DGIdb - XIAP Gene Record

XIAP 331 Druggable GenomeClinically Actionable

Alternate Names:

331
X-LINKED INHIBITOR OF APOPTOSIS
XIAP
API3
BIRC4
IAP-3
ILP1
MIHA
XLP2
hIAP-3
hIAP3
300079
592
ENSG00000101966
OTTHUMG00000022336
X-LINKED INHIBITOR OF APOPTOSIS PROTEIN
P98170
BE0001156
2790
PA25361
T16769
E3 ubiquitin-protein ligase XIAP
NM_001167
NP_001158

Gene Info:

Target Class	Miscellaneous
Target Subclass	Inhibitor of apoptosis
Gene Biotype	PROTEIN_CODING
GuideToPharmacology Gene Category Name	Inhibitors of apoptosis (IAP) protein family
GuideToPharmacology Gene Category ID	889

(11 More Sources)

Gene Categories: Category Details

KINASE
PROTEASE INHIBITOR
DRUGGABLE GENOME
CLINICALLY ACTIONABLE
ENZYME

Publications:

Chow et al., 2003, Synergistic effects of chemotherapeutic drugs in lymphoma cells are associated with down-regulation of inhibitor of apoptosis proteins (IAPs), prostate-apoptosis-response-gene 4 (Par-4), death-associated protein (Daxx) and with enforced caspase activation., Biochem. Pharmacol.
Duechler et al., 2005, In vitro cytotoxic effect of proteasome inhibitor bortezomib in combination with purine nucleoside analogues on chronic lymphocytic leukaemia cells., Eur. J. Haematol.
Liu N et al., 2014, Debio 1143, an antagonist of multiple inhibitor-of-apoptosis proteins, activates apoptosis and enhances radiosensitization of non-small cell lung cancer cells in vitro., Am J Cancer Res
Porosnicu et al., 2001, Co-treatment with As2O3 enhances selective cytotoxic effects of STI-571 against Brc-Abl-positive acute leukemia cells., Leukemia
Nimmanapalli et al., 2001, Cotreatment with STI-571 enhances tumor necrosis factor alpha-related apoptosis-inducing ligand (TRAIL or apo-2L)-induced apoptosis of Bcr-Abl-positive human acute leukemia cells., Clin. Cancer Res.
Sun H et al., 2011, Potent bivalent Smac mimetics: effect of the linker on binding to inhibitor of apoptosis proteins (IAPs) and anticancer activity., J Med Chem
Vaziri et al., c-IAP1 is overexpressed in HL-60 cells selected for doxorubicin resistance: effects on etoposide-induced apoptosis., Anticancer Res.
Li et al., 2001, Human ovarian cancer and cisplatin resistance: possible role of inhibitor of apoptosis proteins., Endocrinology
Nomura et al., Cisplatin inhibits the expression of X-linked inhibitor of apoptosis protein in human LNCaP cells., Urol. Oncol.
Maggio et al., 2004, The histone deacetylase inhibitor MS-275 interacts synergistically with fludarabine to induce apoptosis in human leukemia cells., Cancer Res.
Alas et al., 2002, Rituximab modifies the cisplatin-mitochondrial signaling pathway, resulting in apoptosis in cisplatin-resistant non-Hodgkin's lymphoma., Clin. Cancer Res.
Kitada et al., 2000, Protein kinase inhibitors flavopiridol and 7-hydroxy-staurosporine down-regulate antiapoptosis proteins in B-cell chronic lymphocytic leukemia., Blood
Gao et al., 2004, Contribution of disruption of the nuclear factor-kappaB pathway to induction of apoptosis in human leukemia cells by histone deacetylase inhibitors and flavopiridol., Mol. Pharmacol.
Motwani et al., 2001, Augmentation of apoptosis and tumor regression by flavopiridol in the presence of CPT-11 in Hct116 colon cancer monolayers and xenografts., Clin. Cancer Res.
Piva et al., 2005, 15-Deoxy-delta 12,14-prostaglandin J2 induces apoptosis in human malignant B cells: an effect associated with inhibition of NF-kappa B activity and down-regulation of antiapoptotic proteins., Blood
Jazirehi et al., 2001, Adriamycin sensitizes the adriamycin-resistant 8226/Dox40 human multiple myeloma cells to Apo2L/tumor necrosis factor-related apoptosis-inducing ligand-mediated (TRAIL) apoptosis., Clin. Cancer Res.
Jia et al., 2003, Synergistic antileukemic interactions between 17-AAG and UCN-01 involve interruption of RAF/MEK- and AKT-related pathways., Blood
Shankar et al., 2004, UCN-01 alters phosphorylation of Akt and GSK3beta and induces apoptosis in six independent human neuroblastoma cell lines., J. Neurochem.
Orzáez M et al., 2011, Characterization of dequalinium as a XIAP antagonist that targets the BIR2 domain., Apoptosis
Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

CHEMBL1230662 XIAP

Interaction Score: 9.47

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10592235 17139284 17016423

Sources:
DrugBank
CHEMBL1230661 XIAP

Interaction Score: 2.37

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DrugBank
BIRINAPANT XIAP

Interaction Score: 2.37

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Notes

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
TTD TALC GuideToPharmacology
CHEMBL481422 XIAP

