Details of the Target

General Information of Target

Target ID LDTP02486
Target Name Lysosomal alpha-glucosidase (GAA)
Gene Name GAA
Gene ID 2548
Synonyms
Lysosomal alpha-glucosidase; EC 3.2.1.20; Acid maltase; Aglucosidase alfa) [Cleaved into: 76 kDa lysosomal alpha-glucosidase; 70 kDa lysosomal alpha-glucosidase]
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MGVRHPPCSHRLLAVCALVSLATAALLGHILLHDFLLVPRELSGSSPVLEETHPAHQQGA
SRPGPRDAQAHPGRPRAVPTQCDVPPNSRFDCAPDKAITQEQCEARGCCYIPAKQGLQGA
QMGQPWCFFPPSYPSYKLENLSSSEMGYTATLTRTTPTFFPKDILTLRLDVMMETENRLH
FTIKDPANRRYEVPLETPHVHSRAPSPLYSVEFSEEPFGVIVRRQLDGRVLLNTTVAPLF
FADQFLQLSTSLPSQYITGLAEHLSPLMLSTSWTRITLWNRDLAPTPGANLYGSHPFYLA
LEDGGSAHGVFLLNSNAMDVVLQPSPALSWRSTGGILDVYIFLGPEPKSVVQQYLDVVGY
PFMPPYWGLGFHLCRWGYSSTAITRQVVENMTRAHFPLDVQWNDLDYMDSRRDFTFNKDG
FRDFPAMVQELHQGGRRYMMIVDPAISSSGPAGSYRPYDEGLRRGVFITNETGQPLIGKV
WPGSTAFPDFTNPTALAWWEDMVAEFHDQVPFDGMWIDMNEPSNFIRGSEDGCPNNELEN
PPYVPGVVGGTLQAATICASSHQFLSTHYNLHNLYGLTEAIASHRALVKARGTRPFVISR
STFAGHGRYAGHWTGDVWSSWEQLASSVPEILQFNLLGVPLVGADVCGFLGNTSEELCVR
WTQLGAFYPFMRNHNSLLSLPQEPYSFSEPAQQAMRKALTLRYALLPHLYTLFHQAHVAG
ETVARPLFLEFPKDSSTWTVDHQLLWGEALLITPVLQAGKAEVTGYFPLGTWYDLQTVPV
EALGSLPPPPAAPREPAIHSEGQWVTLPAPLDTINVHLRAGYIIPLQGPGLTTTESRQQP
MALAVALTKGGEARGELFWDDGESLEVLERGAYTQVIFLARNNTIVNELVRVTSEGAGLQ
LQKVTVLGVATAPQQVLSNGVPVSNFTYSPDTKVLDICVSLLMGEQFLVSWC
Target Type
Successful
Target Bioclass
Enzyme
Family
Glycosyl hydrolase 31 family
Subcellular location
Lysosome
Function Essential for the degradation of glycogen in lysosomes. Has highest activity on alpha-1,4-linked glycosidic linkages, but can also hydrolyze alpha-1,6-linked glucans.
