Details of the Target

General Information of Target

Target ID LDTP07894
Target Name Phosphatidylinositol 3,4,5-trisphosphate-dependent Rac exchanger 2 protein (PREX2)
Gene Name PREX2
Gene ID 80243
Synonyms
DEPDC2; Phosphatidylinositol 3,4,5-trisphosphate-dependent Rac exchanger 2 protein; P-Rex2; PtdIns(3,4,5)-dependent Rac exchanger 2; DEP domain-containing protein 2
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSEDSRGDSRAESAKDLEKQLRLRVCVLSELQKTERDYVGTLEFLVSAFLHRMNQCAASK
VDKNVTEETVKMLFSNIEDILAVHKEFLKVVEECLHPEPNAQQEVGTCFLHFKDKFRIYD
EYCSNHEKAQKLLLELNKIRTIRTFLLNCMLLGGRKNTDVPLEGYLVTPIQRICKYPLIL
KELLKRTPRKHSDYAAVMEALQAMKAVCSNINEAKRQMEKLEVLEEWQSHIEGWEGSNIT
DTCTEMLMCGVLLKISSGNIQERVFFLFDNLLVYCKRKHRRLKNSKASTDGHRYLFRGRI
NTEVMEVENVDDGTADFHSSGHIVVNGWKIHNTAKNKWFVCMAKTPEEKHEWFEAILKER
ERRKGLKLGMEQDTWVMISEQGEKLYKMMCRQGNLIKDRKRKLTTFPKCFLGSEFVSWLL
EIGEIHRPEEGVHLGQALLENGIIHHVTDKHQFKPEQMLYRFRYDDGTFYPRNEMQDVIS
KGVRLYCRLHSLFTPVIRDKDYHLRTYKSVVMANKLIDWLIAQGDCRTREEAMIFGVGLC
DNGFMHHVLEKSEFKDEPLLFRFFSDEEMEGSNMKHRLMKHDLKVVENVIAKSLLIKSNE
GSYGFGLEDKNKVPIIKLVEKGSNAEMAGMEVGKKIFAINGDLVFMRPFNEVDCFLKSCL
NSRKPLRVLVSTKPRETVKIPDSADGLGFQIRGFGPSVVHAVGRGTVAAAAGLHPGQCII
KVNGINVSKETHASVIAHVTACRKYRRPTKQDSIQWVYNSIESAQEDLQKSHSKPPGDEA
GDAFDCKVEEVIDKFNTMAIIDGKKEHVSLTVDNVHLEYGVVYEYDSTAGIKCNVVEKMI
EPKGFFSLTAKILEALAKSDEHFVQNCTSLNSLNEVIPTDLQSKFSALCSERIEHLCQRI
SSYKKFSRVLKNRAWPTFKQAKSKISPLHSSDFCPTNCHVNVMEVSYPKTSTSLGSAFGV
QLDSRKHNSHDKENKSSEQGKLSPMVYIQHTITTMAAPSGLSLGQQDGHGLRYLLKEEDL
ETQDIYQKLLGKLQTALKEVEMCVCQIDDLLSSITYSPKLERKTSEGIIPTDSDNEKGER
NSKRVCFNVAGDEQEDSGHDTISNRDSYSDCNSNRNSIASFTSICSSQCSSYFHSDEMDS
GDELPLSVRISHDKQDKIHSCLEHLFSQVDSITNLLKGQAVVRAFDQTKYLTPGRGLQEF
QQEMEPKLSCPKRLRLHIKQDPWNLPSSVRTLAQNIRKFVEEVKCRLLLALLEYSDSETQ
LRRDMVFCQTLVATVCAFSEQLMAALNQMFDNSKENEMETWEASRRWLDQIANAGVLFHF
QSLLSPNLTDEQAMLEDTLVALFDLEKVSFYFKPSEEEPLVANVPLTYQAEGSRQALKVY
FYIDSYHFEQLPQRLKNGGGFKIHPVLFAQALESMEGYYYRDNVSVEEFQAQINAASLEK
VKQYNQKLRAFYLDKSNSPPNSTSKAAYVDKLMRPLNALDELYRLVASFIRSKRTAACAN
TACSASGVGLLSVSSELCNRLGACHIIMCSSGVHRCTLSVTLEQAIILARSHGLPPRYIM
QATDVMRKQGARVQNTAKNLGVRDRTPQSAPRLYKLCEPPPPAGEE
Target Bioclass
Other
Function
Functions as a RAC1 guanine nucleotide exchange factor (GEF), activating Rac proteins by exchanging bound GDP for free GTP. Its activity is synergistically activated by phosphatidylinositol 3,4,5-trisphosphate and the beta gamma subunits of heterotrimeric G protein. Mediates the activation of RAC1 in a PI3K-dependent manner. May be an important mediator of Rac signaling, acting directly downstream of both G protein-coupled receptors and phosphoinositide 3-kinase.
Uniprot ID
Q70Z35
Ensemble ID
ENST00000288368.5
HGNC ID
HGNC:22950