Interaction Score: 2.37

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
21462933

Sources:
DTC GuideToPharmacology
GDC-0917 XIAP

Interaction Score: 2.37

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Novel Target

Trial Name CUDC-427

PMIDs:
None found

Sources:
TdgClinicalTrial
AT-406 XIAP

Interaction Score: 2.37

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
25520882

Sources:
TTD TALC GuideToPharmacology
LCL-161 XIAP

Interaction Score: 1.58

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Notes

Details of the Assay for Interaction Assay uses recombinantly expressed BIR3 domain of XIAP

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
TALC GuideToPharmacology
GDC-0152 XIAP

Interaction Score: 1.18

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Details of the Assay for Interaction BIR3 domain of hXIAP

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
TTD GuideToPharmacology
CHEMBL504559 XIAP

Interaction Score: 0.79

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Details of the Assay for Interaction Fluorescence polarization assay using hXIAP BIR3 domain (residues 241-356)

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
ETOPOSIDE PHOSPHATE XIAP

Interaction Score: 0.68

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
14666661

Sources:
NCI
EMAPALUMAB XIAP

Interaction Score: 0.59

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
FDA PharmGKB
IDRONOXIL XIAP

Interaction Score: 0.47

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
ClearityFoundationClinicalTrial
ALVOCIDIB XIAP

Interaction Score: 0.43

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10887097 15235103 11751522

Sources:
NCI
TANESPIMYCIN XIAP

Interaction Score: 0.36

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12738674

Sources:
NCI
UCN-01 XIAP

Interaction Score: 0.36

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12738674 15255949

Sources:
NCI
DEQUALINIUM XIAP

Interaction Score: 0.34

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

PMIDs:
21340509

Sources:
DrugBank
RITUXIMAB XIAP

Interaction Score: 0.34

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
11895917

Sources:
NCI
CLADRIBINE XIAP

Interaction Score: 0.34

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12948851 15813915

Sources:
NCI
ADRIAMYCIN XIAP

Interaction Score: 0.25

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
11751478

Sources:
NCI
FLUDARABINE XIAP

Interaction Score: 0.24

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15059916

Sources:
NCI
TROGLITAZONE XIAP

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15498850

Sources:
NCI
IMATINIB XIAP

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
11368438 11234890

Sources:
NCI
BORTEZOMIB XIAP

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15813915

Sources:
NCI
CISPLATIN XIAP

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
11145600 15610860

Sources:
NCI

Ensembl: ENSG00000101966
- Version: 101_38
Alternate Names:

XIAP Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
TdgClinicalTrial: P98170
- Version: January-2014
Alternate Names:

XIAP Gene Symbol

Gene Info:

Target Class Miscellaneous

Target Subclass Inhibitor of apoptosis

Publications:
GuideToPharmacology: 331
- Version: 29-September-2020
Alternate Names:

592 HUGO Gene ID

592 HUGO Gene Symbol

X-linked inhibitor of apoptosis HUGO Gene Name

Gene Info:

GuideToPharmacology Gene Category Name Inhibitors of apoptosis (IAP) protein family

GuideToPharmacology Gene Category ID 889

Publications:

DrugBank: BE0001156

Version: 5.1.7

Alternate Names:

XIAP DrugBank Gene Name

P98170 UniProt Accession

331 Entrez Gene Id

Gene Info:

Publications:

Orzáez M et al., 2011, Characterization of dequalinium as a XIAP antagonist that targets the BIR2 domain., Apoptosis

Shaw TJ et al., 2008, Downregulation of XIAP expression in ovarian cancer cells induces cell death in vitro and in vivo., Int J Cancer

Lacasse EC et al., 2005, Application of XIAP antisense to cancer and other proliferative disorders: development of AEG35156/ GEM640., Ann N Y Acad Sci

TTD: X-linked inhibitor of apoptosis protein

Version: 2020.06.01

Alternate Names:

XIAP TTD Gene Abbreviation

T16769 TTD Target ID

Gene Info:

Publications:

Liu N et al., 2014, Debio 1143, an antagonist of multiple inhibitor-of-apoptosis proteins, activates apoptosis and enhances radiosensitization of non-small cell lung cancer cells in vitro., Am J Cancer Res

NCI: XIAP

Version: 14-September-2017

Alternate Names:

Gene Info:

Publications:

Li et al., 2001, Human ovarian cancer and cisplatin resistance: possible role of inhibitor of apoptosis proteins., Endocrinology

Nomura et al., Cisplatin inhibits the expression of X-linked inhibitor of apoptosis protein in human LNCaP cells., Urol. Oncol.

Maggio et al., 2004, The histone deacetylase inhibitor MS-275 interacts synergistically with fludarabine to induce apoptosis in human leukemia cells., Cancer Res.

