Details of the Target

General Information of Target

Target ID LDTP08784
Target Name Rho guanine nucleotide exchange factor 28 (ARHGEF28)
Gene Name ARHGEF28
Gene ID 64283
Synonyms
KIAA1998; RGNEF; Rho guanine nucleotide exchange factor 28; 190 kDa guanine nucleotide exchange factor; p190-RhoGEF; p190RhoGEF; Rho guanine nucleotide exchange factor
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MELSCSEAPLYGQMMIYAKFDKNVYLPEDAEFYFTYDGSHQRHVMIAERIEDNVLQSSVP
GHGLQETVTVSVCLCSEGYSPVTMGSGSVTYVDNMACRLARLLVTQANRLTACSHQTLLT
PFALTAGALPALDEELVLALTHLELPLEWTVLGSSSLEVSSHRESLLHLAMRWGLAKLSQ
FFLCLPGGVQALALPNEEGATPLDLALREGHSKLVEDVTNFQGRWSPSFSRVQLSEEASL
HYIHSSETLTLTLNHTAEHLLEADIKLFRKYFWDRAFLVKAFEPEARPEERTAMPSSGAE
TEEEIKNSVSSRSAAEKEDIKRVKSLVVQHNEHEDQHSLDLDRSFDILKKSKPPSTLLAA
GRLSDMLNGGDEVYANCMVIDQVGDLDISYINIEGITATTSPESRGCTLWPQSSKHTLPT
ETSPSVYPLSENVEGTAHTEAQQSFMSPSSSCASNLNLSFGWHGFEKEQSHLKKRSSSLD
ALDADSEGEGHSEPSHICYTPGSQSSSRTGIPSGDELDSFETNTEPDFNISRAESLPLSS
NLQSKESLLSGVRSRSYSCSSPKISLGKTRLVRELTVCSSSEEQRAYSLSEPPRENRIQE
EEWDKYIIPAKSESEKYKVSRTFSFLMNRMTSPRNKSKTKSKDAKDKEKLNRHQFAPGTF
SGVLQCLVCDKTLLGKESLQCSNCNANVHKGCKDAAPACTKKFQEKYNKNKPQTILGNSS
FRDIPQPGLSLHPSSSVPVGLPTGRRETVGQVHPLSRSVPGTTLESFRRSATSLESESDH
NSCRSRSHSDELLQSMGSSPSTESFIMEDVVDSSLWSDLSSDAQEFEAESWSLVVDPSFC
NRQEKDVIKRQDVIFELMQTEMHHIQTLFIMSEIFRKGMKEELQLDHSTVDKIFPCLDEL
LEIHRHFFYSMKERRQESCAGSDRNFVIDRIGDILVQQFSEENASKMKKIYGEFCCHHKE
AVNLFKELQQNKKFQNFIKLRNSNLLARRRGIPECILLVTQRITKYPVLVERILQYTKER
TEEHKDLRKALCLIKDMIATVDLKVNEYEKNQKWLEILNKIENKTYTKLKNGHVFRKQAL
MSEERTLLYDGLVYWKTATGRFKDILALLLTDVLLFLQEKDQKYIFAAVDQKPSVISLQK
LIAREVANEERGMFLISASSAGPEMYEIHTNSKEERNNWMRRIQQAVESCPEEKGGRTSE
SDEDKRKAEARVAKIQQCQEILTNQDQQICAYLEEKLHIYAELGELSGFEDVHLEPHLLI
KPDPGEPPQAASLLAAALKEAESLQVAVKASQMGAVSQSCEDSCGDSVLADTLSSHDVPG
SPTASLVTGGREGRGCSDVDPGIQGVVTDLAVSDAGEKVECRNFPGSSQSEIIQAIQNLT
RLLYSLQAALTIQDSHIEIHRLVLQQQEGLSLGHSILRGGPLQDQKSRDADRQHEELANV
HQLQHQLQQEQRRWLRRCEQQQRAQATRESWLQERERECQSQEELLLRSRGELDLQLQEY
QHSLERLREGQRLVEREQARMRAQQSLLGHWKHGRQRSLPAVLLPGGPEVMELNRSESLC
HENSFFINEALVQMSFNTFNKLNPSVIHQDATYPTTQSHSDLVRTSEHQVDLKVDPSQPS
NVSHKLWTAAGSGHQILPFHESSKDSCKNDLDTSHTESPTPHDSNSHRPQLQAFITEAKL
NLPTRTMTRQDGETGDGAKENIVYL
Target Bioclass
Other
Subcellular location
Cytoplasm
Function
Functions as a RHOA-specific guanine nucleotide exchange factor regulating signaling pathways downstream of integrins and growth factor receptors. Functions in axonal branching, synapse formation and dendritic morphogenesis. Functions also in focal adhesion formation, cell motility and B-lymphocytes activation. May regulate NEFL expression and aggregation and play a role in apoptosis.
