Details of the Target

General Information of Target

Target ID LDTP05892
Target Name Baculoviral IAP repeat-containing protein 3 (BIRC3)
Gene Name BIRC3
Gene ID 330
Synonyms
API2; MIHC; RNF49; Baculoviral IAP repeat-containing protein 3; EC 2.3.2.27; Apoptosis inhibitor 2; API2; Cellular inhibitor of apoptosis 2; C-IAP2; IAP homolog C; Inhibitor of apoptosis protein 1; hIAP-1; hIAP1; RING finger protein 49; RING-type E3 ubiquitin transferase BIRC3; TNFR2-TRAF-signaling complex protein 1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MNIVENSIFLSNLMKSANTFELKYDLSCELYRMSTYSTFPAGVPVSERSLARAGFYYTGV
NDKVKCFCCGLMLDNWKRGDSPTEKHKKLYPSCRFVQSLNSVNNLEATSQPTFPSSVTNS
THSLLPGTENSGYFRGSYSNSPSNPVNSRANQDFSALMRSSYHCAMNNENARLLTFQTWP
LTFLSPTDLAKAGFYYIGPGDRVACFACGGKLSNWEPKDNAMSEHLRHFPKCPFIENQLQ
DTSRYTVSNLSMQTHAARFKTFFNWPSSVLVNPEQLASAGFYYVGNSDDVKCFCCDGGLR
CWESGDDPWVQHAKWFPRCEYLIRIKGQEFIRQVQASYPHLLEQLLSTSDSPGDENAESS
IIHFEPGEDHSEDAIMMNTPVINAAVEMGFSRSLVKQTVQRKILATGENYRLVNDLVLDL
LNAEDEIREEERERATEEKESNDLLLIRKNRMALFQHLTCVIPILDSLLTAGIINEQEHD
VIKQKTQTSLQARELIDTILVKGNIAATVFRNSLQEAEAVLYEHLFVQQDIKYIPTEDVS
DLPVEEQLRRLQEERTCKVCMDKEVSIVFIPCGHLVVCKDCAPSLRKCPICRSTIKGTVR
TFLS
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
IAP family
Subcellular location
Cytoplasm
Function
Multi-functional protein which regulates not only caspases and apoptosis, but also modulates inflammatory signaling and immunity, mitogenic kinase signaling and cell proliferation, as well as cell invasion and metastasis. Acts as an E3 ubiquitin-protein ligase regulating NF-kappa-B signaling and regulates both canonical and non-canonical NF-kappa-B signaling by acting in opposite directions: acts as a positive regulator of the canonical pathway and suppresses constitutive activation of non-canonical NF-kappa-B signaling. The target proteins for its E3 ubiquitin-protein ligase activity include: RIPK1, RIPK2, RIPK3, RIPK4, CASP3, CASP7, CASP8, IKBKE, TRAF1, and BCL10. Acts as an important regulator of innate immune signaling via regulation of Toll-like receptors (TLRs), Nodlike receptors (NLRs) and RIG-I like receptors (RLRs), collectively referred to as pattern recognition receptors (PRRs). Protects cells from spontaneous formation of the ripoptosome, a large multi-protein complex that has the capability to kill cancer cells in a caspase-dependent and caspase-independent manner. Suppresses ripoptosome formation by ubiquitinating RIPK1 and CASP8.
TTD ID
T35173
Uniprot ID
Q13489
DrugMap ID
TTIRY6K
Ensemble ID
ENST00000263464.9
HGNC ID
HGNC:591
ChEMBL ID
CHEMBL5335