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CALU6 SNV: p.E262Ter .
CCK81 SNV: p.Y1190H .
CHL1 SNV: p.A11T DBIA    Probe Info 
DU145 SNV: p.T141R; p.A315G; p.D1564Y .
FTC133 SNV: p.L147S .
HCC15 SNV: p.S983I .
HCC1806 SNV: p.E1241V .
HCT116 Deletion: p.S565RfsTer10 .
HCT15 SNV: p.C1161Y .
HEPG2 SNV: p.L50V .
HS936T SNV: p.E1481K .
HT115 SNV: p.K131Q; p.P1475S .
ICC12 SNV: p.T187S; p.T1501P .
IGR1 Substitution: p.V223N .
IGROV1 SNV: p.R1195Ter DBIA    Probe Info 
JHH7 SNV: p.I231S .
LS513 SNV: p.Q898H .
MEWO SNV: p.L146F DBIA    Probe Info 
NCIH1299 SNV: p.C243F .
NCIH1793 SNV: p.K71N .
NCIH2286 SNV: p.M1415I .
PF382 SNV: p.S1120P .
RKO Deletion: p.S565RfsTer10 .
SAOS2 SNV: p.S809N .
SW1116 SNV: p.M569I .
TF1 Deletion: p.S565RfsTer10 .
U2OS SNV: p.H322Y .

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  		C26(1.52)  LDD3323  [1]
IA-alkyne
 Probe Info  		N.A.  LDD2241  [2]
IPM
 Probe Info  		N.A.  LDD0005  [3]
NAIA_5
 Probe Info  		C174(0.00); C341(0.00)  LDD2223  [4]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C26(1.12)  LDD1507  [5]
 LDCM0237  AC12 HEK-293T C26(1.06)  LDD1510  [5]
 LDCM0276  AC17 HEK-293T C26(1.04)  LDD1515  [5]
 LDCM0280  AC20 HEK-293T C26(0.94)  LDD1519  [5]
 LDCM0285  AC25 HEK-293T C26(1.19)  LDD1524  [5]
 LDCM0288  AC28 HEK-293T C26(0.91)  LDD1527  [5]
 LDCM0294  AC33 HEK-293T C26(0.82)  LDD1533  [5]
 LDCM0297  AC36 HEK-293T C26(0.99)  LDD1536  [5]
 LDCM0301  AC4 HEK-293T C26(0.91)  LDD1540  [5]
 LDCM0303  AC41 HEK-293T C26(1.19)  LDD1542  [5]
 LDCM0306  AC44 HEK-293T C26(0.93)  LDD1545  [5]
 LDCM0311  AC49 HEK-293T C26(1.05)  LDD1550  [5]
 LDCM0315  AC52 HEK-293T C26(0.97)  LDD1554  [5]
 LDCM0320  AC57 HEK-293T C26(1.14)  LDD1559  [5]
 LDCM0324  AC60 HEK-293T C26(0.85)  LDD1563  [5]
 LDCM0356  AKOS034007680 HEK-293T C26(1.07)  LDD1570  [5]
 LDCM0404  CL17 HEK-293T C26(1.36)  LDD1608  [5]
 LDCM0408  CL20 HEK-293T C26(1.07)  LDD1612  [5]
 LDCM0417  CL29 HEK-293T C26(1.04)  LDD1621  [5]
 LDCM0421  CL32 HEK-293T C26(1.29)  LDD1625  [5]
 LDCM0431  CL41 HEK-293T C26(0.89)  LDD1635  [5]
 LDCM0434  CL44 HEK-293T C26(1.27)  LDD1638  [5]
 LDCM0440  CL5 HEK-293T C26(1.15)  LDD1644  [5]
 LDCM0444  CL53 HEK-293T C26(1.03)  LDD1647  [5]
 LDCM0447  CL56 HEK-293T C26(0.89)  LDD1650  [5]
 LDCM0457  CL65 HEK-293T C26(1.14)  LDD1660  [5]
 LDCM0460  CL68 HEK-293T C26(0.94)  LDD1663  [5]
 LDCM0470  CL77 HEK-293T C26(1.23)  LDD1673  [5]
 LDCM0473  CL8 HEK-293T C26(1.23)  LDD1676  [5]
 LDCM0474  CL80 HEK-293T C26(0.98)  LDD1677  [5]
 LDCM0483  CL89 HEK-293T C26(0.77)  LDD1686  [5]
 LDCM0487  CL92 HEK-293T C26(1.02)  LDD1690  [5]
 LDCM0022  KB02 A101D C372(2.36)  LDD2250  [1]
 LDCM0023  KB03 769-P C897(2.42)  LDD2663  [1]
 LDCM0024  KB05 SKMEL24 C26(1.52)  LDD3323  [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 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
3 A modification-centric assessment tool for the performance of chemoproteomic probes. Nat Chem Biol. 2022 Aug;18(8):904-912. doi: 10.1038/s41589-022-01074-8. Epub 2022 Jul 21.
Mass spectrometry data entry: PXD027758 , PXD027755 , PXD027760 , PXD027762 , PXD027756 , PXD027591 , PXD007149 , PXD030064 , PXD032392 , PXD027789 , PXD027767 , PXD027764
4 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
5 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