Uniprot ID
Q8N1W1
Ensemble ID
ENST00000296794.10
HGNC ID
HGNC:30322

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
A375 SNV: p.E66K DBIA    Probe Info 
CHL1 SNV: p.H211Y .
FADU SNV: p.V1339M .
HCT116 SNV: p.A1213P .
KASUMI2 SNV: p.R988Ter .
LNCaP clone FGC SNV: p.Q1292H .
MCC13 SNV: p.V1318L
Substitution: p.A191V		 .
MDAMB453 SNV: p.E825Q .
MEWO SNV: p.P526S DBIA    Probe Info 
MOLT4 SNV: p.I1702V .
NCIH1048 SNV: p.R532G .
NCIH1793 SNV: p.K568R DBIA    Probe Info 
P31FUJ SNV: p.H1238Q .
REH SNV: p.G1345S .
RKO SNV: p.Y1016H .
RL952 SNV: p.R475I .
SKN SNV: p.D1202N DBIA    Probe Info 
SNGM SNV: p.K1205T .
SW756 SNV: p.S734C; p.R924S .
TE1 SNV: p.L102M .
TE4 SNV: p.V1339M .
U118MG SNV: p.P742Q DBIA    Probe Info 

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
STPyne
 Probe Info  		K973(5.26); K979(8.33)  LDD0277  [1]
DBIA
 Probe Info  		C559(2.10)  LDD3314  [2]
BTD
 Probe Info  		C1458(0.42); C1032(0.59)  LDD2109  [3]
NAIA_4
 Probe Info  		C498(0.00); C578(0.00); C783(0.00); C1336(0.00)  LDD2226  [4]
NAIA_5
 Probe Info  		N.A.  LDD2225  [4]
WYneN
 Probe Info  		C1032(0.00); C896(0.00)  LDD0021  [5]
IPM
 Probe Info  		C783(0.00); C559(0.00); C1479(0.00)  LDD0147  [6]
TFBX
 Probe Info  		N.A.  LDD0148  [6]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0259  AC14 HEK-293T C559(1.07)  LDD1512  [7]
 LDCM0270  AC15 HEK-293T C559(0.86); C919(1.28)  LDD1513  [7]
 LDCM0281  AC21 HEK-293T C559(1.23)  LDD1520  [7]
 LDCM0282  AC22 HEK-293T C559(1.04)  LDD1521  [7]
 LDCM0283  AC23 HEK-293T C559(0.90); C919(1.01)  LDD1522  [7]
 LDCM0284  AC24 HEK-293T C919(0.98)  LDD1523  [7]
 LDCM0289  AC29 HEK-293T C559(1.10)  LDD1528  [7]
 LDCM0291  AC30 HEK-293T C559(0.88)  LDD1530  [7]
 LDCM0292  AC31 HEK-293T C559(0.86); C919(1.08)  LDD1531  [7]
 LDCM0293  AC32 HEK-293T C919(0.91)  LDD1532  [7]
 LDCM0298  AC37 HEK-293T C559(1.08)  LDD1537  [7]
 LDCM0299  AC38 HEK-293T C559(0.87)  LDD1538  [7]
 LDCM0300  AC39 HEK-293T C559(0.84); C919(1.02)  LDD1539  [7]
 LDCM0302  AC40 HEK-293T C919(0.84)  LDD1541  [7]
 LDCM0307  AC45 HEK-293T C559(0.97)  LDD1546  [7]
 LDCM0308  AC46 HEK-293T C559(1.20)  LDD1547  [7]
 LDCM0309  AC47 HEK-293T C559(0.80); C919(1.22)  LDD1548  [7]
 LDCM0310  AC48 HEK-293T C919(0.96)  LDD1549  [7]
 LDCM0312  AC5 HEK-293T C559(0.87)  LDD1551  [7]
 LDCM0316  AC53 HEK-293T C559(1.04)  LDD1555  [7]
 LDCM0317  AC54 HEK-293T C559(0.92)  LDD1556  [7]
 LDCM0318  AC55 HEK-293T C559(0.75); C919(1.01)  LDD1557  [7]