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 4 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		15.00  LDD0402  [1]
DBIA
 Probe Info  		C28(1.00)  LDD0078  [2]
IA-alkyne
 Probe Info  		N.A.  LDD0175  [3]
IPM
 Probe Info  		N.A.  LDD0147  [4]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0216  AC100 PaTu 8988t C28(1.05)  LDD1095  [2]
 LDCM0217  AC101 PaTu 8988t C28(0.79)  LDD1096  [2]
 LDCM0218  AC102 PaTu 8988t C28(0.89)  LDD1097  [2]
 LDCM0219  AC103 PaTu 8988t C28(1.10)  LDD1098  [2]
 LDCM0220  AC104 PaTu 8988t C28(0.80)  LDD1099  [2]
 LDCM0221  AC105 PaTu 8988t C28(0.91)  LDD1100  [2]
 LDCM0222  AC106 PaTu 8988t C28(0.95)  LDD1101  [2]
 LDCM0223  AC107 PaTu 8988t C28(0.88)  LDD1102  [2]
 LDCM0224  AC108 PaTu 8988t C28(1.03)  LDD1103  [2]
 LDCM0225  AC109 PaTu 8988t C28(0.92)  LDD1104  [2]
 LDCM0227  AC110 PaTu 8988t C28(1.27)  LDD1106  [2]
 LDCM0228  AC111 PaTu 8988t C28(1.39)  LDD1107  [2]
 LDCM0229  AC112 PaTu 8988t C28(1.16)  LDD1108  [2]
 LDCM0263  AC143 PaTu 8988t C28(1.27)  LDD1142  [2]
 LDCM0264  AC144 PaTu 8988t C28(1.67)  LDD1143  [2]
 LDCM0265  AC145 PaTu 8988t C28(1.17)  LDD1144  [2]
 LDCM0266  AC146 PaTu 8988t C28(1.78)  LDD1145  [2]
 LDCM0267  AC147 PaTu 8988t C28(1.01)  LDD1146  [2]
 LDCM0268  AC148 PaTu 8988t C28(1.80)  LDD1147  [2]
 LDCM0269  AC149 PaTu 8988t C28(2.79)  LDD1148  [2]
 LDCM0271  AC150 PaTu 8988t C28(2.30)  LDD1150  [2]
 LDCM0272  AC151 PaTu 8988t C28(4.08)  LDD1151  [2]
 LDCM0273  AC152 PaTu 8988t C28(1.76)  LDD1152  [2]
 LDCM0274  AC153 PaTu 8988t C28(2.75)  LDD1153  [2]
 LDCM0621  AC154 PaTu 8988t C28(4.23)  LDD2166  [2]
 LDCM0622  AC155 PaTu 8988t C28(2.79)  LDD2167  [2]
 LDCM0623  AC156 PaTu 8988t C28(2.35)  LDD2168  [2]
 LDCM0624  AC157 PaTu 8988t C28(2.99)  LDD2169  [2]
 LDCM0365  AC98 PaTu 8988t C28(0.85)  LDD1244  [2]
 LDCM0366  AC99 PaTu 8988t C28(0.86)  LDD1245  [2]
 LDCM0156  Aniline NCI-H1299 11.43  LDD0403  [1]
 LDCM0020  ARS-1620 HCC44 C28(1.00)  LDD0078  [2]
 LDCM0403  CL16 PaTu 8988t C28(1.62)  LDD1282  [2]
 LDCM0404  CL17 PaTu 8988t C28(2.30)  LDD1283  [2]
 LDCM0405  CL18 PaTu 8988t C28(2.74)  LDD1284  [2]
 LDCM0406  CL19 PaTu 8988t C28(2.21)  LDD1285  [2]
 LDCM0408  CL20 PaTu 8988t C28(4.97)  LDD1287  [2]
 LDCM0409  CL21 PaTu 8988t C28(6.95)  LDD1288  [2]
 LDCM0410  CL22 PaTu 8988t C28(7.16)  LDD1289  [2]
 LDCM0411  CL23 PaTu 8988t C28(3.81)  LDD1290  [2]
 LDCM0412  CL24 PaTu 8988t C28(1.79)  LDD1291  [2]
 LDCM0413  CL25 PaTu 8988t C28(1.56)  LDD1292  [2]
 LDCM0414  CL26 PaTu 8988t C28(3.14)  LDD1293  [2]
 LDCM0415  CL27 PaTu 8988t C28(2.78)  LDD1294  [2]
 LDCM0416  CL28 PaTu 8988t C28(9.62)  LDD1295  [2]
 LDCM0417  CL29 PaTu 8988t C28(7.20)  LDD1296  [2]
 LDCM0419  CL30 PaTu 8988t C28(4.03)  LDD1298  [2]
 LDCM0420  CL31 PaTu 8988t C28(1.69)  LDD1299  [2]
 LDCM0421  CL32 PaTu 8988t C28(2.59)  LDD1300  [2]
 LDCM0422  CL33 PaTu 8988t C28(4.14)  LDD1301  [2]
 LDCM0423  CL34 PaTu 8988t C28(2.42)  LDD1302  [2]
 LDCM0424  CL35 PaTu 8988t C28(1.94)  LDD1303  [2]
 LDCM0425  CL36 PaTu 8988t C28(4.98)  LDD1304  [2]
 LDCM0426  CL37 PaTu 8988t C28(2.70)  LDD1305  [2]
 LDCM0428  CL39 PaTu 8988t C28(4.71)  LDD1307  [2]
 LDCM0430  CL40 PaTu 8988t C28(1.28)  LDD1309  [2]
 LDCM0431  CL41 PaTu 8988t C28(1.67)  LDD1310  [2]
 LDCM0432  CL42 PaTu 8988t C28(2.36)  LDD1311  [2]
 LDCM0433  CL43 PaTu 8988t C28(4.98)  LDD1312  [2]
 LDCM0434  CL44 PaTu 8988t C28(2.06)  LDD1313  [2]
 LDCM0435  CL45 PaTu 8988t C28(5.13)  LDD1314  [2]