DTC: XIAP
- Version: 02-September-2020
Alternate Names:

Gene Info:

Publications:

Sun H et al., 2011, Potent bivalent Smac mimetics: effect of the linker on binding to inhibitor of apoptosis proteins (IAPs) and anticancer activity., J Med Chem
TALC: XIAP
- Version: 12-May-2016
Alternate Names:

XIAP Gene Symbol

Gene Info:

Publications:
HingoraniCasas: ENSG00000101966
- Version: 31-May-2017
Alternate Names:

ENSG00000101966 Gene Symbol

XIAP Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
PharmGKB: XIAP
- Version: 18-August-2020
Alternate Names:

PA25361 PharmGKB ID

Gene Info:

Publications:
Pharos: XIAP
- Version: 03-September-2020
Alternate Names:

E3 ubiquitin-protein ligase XIAP Gene Name

P98170 UniProt ID

Gene Info:

Gene Categories:

KINASE, ENZYME

Publications:
dGene: XIAP
- Version: 27-Jun-2013
Alternate Names:

331 Gene ID

API3 dGene Synonym

BIRC4 dGene Synonym

Gene Info:

Gene Categories:

PROTEASE INHIBITOR

Publications:
ClearityFoundationClinicalTrial: XIAP
- Version: 15-June-2013
Alternate Names:

Gene Info:

Publications:
MskImpact: XIAP
- Version: May-2015
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
FDA: XIAP
- Version: 04-September-2020
Alternate Names:

Gene Info:

Publications:

Notes
Specific Action of the Ligand	Antagonist
Endogenous Drug?	False

Specific Action of the Ligand	Inhibition
Endogenous Drug?	False
Direct Interaction?	False

Notes
Details of the Assay for Interaction	Assay uses recombinantly expressed BIR3 domain of XIAP
Specific Action of the Ligand	Inhibition

Details of the Assay for Interaction	BIR3 domain of hXIAP
Specific Action of the Ligand	Antagonist
Endogenous Drug?	False

Details of the Assay for Interaction	Fluorescence polarization assay using hXIAP BIR3 domain (residues 241-356)
Specific Action of the Ligand	Antagonist
Endogenous Drug?	False

592	HUGO Gene ID
592	HUGO Gene Symbol
X-linked inhibitor of apoptosis	HUGO Gene Name

XIAP	DrugBank Gene Name
P98170	UniProt Accession
331	Entrez Gene Id

Novel drug target	Novel Target
Trial Name	CUDC-427

antagonist (inhibitory)
inhibitor (inhibitory)

antagonist (inhibitory)
inhibitor (inhibitory)

XIAP Gene Record

XIAP 331 Druggable GenomeClinically Actionable

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 10592235 17139284 17016423

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DrugBank

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Notes Specific Action of the Ligand Antagonist Endogenous Drug? False

PMIDs: None found

Sources: TTD TALC GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

PMIDs: 21462933

Sources: DTC GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info: Novel drug target Novel Target Trial Name CUDC-427

PMIDs: None found

Sources: TdgClinicalTrial

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Direct Interaction? False Endogenous Drug? False Specific Action of the Ligand Antagonist

PMIDs: 25520882

Sources: TTD TALC GuideToPharmacology

Interaction Types & Directionality: antagonist (inhibitory) inhibitor (inhibitory)

Interaction Info: Notes Details of the Assay for Interaction Assay uses recombinantly expressed BIR3 domain of XIAP Specific Action of the Ligand Inhibition

PMIDs: None found

Sources: TALC GuideToPharmacology

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Details of the Assay for Interaction BIR3 domain of hXIAP Specific Action of the Ligand Antagonist Endogenous Drug? False

PMIDs: None found

Sources: TTD GuideToPharmacology

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Details of the Assay for Interaction Fluorescence polarization assay using hXIAP BIR3 domain (residues 241-356) Specific Action of the Ligand Antagonist Endogenous Drug? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 14666661

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: FDA PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: ClearityFoundationClinicalTrial

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 10887097 15235103 11751522

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 12738674

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 12738674 15255949

Sources: NCI

Interaction Types & Directionality: antagonist (inhibitory) inhibitor (inhibitory)

Interaction Info:

PMIDs: 21340509

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 11895917

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 12948851 15813915

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

Interaction Types & Directionality:

n/a

PMIDs:
10592235 17139284 17016423

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DrugBank

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Notes

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
TTD TALC GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
21462933

Sources:
DTC GuideToPharmacology

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Novel Target

Trial Name CUDC-427

PMIDs:
None found

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
25520882

Sources:
TTD TALC GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Notes

Details of the Assay for Interaction Assay uses recombinantly expressed BIR3 domain of XIAP

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
TALC GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Details of the Assay for Interaction BIR3 domain of hXIAP

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
TTD GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Details of the Assay for Interaction Fluorescence polarization assay using hXIAP BIR3 domain (residues 241-356)

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
14666661

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
FDA PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
ClearityFoundationClinicalTrial

Interaction Types & Directionality:

n/a

PMIDs:
10887097 15235103 11751522

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
12738674

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
12738674 15255949

Sources:
NCI

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

PMIDs:
21340509

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
11895917

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
12948851 15813915

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
11751478

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
15059916

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
15498850

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
11368438 11234890

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
15813915

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
11145600 15610860

Sources:
NCI

Alternate Names:

XIAP Ensembl Gene Name