TTD ID
T31514
Uniprot ID
P10253
DrugMap ID
TTLPC70
Ensemble ID
ENST00000302262.8
HGNC ID
HGNC:4065
ChEMBL ID
CHEMBL2608

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 11 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		15.00  LDD0402  [1]
Alkylaryl probe 1
 Probe Info  		9.00  LDD0387  [2]
Alkylaryl probe 2
 Probe Info  		20.00  LDD0391  [2]
FBPP2
 Probe Info  		5.97  LDD0318  [3]
TH216
 Probe Info  		Y407(17.27)  LDD0259  [4]
YN-1
 Probe Info  		100.00  LDD0444  [5]
Acrolein
 Probe Info  		N.A.  LDD0222  [6]
IA-alkyne
 Probe Info  		N.A.  LDD0036  [7]
Lodoacetamide azide
 Probe Info  		N.A.  LDD0037  [7]
NAIA_5
 Probe Info  		N.A.  LDD2223  [8]
HHS-482
 Probe Info  		Y458(0.38)  LDD2239  [9]
PAL-AfBPP Probe
Click To Hide/Show 71 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C022
 Probe Info  		12.47  LDD1728  [10]
C026
 Probe Info  		5.94  LDD1732  [10]
C040
 Probe Info  		6.45  LDD1740  [10]
C053
 Probe Info  		5.78  LDD1751  [10]
C070
 Probe Info  		9.78  LDD1766  [10]
C073
 Probe Info  		5.66  LDD1769  [10]
C082
 Probe Info  		5.62  LDD1774  [10]
C087
 Probe Info  		11.31  LDD1779  [10]
C106
 Probe Info  		43.11  LDD1793  [10]
C107
 Probe Info  		6.82  LDD1794  [10]
C108
 Probe Info  		10.78  LDD1795  [10]
C112
 Probe Info  		21.26  LDD1799  [10]
C115
 Probe Info  		7.57  LDD1802  [10]
C130
 Probe Info  		8.11  LDD1812  [10]
C134
 Probe Info  		35.75  LDD1816  [10]
C140
 Probe Info  		9.00  LDD1822  [10]
C149
 Probe Info  		7.01  LDD1830  [10]
C159
 Probe Info  		9.06  LDD1839  [10]
C160
 Probe Info  		8.00  LDD1840  [10]
C164
 Probe Info  		5.58  LDD1844  [10]
C170
 Probe Info  		30.27  LDD1850  [10]
C171
 Probe Info  		8.06  LDD1851  [10]
C178
 Probe Info  		17.88  LDD1857  [10]
C186
 Probe Info  		10.85  LDD1864  [10]
C197
 Probe Info  		7.21  LDD1873  [10]
C201
 Probe Info  		25.81  LDD1877  [10]
C206
 Probe Info  		17.51  LDD1881  [10]
C208
 Probe Info  		13.83  LDD1883  [10]
C211
 Probe Info  		9.06  LDD1885  [10]
C213
 Probe Info  		16.22  LDD1887  [10]
C220
 Probe Info  		13.93  LDD1894  [10]
C221
 Probe Info  		9.38  LDD1895  [10]
C223
 Probe Info  		16.00  LDD1897  [10]
C225
 Probe Info  		5.74  LDD1898  [10]
C232
 Probe Info  		36.76  LDD1905  [10]
C237
 Probe Info  		10.85  LDD1910  [10]
C281
 Probe Info  		6.54  LDD1951  [10]
C302
 Probe Info  		9.65  LDD1971  [10]
C305
 Probe Info  		10.41  LDD1974  [10]
C310
 Probe Info  		20.11  LDD1977  [10]
C326
 Probe Info  		10.27  LDD1990  [10]
C334
 Probe Info  		4.99  LDD1997  [10]
C339
 Probe Info  		5.62  LDD2002  [10]
C346
 Probe Info  		12.91  LDD2007  [10]
C349
 Probe Info  		10.27  LDD2010  [10]
C350
 Probe Info  		37.01  LDD2011  [10]
C355
 Probe Info  		27.47  LDD2016  [10]
C356
 Probe Info  		11.88  LDD2017  [10]
C357
 Probe Info  		5.31  LDD2018  [10]
C362
 Probe Info  		60.97  LDD2023  [10]
C363
 Probe Info  		32.45  LDD2024  [10]
C364
 Probe Info  		20.82  LDD2025  [10]
C390
 Probe Info  		21.86  LDD2049  [10]
C399
 Probe Info  		7.62  LDD2058  [10]
C403
 Probe Info  		14.52  LDD2061  [10]
C413
 Probe Info  		11.00  LDD2069  [10]
C419
 Probe Info  		8.94  LDD2074  [10]
C420
 Probe Info  		10.56  LDD2075  [10]
C425
 Probe Info  		17.39  LDD2080  [10]
C429
 Probe Info  		23.92  LDD2084  [10]
C431
 Probe Info  		18.25  LDD2086  [10]
FFF probe11
 Probe Info  		20.00  LDD0471  [11]
FFF probe12
 Probe Info  		20.00  LDD0473  [11]
FFF probe13
 Probe Info  		20.00  LDD0475  [11]
FFF probe14
 Probe Info  		20.00  LDD0477  [11]
FFF probe15
 Probe Info  		20.00  LDD0478  [11]
FFF probe2
 Probe Info  		16.85  LDD0463  [11]
FFF probe4
 Probe Info  		15.28  LDD0466  [11]
FFF probe9
 Probe Info  		20.00  LDD0470  [11]