 LDCM0436  CL46 PaTu 8988t C28(5.75)  LDD1315  [2]
 LDCM0437  CL47 PaTu 8988t C28(2.74)  LDD1316  [2]
 LDCM0438  CL48 PaTu 8988t C28(0.98)  LDD1317  [2]
 LDCM0439  CL49 PaTu 8988t C28(1.31)  LDD1318  [2]
 LDCM0441  CL50 PaTu 8988t C28(1.56)  LDD1320  [2]
 LDCM0442  CL51 PaTu 8988t C28(1.32)  LDD1321  [2]
 LDCM0443  CL52 PaTu 8988t C28(1.27)  LDD1322  [2]
 LDCM0444  CL53 PaTu 8988t C28(1.26)  LDD1323  [2]
 LDCM0445  CL54 PaTu 8988t C28(11.70)  LDD1324  [2]
 LDCM0446  CL55 PaTu 8988t C28(1.24)  LDD1325  [2]
 LDCM0447  CL56 PaTu 8988t C28(3.33)  LDD1326  [2]
 LDCM0448  CL57 PaTu 8988t C28(1.79)  LDD1327  [2]
 LDCM0449  CL58 PaTu 8988t C28(0.99)  LDD1328  [2]
 LDCM0450  CL59 PaTu 8988t C28(1.34)  LDD1329  [2]
 LDCM0452  CL60 PaTu 8988t C28(5.81)  LDD1331  [2]
 LDCM0469  CL76 PaTu 8988t C28(1.12)  LDD1348  [2]
 LDCM0470  CL77 PaTu 8988t C28(3.02)  LDD1349  [2]
 LDCM0471  CL78 PaTu 8988t C28(1.51)  LDD1350  [2]
 LDCM0472  CL79 PaTu 8988t C28(1.63)  LDD1351  [2]
 LDCM0474  CL80 PaTu 8988t C28(1.53)  LDD1353  [2]
 LDCM0475  CL81 PaTu 8988t C28(2.64)  LDD1354  [2]
 LDCM0476  CL82 PaTu 8988t C28(1.63)  LDD1355  [2]
 LDCM0477  CL83 PaTu 8988t C28(2.70)  LDD1356  [2]
 LDCM0478  CL84 PaTu 8988t C28(1.48)  LDD1357  [2]
 LDCM0479  CL85 PaTu 8988t C28(1.24)  LDD1358  [2]
 LDCM0480  CL86 PaTu 8988t C28(1.80)  LDD1359  [2]
 LDCM0481  CL87 PaTu 8988t C28(1.53)  LDD1360  [2]
 LDCM0482  CL88 PaTu 8988t C28(1.71)  LDD1361  [2]
 LDCM0483  CL89 PaTu 8988t C28(1.44)  LDD1362  [2]
 LDCM0485  CL90 PaTu 8988t C28(2.91)  LDD1364  [2]
 LDCM0201  EV-3 T cell C28(5.15)  LDD0515  [5]
 LDCM0625  F8 Ramos C28(0.87); C164(1.87)  LDD2187  [6]
 LDCM0573  Fragment11 Ramos C164(7.97)  LDD2190  [6]
 LDCM0575  Fragment13 Ramos C28(1.27); C164(1.14)  LDD2192  [6]
 LDCM0576  Fragment14 Ramos C28(2.10); C164(1.26)  LDD2193  [6]
 LDCM0580  Fragment21 Ramos C164(1.07)  LDD2195  [6]
 LDCM0582  Fragment23 Ramos C28(4.23); C164(1.19)  LDD2196  [6]
 LDCM0578  Fragment27 Ramos C164(0.99)  LDD2197  [6]
 LDCM0586  Fragment28 Ramos C28(1.31); C164(0.63)  LDD2198  [6]
 LDCM0588  Fragment30 Ramos C28(2.18); C164(1.61)  LDD2199  [6]
 LDCM0589  Fragment31 Ramos C28(0.72); C164(1.16)  LDD2200  [6]
 LDCM0468  Fragment33 Ramos C164(2.01)  LDD2202  [6]
 LDCM0596  Fragment38 Ramos C28(0.75); C164(1.40)  LDD2203  [6]
 LDCM0566  Fragment4 Ramos C28(0.72); C164(1.21)  LDD2184  [6]
 LDCM0427  Fragment51 PaTu 8988t C28(4.31)  LDD1306  [2]
 LDCM0610  Fragment52 Ramos C164(1.18)  LDD2204  [6]
 LDCM0614  Fragment56 Ramos C28(0.74); C164(1.19)  LDD2205  [6]
 LDCM0569  Fragment7 Ramos C28(1.24)  LDD2186  [6]
 LDCM0022  KB02 T cell C28(20.00)  LDD1703  [5]
 LDCM0024  KB05 T cell-activated C28(6.03)  LDD1706  [5]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 7 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Receptor-interacting serine/threonine-protein kinase 1 (RIPK1) TKL Ser/Thr protein kinase family Q13546
Receptor-interacting serine/threonine-protein kinase 2 (RIPK2) TKL Ser/Thr protein kinase family O43353
Receptor-interacting serine/threonine-protein kinase 3 (RIPK3) TKL Ser/Thr protein kinase family Q9Y572
Receptor-interacting serine/threonine-protein kinase 4 (RIPK4) TKL Ser/Thr protein kinase family P57078
TNF receptor-associated factor 2 (TRAF2) TNF receptor-associated factor family Q12933
Ubiquitin-conjugating enzyme E2 D2 (UBE2D2) Ubiquitin-conjugating enzyme family P62837
Ubiquitin-conjugating enzyme E2 N (UBE2N) Ubiquitin-conjugating enzyme family P61088

