General Information of Target

Target ID LDTP02425
Target Name SLIT-ROBO Rho GTPase-activating protein 2C (SRGAP2C)
Gene Name SRGAP2C
Gene ID 653464
Synonyms
SRGAP2P1; SLIT-ROBO Rho GTPase-activating protein 2C; SLIT-ROBO Rho GTPase activating protein 2 pseudogene 1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MTSPAKFKKDKEIIAEYDTQVKEIRAQLTEQMKCLDQQCELRVQLLQDLQDFFRKKAEIE
MDYSRNLEKLAEHFLAKTRSTKDQQFKKDQNVLSPVNCWNLLLNQVKWESRDHTTLSDIY
LNNIIPRFVQVSEDSGRLFKKSKEVGQQLQDDLMKVLNELYSVMKTYHMYNADSISAQSK
LKEAEKQEEKQIGKSVKQEDRQTPCSPDSTANVRIEEKHVRRSSVKKIEKMKEKHQAKYT
ENKLKAIKAQNEYLLALEATNASVFKYYIHDLSDLIDQCCDLGYHASLNRALRTFLSAEL
NLEQSKHEGLDAIENAVENLDATSDKQRLMEMYNNVFCPPMKFEFQPHMGDMASQLCAQQ
PVQSELVQRCQQLQSRLSTLKIENEEVKKTMEATLQTIQDIVTVEDFDVSDCFQYSNSME
SVKSTVSETFMSKPSIAKRRANQQETEQFYFTVRECYGF
Target Bioclass
Other
Function
Human-specific protein that acts as a key modifier of cortical connectivity in the human brain. Acts by inhibiting the functions of ancestral paralog SRGAP2/SRGAP2A, a postsynaptic protein that regulates excitatory and inhibitory synapse maturation and density in cortical pyramidal neurons. SRGAP2C is unstable but is able to heterodimerize with SRGAP2/SRGAP2A, thereby reducing SRGAP2/SRGAP2A levels through proteasome-dependent degradation. Inhibition of SRGAP2/SRGAP2A by SRGAP2C leads to an increase in synaptic density and protracted synaptic maturation of both excitatory and inhibitory synapses. Modifies cortical circuit connectivity by increasing the number of local and long-range cortical inputs received by layer 2/3 pyramidal neurons. Also able to increase the probability of sensory-evoked responses by layer 2/3 pyramidal neurons.
Uniprot ID
P0DJJ0
Ensemble ID
ENST00000367123.8
HGNC ID
HGNC:30584

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 4 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info 
C357(1.29)  LDD3410  [1]
HHS-475
 Probe Info 
Y170(1.01)  LDD0264  [2]
HHS-465
 Probe Info 
Y170(10.00)  LDD2237  [3]
IA-alkyne
 Probe Info 
N.A.  LDD0163  [4]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0116  HHS-0101 DM93 Y170(1.01)  LDD0264  [2]
 LDCM0117  HHS-0201 DM93 Y170(0.68)  LDD0265  [2]
 LDCM0118  HHS-0301 DM93 Y170(0.64)  LDD0266  [2]
 LDCM0119  HHS-0401 DM93 Y170(0.72)  LDD0267  [2]
 LDCM0120  HHS-0701 DM93 Y170(1.65)  LDD0268  [2]
 LDCM0022  KB02 A-375 C357(1.84)  LDD2255  [1]
 LDCM0023  KB03 HMCB C357(3.73)  LDD2776  [1]
 LDCM0024  KB05 RPMI-7951 C357(1.29)  LDD3410  [1]

References

1 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
2 Discovery of a Cell-Active SuTEx Ligand of Prostaglandin Reductase 2. Chembiochem. 2021 Jun 15;22(12):2134-2139. doi: 10.1002/cbic.202000879. Epub 2021 Apr 29.
3 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.
4 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060