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- NCIT_C179922 IAO_0000115 "An anti-apoptotic protein B-cell lymphoma-extra large (Bcl-XL) targeted protein degrader, using the proteolysis targeting chimera (PROTAC) technology, with potential pro-apoptotic, immunomodulating and antineoplastic activities. DT2216 is composed of a Bcl-XL ligand attached to a Von Hippel-Lindau (VHL) E3 ligase ligand. Upon administration of DT2216, the Bcl-XL binding moiety specifically targets and binds to Bcl-XL which is expressed on tumor-infiltrating regulatory T-cells (Tregs) in the tumor microenvironment (TME) and cancer cells that are dependent on Bcl-XL for their survival, such as certain Bcl-XL-dependent T-cell malignancies. In turn, the VHL E3 ligase ligand is recruited to the endoplasmic reticulum (ER) and Bcl-XL is tagged by ubiquitin. This causes ubiquitination and proteasome-mediated degradation of Bcl-XL. The degradation of Bcl-XL leads to an inhibition of the anti-apoptotic activity of Bcl-XL and restores apoptotic processes in and causes depletion of Bcl-XL-expressing Tregs and Bcl-XL-dependent cancer cells. Reduction of Tregs may activate anti-tumor CD8-positive-mediated immune responses. This leads to the inhibition of tumor growth. Bcl-XL, a protein belonging to the Bcl-2 family, plays an important role in the negative regulation of apoptosis. Their expression in tumors is associated with increased Tregs survival. Tregs play a key role in cancer progression and tumor immunosuppression. Compared to other Bcl-XL inhibitors, DT2216 does not cause platelet toxicity as the VHL E3 ligase is not highly expressed in platelets." @default.
- NCIT_C179922 NCIT_A7 NCIT_C17698 @default.
- NCIT_C179922 NCIT_NHC0 "C179922" @default.
- NCIT_C179922 NCIT_P106 "Pharmacologic Substance" @default.
- NCIT_C179922 NCIT_P107 "Bcl-XL Proteolysis Targeting Chimera DT2216" @default.
- NCIT_C179922 NCIT_P108 "Bcl-XL Proteolysis Targeting Chimera DT2216" @default.
- NCIT_C179922 NCIT_P208 "CL1662636" @default.
- NCIT_C179922 NCIT_P322 "CTRP" @default.
- NCIT_C179922 NCIT_P322 "GDC" @default.
- NCIT_C179922 NCIT_P399 "805721" @default.
- NCIT_C179922 normalizedInformationContent "100" @default.
- NCIT_C179922 referenceCount "1" @default.
- NCIT_C179922 hasExactSynonym "APTaD DT2216" @default.
- NCIT_C179922 hasExactSynonym "Antiapoptotic Protein Targeted Degrader DT2216" @default.
- NCIT_C179922 hasExactSynonym "BCL-XL-specific PROTAC DT2216" @default.
- NCIT_C179922 hasExactSynonym "Bcl-XL Degrader DT2216" @default.
- NCIT_C179922 hasExactSynonym "Bcl-XL PROTAC DT2216" @default.
- NCIT_C179922 hasExactSynonym "Bcl-XL Proteolysis Targeting Chimera DT2216" @default.
- NCIT_C179922 hasExactSynonym "DT 2216" @default.
- NCIT_C179922 hasExactSynonym "DT-2216" @default.
- NCIT_C179922 hasExactSynonym "DT2216" @default.
- NCIT_C179922 hasExactSynonym "PROTAC Bcl-XL Deagrader DT2216" @default.
- NCIT_C179922 hasExactSynonym "PROTAC DT2216" @default.
- NCIT_C179922 hasExactSynonym "Proteolysis-targeting Chimera Protein Degrader DT2216" @default.
- NCIT_C179922 inSubset NCIT_C116977 @default.
- NCIT_C179922 inSubset NCIT_C116978 @default.
- NCIT_C179922 inSubset NCIT_C128784 @default.
- NCIT_C179922 inSubset NCIT_C157711 @default.
- NCIT_C179922 inSubset NCIT_C157712 @default.
- NCIT_C179922 inSubset NCIT_C176424 @default.
- NCIT_C179922 type Class @default.
- NCIT_C179922 isDefinedBy ncit.owl @default.
- NCIT_C179922 label "Bcl-XL Proteolysis Targeting Chimera DT2216" @default.
- NCIT_C179922 subClassOf NCIT_C129839 @default.
- NCIT_C179922 subClassOf NCIT_C159200 @default.
- NCIT_C179922 subClassOf NCIT_C163758 @default.
- NCIT_C179922 subClassOf NCIT_C179922 @default.
- NCIT_C179922 subClassOf NCIT_C1908 @default.
- NCIT_C179922 subClassOf NCIT_C1909 @default.
- NCIT_C179922 subClassOf NCIT_C192025 @default.
- NCIT_C179922 subClassOf NCIT_C274 @default.