Details of the Target

General Information of Target

Target ID LDTP03670
Target Name Guanylate cyclase soluble subunit alpha-2 (GUCY1A2)
Gene Name GUCY1A2
Gene ID 2977
Synonyms
GUC1A2; GUCSA2; Guanylate cyclase soluble subunit alpha-2; GCS-alpha-2; EC 4.6.1.2
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSRRKISSESFSSLGSDYLETSPEEEGECPLSRLCWNGSRSPPGPLEPSPAAAAAAAAPA
PTPAASAAAAAATAGARRVQRRRRVNLDSLGESISRLTAPSPQTIQQTLKRTLQYYEHQV
IGYRDAEKNFHNISNRCSYADHSNKEEIEDVSGILQCTANILGLKFEEIQKRFGEEFFNI
CFHENERVLRAVGGTLQDFFNGFDALLEHIRTSFGKQATLESPSFLCKELPEGTLMLHYF
HPHHIVGFAMLGMIKAAGKKIYRLDVEVEQVANEKLCSDVSNPGNCSCLTFLIKECENTN
IMKNLPQGTSQVPADLRISINTFCRAFPFHLMFDPSMSVLQLGEGLRKQLRCDTHKVLKF
EDCFEIVSPKVNATFERVLLRLSTPFVIRTKPEASGSENKDKVMEVKGQMIHVPESNSIL
FLGSPCVDKLDELMGRGLHLSDIPIHDATRDVILVGEQAKAQDGLKKRMDKLKATLERTH
QALEEEKKKTVDLLYSIFPGDVAQQLWQGQQVQARKFDDVTMLFSDIVGFTAICAQCTPM
QVISMLNELYTRFDHQCGFLDIYKVETIGDAYCVAAGLHRKSLCHAKPIALMALKMMELS
EEVLTPDGRPIQMRIGIHSGSVLAGVVGVRMPRYCLFGNNVTLASKFESGSHPRRINVSP
TTYQLLKREESFTFIPRSREELPDNFPKEIPGICYFLEVRTGPKPPKPSLSSSRIKKVSY
NIGTMFLRETSL
Target Bioclass
Enzyme
Family
Adenylyl cyclase class-4/guanylyl cyclase family
Subcellular location
Cytoplasm
Function Has guanylyl cyclase on binding to the beta-1 subunit.; Isoform 2 acts as a negative regulator of guanylyl cyclase activity as it forms non-functional heterodimers with the beta subunits.
Uniprot ID
P33402
Ensemble ID
ENST00000282249.6
HGNC ID
HGNC:4684
ChEMBL ID
CHEMBL2111348

