Details of the Target

General Information of Target

Target ID LDTP01811
Target Name Alpha-1-antitrypsin (SERPINA1)
Gene Name SERPINA1
Gene ID 5265
Synonyms
AAT; PI; Alpha-1-antitrypsin; Alpha-1 protease inhibitor; Alpha-1-antiproteinase; Serpin A1) [Cleaved into: Short peptide from AAT; SPAAT)]
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MPSSVSWGILLLAGLCCLVPVSLAEDPQGDAAQKTDTSHHDQDHPTFNKITPNLAEFAFS
LYRQLAHQSNSTNIFFSPVSIATAFAMLSLGTKADTHDEILEGLNFNLTEIPEAQIHEGF
QELLRTLNQPDSQLQLTTGNGLFLSEGLKLVDKFLEDVKKLYHSEAFTVNFGDTEEAKKQ
INDYVEKGTQGKIVDLVKELDRDTVFALVNYIFFKGKWERPFEVKDTEEEDFHVDQVTTV
KVPMMKRLGMFNIQHCKKLSSWVLLMKYLGNATAIFFLPDEGKLQHLENELTHDIITKFL
ENEDRRSASLHLPKLSITGTYDLKSVLGQLGITKVFSNGADLSGVTEEAPLKLSKAVHKA
VLTIDEKGTEAAGAMFLEAIPMSIPPEVKFNKPFVFLMIEQNTKSPLFMGKVVNPTQK
Target Type
Successful
Target Bioclass
Other
Family
Serpin family
Subcellular location
Secreted; Secreted, extracellular space, extracellular matrix
Function
Inhibitor of serine proteases. Its primary target is elastase, but it also has a moderate affinity for plasmin and thrombin. Irreversibly inhibits trypsin, chymotrypsin and plasminogen activator. The aberrant form inhibits insulin-induced NO synthesis in platelets, decreases coagulation time and has proteolytic activity against insulin and plasmin.; [Short peptide from AAT]: Reversible chymotrypsin inhibitor. It also inhibits elastase, but not trypsin. Its major physiological function is the protection of the lower respiratory tract against proteolytic destruction by human leukocyte elastase (HLE).
TTD ID
T28265
Uniprot ID
P01009
DrugMap ID
TT2L4TV
Ensemble ID
ENST00000355814.8
HGNC ID
HGNC:8941

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
AGS SNV: p.F276V .
CHL1 SNV: p.V242M .
COLO792 SNV: p.Q115Ter .
G401 SNV: p.N53K .
HCC1395 SNV: p.E110D .
HCT116 SNV: p.K267R .
HCT15 SNV: p.Q285P .
KMS12BM SNV: p.D43A .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 5 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
YN-1
 Probe Info  		100.00  LDD0444  [1]
IPM
 Probe Info  		N.A.  LDD0241  [2]
DBIA
 Probe Info  		C256(2.61)  LDD3325  [3]
IA-alkyne
 Probe Info  		C256(20.00)  LDD1704  [4]
W1
 Probe Info  		N.A.  LDD0236  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 T cell-activated C256(20.00)  LDD1704  [4]
 LDCM0023  KB03 BRX211 C256(6.07)  LDD2685  [3]
 LDCM0024  KB05 UACC257 C256(2.61)  LDD3325  [3]
 LDCM0110  W12 Hep-G2 C256(6.85)  LDD0237  [2]
 LDCM0111  W14 Hep-G2 C256(4.76)  LDD0238  [2]
 LDCM0112  W16 Hep-G2 C256(0.85)  LDD0239  [2]
 LDCM0113  W17 Hep-G2 H255(0.82); C256(0.88)  LDD0240  [2]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Transmembrane protease serine 2 (TMPRSS2) Peptidase S1 family O15393
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Translocon-associated protein subunit alpha (SSR1) TRAP-alpha family P43307
Other
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Endoplasmic reticulum-Golgi intermediate compartment protein 3 (ERGIC3) ERGIC family Q9Y282
Alpha-1-antitrypsin (SERPINA1) Serpin family P01009
Melanoma-associated antigen B6 (MAGEB6) . Q8N7X4

The Drug(s) Related To This Target

Approved
Click To Hide/Show 7 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Zemaira Recombinant protein D9EC0G
Copper . DB09130
Glassia . D04ELD
Zinc . DB01593
Zinc Acetate . DB14487
Zinc Chloride . DB14533
Zinc Sulfate Unspecified Form . DB14548
Phase 2
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Igmesine Small molecular drug D0N5LJ
Agtc-0106 . D0QF2W
Investigative
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
2-sulfhydryl-ethanol Small molecular drug D0Q5FV
Mercaptoethanol Small molecular drug DB03345
Ppl-100 Small molecular drug DB05961
2-[34-dihydroxy-2-hydroxymethyl-5-(2-hydroxy-nonyl)-tetrahydro-furan-2-yloxy]-6-hydroxymethyl-tetra Hydro-pyran-345-triol . DB01998
Recombinant Alpha 1-antitrypsin . DB05481

References

1 Ynamide Electrophile for the Profiling of Ligandable Carboxyl Residues in Live Cells and the Development of New Covalent Inhibitors. J Med Chem. 2022 Aug 11;65(15):10408-10418. doi: 10.1021/acs.jmedchem.2c00272. Epub 2022 Jul 26.
2 Oxidant-Induced Bioconjugation for Protein Labeling in Live Cells. ACS Chem Biol. 2023 Jan 20;18(1):112-122. doi: 10.1021/acschembio.2c00740. Epub 2022 Dec 21.
3 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
4 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.