Details of the Target
General Information of Target
| Target ID | LDTP03557 | |||||
|---|---|---|---|---|---|---|
| Target Name | Leukocyte elastase inhibitor (SERPINB1) |
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| Gene Name | SERPINB1 | |||||
| Gene ID | 1992 | |||||
| Synonyms |
ELANH2; MNEI; PI2; Leukocyte elastase inhibitor; LEI; Monocyte/neutrophil elastase inhibitor; EI; M/NEI; Peptidase inhibitor 2; PI-2; Serpin B1 |
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| 3D Structure | ||||||
| Sequence |
MEQLSSANTRFALDLFLALSENNPAGNIFISPFSISSAMAMVFLGTRGNTAAQLSKTFHF
NTVEEVHSRFQSLNADINKRGASYILKLANRLYGEKTYNFLPEFLVSTQKTYGADLASVD FQHASEDARKTINQWVKGQTEGKIPELLASGMVDNMTKLVLVNAIYFKGNWKDKFMKEAT TNAPFRLNKKDRKTVKMMYQKKKFAYGYIEDLKCRVLELPYQGEELSMVILLPDDIEDES TGLKKIEEQLTLEKLHEWTKPENLDFIEVNVSLPRFKLEESYTLNSDLARLGVQDLFNSS KADLSGMSGARDIFISKIVHKSFVEVNEEGTEAAAATAGIATFCMLMPEENFTADHPFLF FIRHNSSGSILFLGRFSSP |
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| Target Bioclass |
Other
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| Family |
Serpin family, Ov-serpin subfamily
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| Subcellular location |
Secreted
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| Function |
Neutrophil serine protease inhibitor that plays an essential role in the regulation of the innate immune response, inflammation and cellular homeostasis. Acts primarily to protect the cell from proteases released in the cytoplasm during stress or infection. These proteases are important in killing microbes but when released from granules, these potent enzymes also destroy host proteins and contribute to mortality. Regulates the activity of the neutrophil proteases elastase, cathepsin G, proteinase-3, chymase, chymotrypsin, and kallikrein-3. Acts also as a potent intracellular inhibitor of GZMH by directly blocking its proteolytic activity. During inflammation, limits the activity of inflammatory caspases CASP1, CASP4 and CASP5 by suppressing their caspase-recruitment domain (CARD) oligomerization and enzymatic activation. When secreted, promotes the proliferation of beta-cells via its protease inhibitory function.
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| Uniprot ID | ||||||
| Ensemble ID | ||||||
| HGNC ID | ||||||
Target Site Mutations in Different Cell Lines
Probe(s) Labeling This Target
ABPP Probe
| Probe name | Structure | Binding Site(Ratio) | Interaction ID | Ref | |
|---|---|---|---|---|---|
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m-APA Probe Info |
 |
15.00 | LDD0402 | [1] | |
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CY-1 Probe Info |
 |
100.00 | LDD0243 | [2] | |
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CY4 Probe Info |
 |
100.00 | LDD0244 | [2] | |
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W1 Probe Info |
 |
16.85 | LDD0235 | [3] | |
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C-Sul Probe Info |
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2.47 | LDD0066 | [4] | |
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YN-1 Probe Info |
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100.00 | LDD0444 | [5] | |
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STPyne Probe Info |
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K137(9.49); K143(4.42); K177(10.00); K196(6.25) | LDD0277 | [6] | |
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AZ-9 Probe Info |
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E210(10.00) | LDD2208 | [7] | |
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Sulforaphane-probe2 Probe Info |
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1.71 | LDD0160 | [8] | |
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HHS-475 Probe Info |
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Y98(0.42) | LDD0264 | [9] | |
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Acrolein Probe Info |
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N.A. | LDD0223 | [10] | |
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ATP probe Probe Info |
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N.A. | LDD0035 | [11] | |
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IA-alkyne Probe Info |
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N.A. | LDD0151 | [12] | |
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AOyne Probe Info |
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13.40 | LDD0443 | [13] | |
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NAIA_5 Probe Info |
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N.A. | LDD2223 | [14] | |
PAL-AfBPP Probe
| Probe name | Structure | Binding Site(Ratio) | Interaction ID | Ref | |
|---|---|---|---|---|---|
|
FFF probe11 Probe Info |
 |
20.00 | LDD0472 | [15] | |
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DFG-out-3 Probe Info |
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2.50 | LDD0074 | [16] | |
Competitor(s) Related to This Target
| Competitor ID | Name | Cell line | Binding Site(Ratio) | Interaction ID | Ref |
|---|---|---|---|---|---|
| LDCM0156 | Aniline | NCI-H1299 | 14.07 | LDD0403 | [1] |
| LDCM0116 | HHS-0101 | DM93 | Y98(0.42) | LDD0264 | [9] |
| LDCM0117 | HHS-0201 | DM93 | Y98(0.41) | LDD0265 | [9] |
| LDCM0118 | HHS-0301 | DM93 | Y98(0.44) | LDD0266 | [9] |
| LDCM0119 | HHS-0401 | DM93 | Y98(0.52) | LDD0267 | [9] |
| LDCM0120 | HHS-0701 | DM93 | Y98(0.42) | LDD0268 | [9] |
| LDCM0109 | NEM | HeLa | N.A. | LDD0223 | [10] |
| LDCM0016 | Ranjitkar_cp1 | A431 | 2.50 | LDD0074 | [16] |
| LDCM0003 | Sulforaphane | MDA-MB-231 | 1.71 | LDD0160 | [8] |
References