General Information of Target

Target ID LDTP09399
Target Name Phosphatidylinositol 3,4,5-trisphosphate-dependent Rac exchanger 1 protein (PREX1)
Gene Name PREX1
Gene ID 57580
Synonyms
KIAA1415; Phosphatidylinositol 3,4,5-trisphosphate-dependent Rac exchanger 1 protein; P-Rex1; PtdIns(3,4,5)-dependent Rac exchanger 1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MEAPSGSEPGGDGAGDCAHPDPRAPGAAAPSSGPGPCAAARESERQLRLRLCVLNEILGT
ERDYVGTLRFLQSAFLHRIRQNVADSVEKGLTEENVKVLFSNIEDILEVHKDFLAALEYC
LHPEPQSQHELGNVFLKFKDKFCVYEEYCSNHEKALRLLVELNKIPTVRAFLLSCMLLGG
RKTTDIPLEGYLLSPIQRICKYPLLLKELAKRTPGKHPDHPAVQSALQAMKTVCSNINET
KRQMEKLEALEQLQSHIEGWEGSNLTDICTQLLLQGTLLKISAGNIQERAFFLFDNLLVY
CKRKSRVTGSKKSTKRTKSINGSLYIFRGRINTEVMEVENVEDGTADYHSNGYTVTNGWK
IHNTAKNKWFVCMAKTAEEKQKWLDAIIREREQRESLKLGMERDAYVMIAEKGEKLYHMM
MNKKVNLIKDRRRKLSTVPKCFLGNEFVAWLLEIGEISKTEEGVNLGQALLENGIIHHVS
DKHQFKNEQVMYRFRYDDGTYKARSELEDIMSKGVRLYCRLHSLYTPVIKDRDYHLKTYK
SVLPGSKLVDWLLAQGDCQTREEAVALGVGLCNNGFMHHVLEKSEFRDESQYFRFHADEE
MEGTSSKNKQLRNDFKLVENILAKRLLILPQEEDYGFDIEEKNKAVVVKSVQRGSLAEVA
GLQVGRKIYSINEDLVFLRPFSEVESILNQSFCSRRPLRLLVATKAKEIIKIPDQPDTLC
FQIRGAAPPYVYAVGRGSEAMAAGLCAGQCILKVNGSNVMNDGAPEVLEHFQAFRSRREE
ALGLYQWIYHTHEDAQEARASQEASTEDPSGEQAQEEDQADSAFPLLSLGPRLSLCEDSP
MVTLTVDNVHLEHGVVYEYVSTAGVRCHVLEKIVEPRGCFGLTAKILEAFAANDSVFVEN
CRRLMALSSAIVTMPHFEFRNICDTKLESIGQRIACYQEFAAQLKSRVSPPFKQAPLEPH
PLCGLDFCPTNCHINLMEVSYPKTTPSVGRSFSIRFGRKPSLIGLDPEQGHLNPMSYTQH
CITTMAAPSWKCLPAAEGDPQGQGLHDGSFGPASGTLGQEDRGLSFLLKQEDREIQDAYL
QLFTKLDVALKEMKQYVTQINRLLSTITEPTSGGSCDASLAEEASSLPLVSEESEMDRSD
HGGIKKVCFKVAEEDQEDSGHDTMSYRDSYSECNSNRDSVLSYTSVRSNSSYLGSDEMGS
GDELPCDMRIPSDKQDKLHGCLEHLFNQVDSINALLKGPVMSRAFEETKHFPMNHSLQEF
KQKEECTIRGRSLIQISIQEDPWNLPNSIKTLVDNIQRYVEDGKNQLLLALLKCTDTELQ
LRRDAIFCQALVAAVCTFSKQLLAALGYRYNNNGEYEESSRDASRKWLEQVAATGVLLHC
QSLLSPATVKEERTMLEDIWVTLSELDNVTFSFKQLDENYVANTNVFYHIEGSRQALKVI
FYLDSYHFSKLPSRLEGGASLRLHTALFTKVLENVEGLPSPGSQAAEDLQQDINAQSLEK
VQQYYRKLRAFYLERSNLPTDASTTAVKIDQLIRPINALDELCRLMKSFVHPKPGAAGSV
GAGLIPISSELCYRLGACQMVMCGTGMQRSTLSVSLEQAAILARSHGLLPKCIMQATDIM
RKQGPRVEILAKNLRVKDQMPQGAPRLYRLCQPPVDGDL
Target Bioclass
Other
Subcellular location
Cytoplasm, cytosol
Function
Functions as a RAC guanine nucleotide exchange factor (GEF), which activates the 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. May function downstream of heterotrimeric G proteins in neutrophils.
Uniprot ID
Q8TCU6
Ensemble ID
ENST00000371941.4
HGNC ID
HGNC:32594

