Details of the Target

General Information of Target

Target ID LDTP10115
Target Name Repulsive guidance molecule A (RGMA)
Gene Name RGMA
Gene ID 56963
Synonyms
RGM; Repulsive guidance molecule A; RGM domain family member A
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MVLGKVKSLTISFDCLNDSNVPVYSSGDTVSGRVNLEVTGEIRVKSLKIHARGHAKVRWT
ESRNAGSNTAYTQNYTEEVEYFNHKDILIGHERDDDNSEEGFHTIHSGRHEYAFSFELPQ
TPLATSFEGRHGSVRYWVKAELHRPWLLPVKLKKEFTVFEHIDINTPSLLSPQAGTKEKT
LCCWFCTSGPISLSAKIERKGYTPGESIQIFAEIENCSSRMVVPKAAIYQTQAFYAKGKM
KEVKQLVANLRGESLSSGKTETWNGKLLKIPPVSPSILDCSIIRVEYSLMVYVDIPGAMD
LFLNLPLVIGTIPLHPFGSRTSSVSSQCSMNMNWLSLSLPERPEAPPSYAEVVTEEQRRN
NLAPVSACDDFERALQGPLFAYIQEFRFLPPPLYSEIDPNPDQSADDRPSCPSR
Target Type
Clinical trial
Target Bioclass
Other
Family
Repulsive guidance molecule (RGM) family
Subcellular location
Cell membrane
Function
Member of the repulsive guidance molecule (RGM) family that performs several functions in the developing and adult nervous system. Regulates cephalic neural tube closure, inhibits neurite outgrowth and cortical neuron branching, and the formation of mature synapses. Binding to its receptor NEO1/neogenin induces activation of RHOA-ROCK1/Rho-kinase signaling pathway through UNC5B-ARHGEF12/LARG-PTK2/FAK1 cascade, leading to collapse of the neuronal growth cone and neurite outgrowth inhibition. Furthermore, RGMA binding to NEO1/neogenin leads to HRAS inactivation by influencing HRAS-PTK2/FAK1-AKT1 pathway. It also functions as a bone morphogenetic protein (BMP) coreceptor that may signal through SMAD1, SMAD5, and SMAD8.
TTD ID
T99313
Uniprot ID
Q96B86
DrugMap ID
TTURJV4
Ensemble ID
ENST00000329082.12
HGNC ID
HGNC:30308
ChEMBL ID
CHEMBL4630886

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
COLO792 SNV: p.A83T .
MEWO SNV: p.G251R .
OVCAR8 Insertion: p.H269AfsTer67
SNV: p.Q268Ter		 .
SKMEL2 SNV: p.G22R .
TOV21G SNV: p.E74Ter .

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
Acrolein
 Probe Info  		N.A.  LDD0225  [1]
DBIA
 Probe Info  		C145(1.07)  LDD1510  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0237  AC12 HEK-293T C145(1.07)  LDD1510  [2]
 LDCM0270  AC15 HEK-293T C145(1.28)  LDD1513  [2]
 LDCM0280  AC20 HEK-293T C145(1.04)  LDD1519  [2]
 LDCM0283  AC23 HEK-293T C145(1.17)  LDD1522  [2]
 LDCM0288  AC28 HEK-293T C145(1.28)  LDD1527  [2]
 LDCM0292  AC31 HEK-293T C145(1.00)  LDD1531  [2]
 LDCM0297  AC36 HEK-293T C145(1.23)  LDD1536  [2]
 LDCM0300  AC39 HEK-293T C145(1.21)  LDD1539  [2]
 LDCM0301  AC4 HEK-293T C145(1.26)  LDD1540  [2]
 LDCM0306  AC44 HEK-293T C145(0.90)  LDD1545  [2]
 LDCM0309  AC47 HEK-293T C145(1.10)  LDD1548  [2]
 LDCM0315  AC52 HEK-293T C145(0.98)  LDD1554  [2]
 LDCM0318  AC55 HEK-293T C145(1.11)  LDD1557  [2]
 LDCM0324  AC60 HEK-293T C145(1.07)  LDD1563  [2]
 LDCM0327  AC63 HEK-293T C145(1.21)  LDD1566  [2]
 LDCM0334  AC7 HEK-293T C145(1.10)  LDD1568  [2]
 LDCM0379  CL11 HEK-293T C145(1.09)  LDD1583  [2]
 LDCM0408  CL20 HEK-293T C145(1.13)  LDD1612  [2]
 LDCM0411  CL23 HEK-293T C145(1.01)  LDD1615  [2]
 LDCM0421  CL32 HEK-293T C145(0.95)  LDD1625  [2]
 LDCM0424  CL35 HEK-293T C145(1.02)  LDD1628  [2]
 LDCM0434  CL44 HEK-293T C145(1.01)  LDD1638  [2]
 LDCM0437  CL47 HEK-293T C145(1.12)  LDD1641  [2]
 LDCM0447  CL56 HEK-293T C145(1.15)  LDD1650  [2]
 LDCM0450  CL59 HEK-293T C145(1.17)  LDD1653  [2]
 LDCM0460  CL68 HEK-293T C145(0.98)  LDD1663  [2]
 LDCM0464  CL71 HEK-293T C145(1.17)  LDD1667  [2]
 LDCM0473  CL8 HEK-293T C145(1.07)  LDD1676  [2]
 LDCM0474  CL80 HEK-293T C145(0.89)  LDD1677  [2]
 LDCM0477  CL83 HEK-293T C145(1.21)  LDD1680  [2]
 LDCM0487  CL92 HEK-293T C145(1.14)  LDD1690  [2]
 LDCM0490  CL95 HEK-293T C145(1.22)  LDD1693  [2]
 LDCM0109  NEM HeLa N.A.  LDD0225  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Telomeric repeat-binding factor 2-interacting protein 1 (TERF2IP) RAP1 family Q9NYB0
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Bone morphogenetic protein 2 (BMP2) TGF-beta family P12643

The Drug(s) Related To This Target

Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Elezanumab Antibody D0DV8Z

References

1 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.
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