default.
- NCIT_C173660 NCIT_A7 NCIT_C18115 @default.
- NCIT_C173660 NCIT_NHC0 "C173660" @default.
- NCIT_C173660 NCIT_P106 "Pharmacologic Substance" @default.
- NCIT_C173660 NCIT_P107 "Dendrimer-conjugated Bcl-2/Bcl-XL Inhibitor AZD0466" @default.
- NCIT_C173660 NCIT_P108 "Dendrimer-conjugated Bcl-2/Bcl-XL Inhibitor AZD0466" @default.
- NCIT_C173660 NCIT_P208 "CL1407404" @default.
- NCIT_C173660 NCIT_P322 "CTRP" @default.
- NCIT_C173660 NCIT_P322 "GDC" @default.
- NCIT_C173660 NCIT_P329 "802253" @default.
- NCIT_C173660 NCIT_P330 "802253" @default.
- NCIT_C173660 NCIT_P375 "Dendrimer-conjugated Bcl-2/Bcl-XL Inhibitor AZD0466" @default.
- NCIT_C173660 NCIT_P399 "802253" @default.
- NCIT_C173660 normalizedInformationContent "100" @default.
- NCIT_C173660 referenceCount "1" @default.
- NCIT_C173660 hasExactSynonym "AZD 0466" @default.
- NCIT_C173660 hasExactSynonym "AZD-0466" @default.
- NCIT_C173660 hasExactSynonym "AZD0466" @default.
- NCIT_C173660 hasExactSynonym "AZD4320-dendrimer Conjugate AZD0466" @default.
- NCIT_C173660 hasExactSynonym "Bcl-2/Bcl-XL Inhibitor-DEP Dendrimer Conjugate AZD0466" @default.
- NCIT_C173660 hasExactSynonym "Bcl-2/Bcl-XL Inhibitor-dendrimer Conjugate AZD0466" @default.
- NCIT_C173660 hasExactSynonym "Dendrimer-conjugated Bcl-2/Bcl-XL Inhibitor AZD0466" @default.
- NCIT_C173660 inSubset NCIT_C116977 @default.
- NCIT_C173660 inSubset NCIT_C116978 @default.
- NCIT_C173660 inSubset NCIT_C128784 @default.
- NCIT_C173660 inSubset NCIT_C157711 @default.
- NCIT_C173660 inSubset NCIT_C157712 @default.
- NCIT_C173660 inSubset NCIT_C176424 @default.
- NCIT_C173660 inSubset NCIT_C177537 @default.
- NCIT_C173660 type Class @default.
- NCIT_C173660 isDefinedBy ncit.owl @default.
- NCIT_C173660 label "Dendrimer-conjugated Bcl-2/Bcl-XL Inhibitor AZD0466" @default.
- NCIT_C173660 subClassOf NCIT_C129839 @default.
- NCIT_C173660 subClassOf NCIT_C159200 @default.
- NCIT_C173660 subClassOf NCIT_C163758 @default.
- NCIT_C173660 subClassOf NCIT_C173660 @default.
- NCIT_C173660 subClassOf NCIT_C1908 @default.
- NCIT_C173660 subClassOf NCIT_C1909 @default.
- NCIT_C173660 subClassOf NCIT_C192025 @default.
- NCIT_C173660 subClassOf NCIT_C274 @default.