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
DU145 SNV: p.G628W; p.R677L .
FADU SNV: p.G396S .
G402 SNV: p.V622L .
HCT15 SNV: p.T98M .
MCC13 SNV: p.M410I .
MEC1 SNV: p.E344D .
NALM6 Deletion: p.F200LfsTer54 .
NCIH1993 SNV: p.M434I .
NCIH2172 SNV: p.E26D .
NCIH2291 SNV: p.T531K .
NCIH716 SNV: p.N417Y .
SKMEL5 SNV: p.R351Ter .
SNGM SNV: p.L90P .
TFK1 SNV: p.E221K .
TOV21G SNV: p.E26Ter; p.G27W .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
IA-alkyne
 Probe Info  		C277(0.66)  LDD2157  [1]
DBIA
 Probe Info  		C296(0.84)  LDD1508  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0215  AC10 HEK-293T C296(0.84)  LDD1508  [2]
 LDCM0277  AC18 HEK-293T C296(0.82)  LDD1516  [2]
 LDCM0279  AC2 HEK-293T C296(0.77)  LDD1518  [2]
 LDCM0281  AC21 HEK-293T C296(0.98)  LDD1520  [2]
 LDCM0286  AC26 HEK-293T C296(1.27)  LDD1525  [2]
 LDCM0289  AC29 HEK-293T C296(0.98)  LDD1528  [2]
 LDCM0295  AC34 HEK-293T C296(0.88)  LDD1534  [2]
 LDCM0298  AC37 HEK-293T C296(1.32)  LDD1537  [2]
 LDCM0304  AC42 HEK-293T C296(0.91)  LDD1543  [2]
 LDCM0307  AC45 HEK-293T C296(1.28)  LDD1546  [2]
 LDCM0312  AC5 HEK-293T C296(1.32)  LDD1551  [2]
 LDCM0313  AC50 HEK-293T C296(1.03)  LDD1552  [2]
 LDCM0316  AC53 HEK-293T C296(0.97)  LDD1555  [2]
 LDCM0321  AC58 HEK-293T C296(0.95)  LDD1560  [2]
 LDCM0325  AC61 HEK-293T C296(0.90)  LDD1564  [2]
 LDCM0248  AKOS034007472 HEK-293T C296(0.89)  LDD1511  [2]
 LDCM0405  CL18 HEK-293T C296(1.20)  LDD1609  [2]
 LDCM0409  CL21 HEK-293T C296(1.26)  LDD1613  [2]
 LDCM0419  CL30 HEK-293T C296(0.95)  LDD1623  [2]
 LDCM0422  CL33 HEK-293T C296(1.44)  LDD1626  [2]
 LDCM0432  CL42 HEK-293T C296(1.06)  LDD1636  [2]
 LDCM0435  CL45 HEK-293T C296(0.96)  LDD1639  [2]
 LDCM0445  CL54 HEK-293T C296(0.96)  LDD1648  [2]
 LDCM0448  CL57 HEK-293T C296(1.35)  LDD1651  [2]
 LDCM0451  CL6 HEK-293T C296(1.15)  LDD1654  [2]
 LDCM0458  CL66 HEK-293T C296(0.79)  LDD1661  [2]
 LDCM0461  CL69 HEK-293T C296(1.11)  LDD1664  [2]
 LDCM0471  CL78 HEK-293T C296(1.18)  LDD1674  [2]
 LDCM0475  CL81 HEK-293T C296(1.11)  LDD1678  [2]
 LDCM0484  CL9 HEK-293T C296(1.33)  LDD1687  [2]
 LDCM0485  CL90 HEK-293T C296(1.16)  LDD1688  [2]
 LDCM0488  CL93 HEK-293T C296(1.26)  LDD1691  [2]
 LDCM0022  KB02 BRX211 C296(1.68)  LDD2268  [3]
 LDCM0023  KB03 BRX211 C296(3.42)  LDD2685  [3]
 LDCM0024  KB05 BRX211 C296(2.03)  LDD3102  [3]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Disks large homolog 1 (DLG1) MAGUK family Q12959
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Homeobox protein goosecoid-2 (GSC2) Paired homeobox family O15499
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Protein scribble homolog (SCRIB) LAP (LRR and PDZ) protein family Q14160

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
Isosorbide Mononitrate Small molecular drug DB01020
Molsidomine Small molecular drug DB09282
Nitric Oxide Small molecular drug DB00435
Pentaerythritol Tetranitrate Small molecular drug DB06154
Plecanatide Small molecular drug DB13170
Riociguat Small molecular drug DB08931
Methylene Blue . DB09241

References

1 From chemoproteomic-detected amino acids to genomic coordinates: insights into precise multi-omic data integration. Mol Syst Biol. 2021 Feb;17(2):e9840. doi: 10.15252/msb.20209840.
Mass spectrometry data entry: PXD022151
2 Accelerating multiplexed profiling of protein-ligand interactions: High-throughput plate-based reactive cysteine profiling with minimal input. Cell Chem Biol. 2024 Mar 21;31(3):565-576.e4. doi: 10.1016/j.chembiol.2023.11.015. Epub 2023 Dec 19.
Mass spectrometry data entry: PXD044402
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