 LDCM0319  AC56 HEK-293T C919(0.97)  LDD1558  [7]
 LDCM0323  AC6 HEK-293T C559(0.97)  LDD1562  [7]
 LDCM0325  AC61 HEK-293T C559(1.09)  LDD1564  [7]
 LDCM0326  AC62 HEK-293T C559(1.14)  LDD1565  [7]
 LDCM0327  AC63 HEK-293T C559(0.87); C919(1.10)  LDD1566  [7]
 LDCM0328  AC64 HEK-293T C919(1.04)  LDD1567  [7]
 LDCM0334  AC7 HEK-293T C559(0.66); C919(1.10)  LDD1568  [7]
 LDCM0345  AC8 HEK-293T C919(0.90)  LDD1569  [7]
 LDCM0248  AKOS034007472 HEK-293T C559(1.21)  LDD1511  [7]
 LDCM0275  AKOS034007705 HEK-293T C919(0.89)  LDD1514  [7]
 LDCM0632  CL-Sc Hep-G2 C783(0.79); C995(0.56)  LDD2227  [4]
 LDCM0368  CL10 HEK-293T C559(0.90)  LDD1572  [7]
 LDCM0371  CL102 HEK-293T C559(0.82)  LDD1575  [7]
 LDCM0375  CL106 HEK-293T C559(1.32)  LDD1579  [7]
 LDCM0379  CL11 HEK-293T C559(0.82); C919(0.93)  LDD1583  [7]
 LDCM0380  CL110 HEK-293T C559(0.82)  LDD1584  [7]
 LDCM0384  CL114 HEK-293T C559(0.83)  LDD1588  [7]
 LDCM0388  CL118 HEK-293T C559(0.86)  LDD1592  [7]
 LDCM0390  CL12 HEK-293T C919(0.86)  LDD1594  [7]
 LDCM0393  CL122 HEK-293T C559(1.04)  LDD1597  [7]
 LDCM0397  CL126 HEK-293T C559(0.99)  LDD1601  [7]
 LDCM0401  CL14 HEK-293T C559(0.89)  LDD1605  [7]
 LDCM0407  CL2 HEK-293T C559(0.81)  LDD1611  [7]
 LDCM0409  CL21 HEK-293T C559(0.87)  LDD1613  [7]
 LDCM0410  CL22 HEK-293T C559(1.18)  LDD1614  [7]
 LDCM0411  CL23 HEK-293T C559(0.75); C919(0.99)  LDD1615  [7]
 LDCM0412  CL24 HEK-293T C919(0.73)  LDD1616  [7]
 LDCM0414  CL26 HEK-293T C559(1.09)  LDD1618  [7]
 LDCM0422  CL33 HEK-293T C559(1.01)  LDD1626  [7]
 LDCM0423  CL34 HEK-293T C559(0.93)  LDD1627  [7]
 LDCM0424  CL35 HEK-293T C559(0.70); C919(1.12)  LDD1628  [7]
 LDCM0425  CL36 HEK-293T C919(0.74)  LDD1629  [7]
 LDCM0435  CL45 HEK-293T C559(0.99)  LDD1639  [7]
 LDCM0436  CL46 HEK-293T C559(1.12)  LDD1640  [7]
 LDCM0437  CL47 HEK-293T C559(0.93); C919(0.78)  LDD1641  [7]
 LDCM0438  CL48 HEK-293T C919(0.83)  LDD1642  [7]
 LDCM0441  CL50 HEK-293T C559(1.15)  LDD1645  [7]
 LDCM0448  CL57 HEK-293T C559(1.29)  LDD1651  [7]
 LDCM0449  CL58 HEK-293T C559(0.88)  LDD1652  [7]
 LDCM0450  CL59 HEK-293T C559(0.78); C919(1.01)  LDD1653  [7]
 LDCM0452  CL60 HEK-293T C919(0.99)  LDD1655  [7]
 LDCM0454  CL62 HEK-293T C559(0.94)  LDD1657  [7]
 LDCM0461  CL69 HEK-293T C559(1.03)  LDD1664  [7]
 LDCM0463  CL70 HEK-293T C559(0.94)  LDD1666  [7]
 LDCM0464  CL71 HEK-293T C559(0.83); C919(0.88)  LDD1667  [7]
 LDCM0465  CL72 HEK-293T C919(0.73)  LDD1668  [7]