The Drug(s) Related To This Target

Phase 3
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
At-406 Small molecular drug D03MXK
Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Azd5582 Small molecular drug D0VK7M
Patented
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pmid25980951-compound-1 Small molecular drug D0R3YM
Pmid25980951-compound-27 Small molecular drug D0B6KC
Pmid25980951-compound-43 Small molecular drug D0HY5Q
Pmid25980951-compound-44 Small molecular drug D0YN1X

References

1 Quantitative and Site-Specific Chemoproteomic Profiling of Targets of Acrolein. Chem Res Toxicol. 2019 Mar 18;32(3):467-473. doi: 10.1021/acs.chemrestox.8b00343. Epub 2019 Jan 15.
2 Reimagining high-throughput profiling of reactive cysteines for cell-based screening of large electrophile libraries. Nat Biotechnol. 2021 May;39(5):630-641. doi: 10.1038/s41587-020-00778-3. Epub 2021 Jan 4.
3 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060
4 Chemoproteomic Profiling by Cysteine Fluoroalkylation Reveals Myrocin G as an Inhibitor of the Nonhomologous End Joining DNA Repair Pathway. J Am Chem Soc. 2021 Dec 8;143(48):20332-20342. doi: 10.1021/jacs.1c09724. Epub 2021 Nov 24.
Mass spectrometry data entry: PXD029255
5 An Activity-Guided Map of Electrophile-Cysteine Interactions in Primary Human T Cells. Cell. 2020 Aug 20;182(4):1009-1026.e29. doi: 10.1016/j.cell.2020.07.001. Epub 2020 Jul 29.
6 Site-specific quantitative cysteine profiling with data-independent acquisition-based mass spectrometry. Methods Enzymol. 2023;679:295-322. doi: 10.1016/bs.mie.2022.07.037. Epub 2022 Sep 7.
Mass spectrometry data entry: PXD027578