General Information of Target

Target ID LDTP09756
Target Name Rap guanine nucleotide exchange factor 4 (RAPGEF4)
Gene Name RAPGEF4
Gene ID 11069
Synonyms
CGEF2; EPAC2; Rap guanine nucleotide exchange factor 4; Exchange factor directly activated by cAMP 2; Exchange protein directly activated by cAMP 2; EPAC 2; cAMP-regulated guanine nucleotide exchange factor II; cAMP-GEFII
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MDDWKPSPLIKPFGARKKRSWYLTWKYKLTNQRALRRFCQTGAVLFLLVTVIVNIKLILD
TRRAISEANEDPEPEQDYDEALGRLEPPRRRGSGPRRVLDVEVYSSRSKVYVAVDGTTVL
EDEAREQGRGIHVIVLNQATGHVMAKRVFDTYSPHEDEAMVLFLNMVAPGRVLICTVKDE
GSFHLKDTAKALLRSLGSQAGPALGWRDTWAFVGRKGGPVFGEKHSKSPALSSWGDPVLL
KTDVPLSSAEEAECHWADTELNRRRRRFCSKVEGYGSVCSCKDPTPIEFSPDPLPDNKVL
NVPVAVIAGNRPNYLYRMLRSLLSAQGVSPQMITVFIDGYYEEPMDVVALFGLRGIQHTP
ISIKNARVSQHYKASLTATFNLFPEAKFAVVLEEDLDIAVDFFSFLSQSIHLLEEDDSLY
CISAWNDQGYEHTAEDPALLYRVETMPGLGWVLRRSLYKEELEPKWPTPEKLWDWDMWMR
MPEQRRGRECIIPDVSRSYHFGIVGLNMNGYFHEAYFKKHKFNTVPGVQLRNVDSLKKEA
YEVEVHRLLSEAEVLDHSKNPCEDSFLPDTEGHTYVAFIRMEKDDDFTTWTQLAKCLHIW
DLDVRGNHRGLWRLFRKKNHFLMVGVPASPYSVKKPPSVTPIFLEPPPKEEGAPGAPEQT
Target Type
Literature-reported
Target Bioclass
Other
Subcellular location
Cytoplasm
Function
Guanine nucleotide exchange factor (GEF) for RAP1A, RAP1B and RAP2A small GTPases that is activated by binding cAMP. Seems not to activate RAB3A. Involved in cAMP-dependent, PKA-independent exocytosis through interaction with RIMS2.
TTD ID
T74607
Uniprot ID
Q8WZA2
DrugMap ID
TTOS63B
Ensemble ID
ENST00000397081.8
HGNC ID
HGNC:16626
ChEMBL ID
CHEMBL2029198

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
22RV1 SNV: p.Y150Ter .
COLO792 SNV: p.H359Y .
EFO27 SNV: p.T106A .
G361 SNV: p.R151Ter .
HCT116 SNV: p.R432Ter; p.L619I .
HEC1 SNV: p.A213V .
HT SNV: p.D449V .
KPL1 SNV: p.Y986F .
KYM1 SNV: p.S97N .
LN18 SNV: p.I373L .
LNCaP clone FGC SNV: p.D595G .
LS123 Substitution: p.H8P .
MEWO SNV: p.E604K .
MOLT4 Substitution: p.G388E .
P31FUJ SNV: p.Y227C .
PATU8988T SNV: p.T809I .
SH4 SNV: p.G337D .
TKKK SNV: p.I397T .
TOV21G SNV: p.E295Ter .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info 
C443(1.41)  LDD2254  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 A2780 C443(1.41)  LDD2254  [1]
 LDCM0023  KB03 A2780 C443(2.17)  LDD2671  [1]
 LDCM0024  KB05 A2780 C443(2.15)  LDD3088  [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