 LDCM0467  CL74 HEK-293T C559(1.04)  LDD1670  [7]
 LDCM0475  CL81 HEK-293T C559(0.97)  LDD1678  [7]
 LDCM0476  CL82 HEK-293T C559(0.92)  LDD1679  [7]
 LDCM0477  CL83 HEK-293T C559(0.86); C919(0.95)  LDD1680  [7]
 LDCM0478  CL84 HEK-293T C919(1.09)  LDD1681  [7]
 LDCM0480  CL86 HEK-293T C559(0.85)  LDD1683  [7]
 LDCM0484  CL9 HEK-293T C559(0.97)  LDD1687  [7]
 LDCM0488  CL93 HEK-293T C559(0.96)  LDD1691  [7]
 LDCM0489  CL94 HEK-293T C559(1.04)  LDD1692  [7]
 LDCM0490  CL95 HEK-293T C559(0.87); C919(1.53)  LDD1693  [7]
 LDCM0491  CL96 HEK-293T C919(1.08)  LDD1694  [7]
 LDCM0493  CL98 HEK-293T C559(0.95)  LDD1696  [7]
 LDCM0427  Fragment51 HEK-293T C559(1.14)  LDD1631  [7]
 LDCM0022  KB02 8305C C94(2.53)  LDD2248  [2]
 LDCM0023  KB03 MDA-MB-231 C1032(19.67)  LDD1701  [3]
 LDCM0024  KB05 IGR37 C559(2.10)  LDD3314  [2]
 LDCM0528  N-(4-bromophenyl)-2-cyano-N-phenylacetamide MDA-MB-231 C919(0.65)  LDD2121  [3]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C1458(0.42); C1032(0.59)  LDD2109  [3]
 LDCM0530  Nucleophilic fragment 28a MDA-MB-231 C1458(0.63)  LDD2123  [3]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C1458(0.95)  LDD2136  [3]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Dihydrolipoyllysine-residue succinyltransferase component of 2-oxoglutarate dehydrogenase complex, mitochondrial (DLST) 2-oxoacid dehydrogenase family P36957
Serine/threonine-protein kinase Nek7 (NEK7) NEK Ser/Thr protein kinase family Q8TDX7
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Calreticulin (CALR) Calreticulin family P27797
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Cancer/testis antigen 1 (CTAG1A; CTAG1B) CTAG/PCC1 family P78358

References

1 A Paal-Knorr agent for chemoproteomic profiling of targets of isoketals in cells. Chem Sci. 2021 Oct 15;12(43):14557-14563. doi: 10.1039/d1sc02230j. eCollection 2021 Nov 10.
Mass spectrometry data entry: PXD028270
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 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761
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 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
6 Chemoproteomic Profiling by Cysteine Fluoroalkylation Reveals Myrocin G as an Inhibitor of the Nonhomologous End Joining DNA Repair Pathway. J Am Chem Soc. 2021 Dec 8;143(48):20332-20342. doi: 10.1021/jacs.1c09724. Epub 2021 Nov 24.
Mass spectrometry data entry: PXD029255
7 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