JN0003
 Probe Info  		20.00  LDD0469  [11]
OEA-DA
 Probe Info  		20.00  LDD0046  [12]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0156  Aniline NCI-H1299 15.00  LDD0403  [1]
 LDCM0108  Chloroacetamide HeLa N.A.  LDD0222  [6]
 LDCM0185  Compound 17 HEK-293T 6.31  LDD0512  [11]
 LDCM0099  Phenelzine MDA-MB-231 4.00  LDD0392  [2]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Acarbose Small molecular drug DB00284
Hydroquinone Small molecular drug DB09526
Miglitol Small molecular drug DB00491
Alpha-arbutin . DB14109
Trastuzumab Deruxtecan . DB14962
Phase 3
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Avalglucosidase Alfa Recombinant protein D34SXJ
Deoxynojirimycin Small molecular drug D0S5LT
Bmn-701 . D05JEG
Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Salacinol Small molecular drug D07TSW
Phase 1
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Gz402666 . D0Q1UB
Preclinical
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
5-(4-(4-acetylphenyl)Piperazin-1-ylsulfonyl)-6-chloroindolin-2-one Small molecular drug DW68KF
Investigative
Click To Hide/Show 10 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
(-)-uniflorine A Small molecular drug D0KE8R
(R)-2,6-bis-hydroxymethyl-piperidine-3,4,5-triol Small molecular drug D0Q1KL
2,5-imino-2,5,6-trideoxy-d-manno-heptitol Small molecular drug D0X6BK
7-o-b-d-glucopyranosyl-a-homonojirimycin Small molecular drug D07JCA
Alpha-7-deoxyhomonojirimycin Small molecular drug D0ZC7V
Alpha-homonojirimycin Small molecular drug D03TYC
N-adamantanemethyloxypentyl-1-deoxynojirimycin Small molecular drug D0N9IX
Uniflorine B Small molecular drug D0J2JM
Valiolamine Small molecular drug D08TQA
At2220 . DB05200

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 Hydrazines as versatile chemical biology probes and drug-discovery tools for cofactor-dependent enzymes. bioRxiv, 2020-06.
3 Tranylcypromine specificity for monoamine oxidase is limited by promiscuous protein labelling and lysosomal trapping. RSC Chem Biol. 2020 Aug 12;1(4):209-213. doi: 10.1039/d0cb00048e. eCollection 2020 Oct 1.
Mass spectrometry data entry: PXD018580
4 Chemoproteomic profiling of kinases in live cells using electrophilic sulfonyl triazole probes. Chem Sci. 2021 Jan 21;12(9):3295-3307. doi: 10.1039/d0sc06623k.
5 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.
6 ACR-Based Probe for the Quantitative Profiling of Histidine Reactivity in the Human Proteome. J Am Chem Soc. 2023 Mar 8;145(9):5252-5260. doi: 10.1021/jacs.2c12653. Epub 2023 Feb 27.
7 Enhancing Cysteine Chemoproteomic Coverage through Systematic Assessment of Click Chemistry Product Fragmentation. Anal Chem. 2022 Mar 8;94(9):3800-3810. doi: 10.1021/acs.analchem.1c04402. Epub 2022 Feb 23.
Mass spectrometry data entry: PXD028853
8 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264
9 Global targeting of functional tyrosines using sulfur-triazole exchange chemistry. Nat Chem Biol. 2020 Feb;16(2):150-159. doi: 10.1038/s41589-019-0404-5. Epub 2019 Nov 25.
10 Large-scale chemoproteomics expedites ligand discovery and predicts ligand behavior in cells. Science. 2024 Apr 26;384(6694):eadk5864. doi: 10.1126/science.adk5864. Epub 2024 Apr 26.
Mass spectrometry data entry: PXD041587
11 Ligand and Target Discovery by Fragment-Based Screening in Human Cells. Cell. 2017 Jan 26;168(3):527-541.e29. doi: 10.1016/j.cell.2016.12.029. Epub 2017 Jan 19.
12 Mapping Protein Targets of Bioactive Small Molecules Using Lipid-Based Chemical Proteomics. ACS Chem Biol. 2017 Oct 20;12(10):2671-2681. doi: 10.1021/acschembio.7b00581. Epub 2017 Sep 20.
Mass spectrometry data entry: PXD007570