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
A3KAW Deletion: p.A29PfsTer105 .
AU565 SNV: p.N643K DBIA    Probe Info 
HUH28 SNV: p.A115T .
IGR1 SNV: p.D717N DBIA    Probe Info 
IGROV1 SNV: p.H578Y; p.V1229A; p.R1534C DBIA    Probe Info 
KMRC3 SNV: p.W787C .
LS180 SNV: p.I911V; p.A1526T .
MELJUSO SNV: p.P986T DBIA    Probe Info 
MFE319 SNV: p.S1569P .
MOLT4 SNV: p.A1616V .
NALM6 SNV: p.D1207V DBIA    Probe Info 
NCIH1155 SNV: p.S458N .
NCIH2172 SNV: p.R990M .
PC14 SNV: p.E1135D .
PC9 SNV: p.E1135D .
PF382 SNV: p.R995H DBIA    Probe Info 
SNU245 SNV: p.R1515L .
SNU308 SNV: p.R778P .
SW1271 SNV: p.D717Y .
SW480 SNV: p.L1193F .
TYKNU SNV: p.S1242T .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 8 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
Probe 1
 Probe Info 
Y406(18.21); Y492(36.99); Y501(15.24); Y592(25.01)  LDD3495  [1]
DBIA
 Probe Info 
C37(2.57); C936(1.27)  LDD3332  [2]
AHL-Pu-1
 Probe Info 
C52(4.21)  LDD0171  [3]
IA-alkyne
 Probe Info 
C1266(9.45)  LDD0516  [4]
N1
 Probe Info 
D1302(0.00); Y1299(0.00)  LDD0245  [5]
Lodoacetamide azide
 Probe Info 
N.A.  LDD0037  [6]
IPM
 Probe Info 
N.A.  LDD2156  [7]
NAIA_5
 Probe Info 
C301(0.00); C175(0.00); C720(0.00); C441(0.00)  LDD2223  [8]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0026  4SU-RNA+native RNA DM93 C52(4.21)  LDD0171  [3]
 LDCM0200  BPK-25 T cell C1266(9.45)  LDD0516  [4]
 LDCM0632  CL-Sc Hep-G2 C1612(20.00); C1173(20.00); C746(20.00); C1543(2.61)  LDD2227  [8]
 LDCM0634  CY-0357 Hep-G2 C1173(2.09); C17(0.93); C37(0.87); C1206(0.50)  LDD2228  [8]
 LDCM0203  EV-96 T cell C1266(4.34)  LDD0523  [4]
 LDCM0204  EV-97 T cell C1266(16.45)  LDD0524  [4]
 LDCM0022  KB02 T cell C37(5.76); C1266(20.00)  LDD1703  [4]
 LDCM0023  KB03 42-MG-BA C37(2.22); C879(2.19)  LDD2661  [2]
 LDCM0024  KB05 MKN45 C37(2.57); C936(1.27)  LDD3332  [2]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Serine/threonine-protein kinase mTOR (MTOR) PI3/PI4-kinase family P42345
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Rapamycin-insensitive companion of mTOR (RICTOR) RICTOR family Q6R327
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Regulatory-associated protein of mTOR (RPTOR) WD repeat RAPTOR family Q8N122

References

1 An Azo Coupling-Based Chemoproteomic Approach to Systematically Profile the Tyrosine Reactivity in the Human Proteome. Anal Chem. 2021 Jul 27;93(29):10334-10342. doi: 10.1021/acs.analchem.1c01935. Epub 2021 Jul 12.
2 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
3 Chemoproteomic capture of RNA binding activity in living cells. Nat Commun. 2023 Oct 7;14(1):6282. doi: 10.1038/s41467-023-41844-z.
Mass spectrometry data entry: PXD044625
4 An Activity-Guided Map of Electrophile-Cysteine Interactions in Primary Human T Cells. Cell. 2020 Aug 20;182(4):1009-1026.e29. doi: 10.1016/j.cell.2020.07.001. Epub 2020 Jul 29.
5 Cyclopropenone, Cyclopropeniminium Ion, and Cyclopropenethione as Novel Electrophilic Warheads for Potential Target Discovery of Triple-Negative Breast Cancer. J Med Chem. 2023 Feb 23;66(4):2851-2864. doi: 10.1021/acs.jmedchem.2c01889. Epub 2023 Feb 10.
6 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
7 Benchmarking Cleavable Biotin Tags for Peptide-Centric Chemoproteomics. J Proteome Res. 2022 May 6;21(5):1349-1358. doi: 10.1021/acs.jproteome.2c00174. Epub 2022 Apr 25.
Mass spectrometry data entry: PXD031019
8 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