Target General Infomation
Target ID
T56510
Former ID
TTDC00168
Target Name
Antiapoptotic protein BCL-XL
Gene Name
BCL2L1
Synonyms
Bcl-XL; Bcl2L1; Bcl2like protein 1; Apoptosis regulator Bcl-X; BCL2L1
Target Type
Clinical Trial
Disease Advanced small cell lung cancer; Relapsed or refractory chronic lymphocytic leukemia; Lymphoid malignancies [ICD9: 140-229, 140-239, 162, 162.9, 202, 204.0, 204.1, 208.9; ICD10: C33-C34, C34.90, C81-C86, C91-C95, C91.0, C91.1]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48]
Function
Isoform Bcl-X(S) promotes apoptosis.
BioChemical Class
Bcl-2 family
Target Validation
T56510
UniProt ID
Sequence
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLA
DSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAY
QSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEP
WIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
Structure
1BXL; 1G5J; 1LXL; 1MAZ; 1R2D; 1R2E; 1R2G; 1R2H; 1R2I; 1YSG; 1YSI; 1YSN; 2B48; 2LP8; 2LPC; 2M03; 2M04; 2ME8; 2ME9; 2MEJ; 2O1Y; 2O2M; 2O2N; 2P1L; 2PON; 2YJ1; 2YQ6; 2YQ7; 2YXJ; 3CVA; 3FDL; 3FDM; 3INQ; 3IO8; 3PL7; 3QKD; 3R85; 3SP7; 3SPF; 3WIZ; 3ZK6; 3ZLN; 3ZLO; 3ZLR; 4A1U; 4A1W; 4AQ3; 4BPK; 4C52; 4C5D; 4CIN; 4EHR; 4HNJ; 4IEH; 4TUH; 1BXL; 1G5J; 1LXL; 1MAZ; 1R2D; 1R2E;1R2G; 1R2H; 1R2I; 1YSG; 1YSI; 1YSN; 2B48; 2LP8; 2LPC; 2M03; 2M04; 2ME8; 2ME9; 2MEJ; 2O1Y; 2O2M; 2O2N; 2P1L; 2PON; 2YJ1; 2YQ6; 2YQ7; 2YXJ; 3CVA; 3FDL; 3FDM; 3INQ; 3IO8; 3PL7; 3QKD; 3R85; 3SP7; 3SPF; 3WIZ; 3ZK6; 3ZLN; 3ZLO; 3ZLR; 4A1U; 4A1W; 4AQ3; 4BPK; 4C52; 4C5D; 4CIN; 4EHR; 4HNJ; 4IEH; 4TUH
Drugs and Mode of Action
Drug(s) ABT-263 Drug Info Phase 2 Advanced small cell lung cancer; Relapsed or refractory chronic lymphocytic leukemia; Lymphoid malignancies [543070], [551607]
Obatoclax Drug Info Phase 2 Solid tumours [531104]
Inhibitor 4'-FLUORO-1,1'-BIPHENYL-4-CARBOXYLIC ACID Drug Info [551374]
ABT-263 Drug Info [536702], [536883], [551607]
Obatoclax Drug Info [531104]
WEHI-0103122 Drug Info [543732]
Modulator E-003 Drug Info [543732]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Ras signaling pathway
NF-kappa B signaling pathway
PI3K-Akt signaling pathway
Apoptosis
Jak-STAT signaling pathway
Amyotrophic lateral sclerosis (ALS)
Toxoplasmosis
HTLV-I infection
Pathways in cancer
Transcriptional misregulation in cancer
Pancreatic cancer
Chronic myeloid leukemia
Small cell lung cancer
NetPath Pathway IL2 Signaling Pathway
TGF_beta_Receptor Signaling Pathway
Notch Signaling Pathway
PANTHER Pathway Apoptosis signaling pathway
CCKR signaling map ST
Pathway Interaction Database IL2 signaling events mediated by PI3K
IL3-mediated signaling events
Caspase Cascade in Apoptosis
EPO signaling pathway
IL2 signaling events mediated by STAT5
Reactome BH3-only proteins associate with and inactivate anti-apoptotic BCL-2 members
The NLRP1 inflammasome
WikiPathways IL-6 signaling pathway
IL-3 Signaling Pathway
Nucleotide-binding domain, leucine rich repeat containing receptor (NLR) signaling pathways
Apoptosis
Amyotrophic lateral sclerosis (ALS)
TNF alpha Signaling Pathway
IL-7 Signaling Pathway
Leptin signaling pathway
Intrinsic Pathway for Apoptosis
Apoptosis Modulation and Signaling
References
Ref 531104Phase II study of obatoclax mesylate (GX15-070), a small-molecule BCL-2 family antagonist, for patients with myelofibrosis. Clin Lymphoma Myeloma Leuk. 2010 Aug;10(4):285-9.
Ref 543070(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8319).
Ref 551607Clinical pipeline report, company report or official report of Roche (2009).
Ref 531104Phase II study of obatoclax mesylate (GX15-070), a small-molecule BCL-2 family antagonist, for patients with myelofibrosis. Clin Lymphoma Myeloma Leuk. 2010 Aug;10(4):285-9.
Ref 536702ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor. Cancer Res. 2008 May 1;68(9):3421-8.
Ref 536883ABT-263 and rapamycin act cooperatively to kill lymphoma cells in vitro and in vivo. Mol Cancer Ther. 2008 Oct;7(10):3265-74.
Ref 543732(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2845).
Ref 551374The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
Ref 551607Clinical pipeline report, company report or official report of Roche (2009).