Details of the Target

General Information of Target

Target ID LDTP06441
Target Name Rho-related GTP-binding protein RhoH (RHOH)
Gene Name RHOH
Gene ID 399
Synonyms
ARHH; TTF; Rho-related GTP-binding protein RhoH; GTP-binding protein TTF; Translocation three four protein
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MLSSIKCVLVGDSAVGKTSLLVRFTSETFPEAYKPTVYENTGVDVFMDGIQISLGLWDTA
GNDAFRSIRPLSYQQADVVLMCYSVANHNSFLNLKNKWIGEIRSNLPCTPVLVVATQTDQ
REMGPHRASCVNAMEGKKLAQDVRAKGYLECSALSNRGVQQVFECAVRTAVNQARRRNRR
RLFSINECKIF
Target Bioclass
Enzyme
Family
Small GTPase superfamily, Rho family
Subcellular location
Cytoplasm
Function
Negative regulator of hematopoietic progenitor cell proliferation, survival and migration. Critical regulator of thymocyte development and T-cell antigen receptor (TCR) signaling by mediating recruitment and activation of ZAP70. Required for phosphorylation of CD3Z, membrane translocation of ZAP70 and subsequent activation of the ZAP70-mediated pathways. Essential for efficient beta-selection and positive selection by promoting the ZAP70-dependent phosphorylation of the LAT signalosome during pre-TCR and TCR signaling. Crucial for thymocyte maturation during DN3 to DN4 transition and during positive selection. Plays critical roles in mast cell function by facilitating phosphorylation of SYK in Fc epsilon RI-mediated signal transduction. Essential for the phosphorylation of LAT, LCP2, PLCG1 and PLCG2 and for Ca(2+) mobilization in mast cells. Binds GTP but lacks intrinsic GTPase activity and is resistant to Rho-specific GTPase-activating proteins. Inhibits the activation of NF-kappa-B by TNF and IKKB and the activation of CRK/p38 by TNF. Inhibits activities of RAC1, RHOA and CDC42. Negatively regulates leukotriene production in neutrophils.
Uniprot ID
Q15669
Ensemble ID
ENST00000381799.10
HGNC ID
HGNC:686

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C130(77.28)  LDD0209  [1]
IA-alkyne
 Probe Info  		C151(0.00); C165(0.00); C130(0.00)  LDD0167  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0202  EV-93 T cell C108(4.05)  LDD0527  [3]
 LDCM0625  F8 Ramos C130(1.16); C7(0.69); C108(0.91); C151(1.05)  LDD2187  [4]
 LDCM0572  Fragment10 Ramos C130(1.70); C7(0.76); C108(1.34); C151(1.07)  LDD2189  [4]
 LDCM0573  Fragment11 Ramos C130(1.44); C7(0.11); C108(2.42); C151(0.38)  LDD2190  [4]
 LDCM0574  Fragment12 Ramos C130(1.11); C7(1.29); C108(1.39); C151(1.18)  LDD2191  [4]
 LDCM0575  Fragment13 Ramos C130(1.03); C7(1.21); C108(0.93); C151(0.81)  LDD2192  [4]
 LDCM0576  Fragment14 Ramos C130(1.03); C7(0.83); C108(1.95); C151(1.24)  LDD2193  [4]
 LDCM0579  Fragment20 Ramos C130(1.53); C7(1.23); C108(1.62); C151(1.61)  LDD2194  [4]
 LDCM0580  Fragment21 Ramos C130(1.11); C7(0.92); C108(1.05); C151(0.79)  LDD2195  [4]
 LDCM0582  Fragment23 Ramos C130(0.59); C7(0.97); C108(0.68); C151(0.52)  LDD2196  [4]
 LDCM0578  Fragment27 Ramos C130(0.97); C7(0.92); C108(1.15); C151(0.80)  LDD2197  [4]
 LDCM0586  Fragment28 Ramos C130(0.62); C7(0.69); C108(0.74); C151(0.69)  LDD2198  [4]
 LDCM0588  Fragment30 Ramos C130(1.20); C7(1.37); C108(0.90); C151(0.93)  LDD2199  [4]
 LDCM0589  Fragment31 Ramos C130(0.90); C7(0.87); C108(0.99); C151(0.85)  LDD2200  [4]
 LDCM0590  Fragment32 Ramos C130(1.40); C7(0.80); C108(1.48); C151(0.93)  LDD2201  [4]
 LDCM0468  Fragment33 Ramos C130(1.23); C7(1.22); C108(0.89); C151(0.73)  LDD2202  [4]
 LDCM0596  Fragment38 Ramos C130(1.32); C7(1.08); C108(0.74); C151(0.73)  LDD2203  [4]
 LDCM0566  Fragment4 Ramos C130(1.37); C7(0.94); C108(1.12); C151(1.28)  LDD2184  [4]
 LDCM0610  Fragment52 Ramos C130(1.13); C7(1.76); C108(0.80); C151(1.58)  LDD2204  [4]
 LDCM0614  Fragment56 Ramos C130(1.19); C7(1.64); C108(0.98); C151(1.69)  LDD2205  [4]
 LDCM0569  Fragment7 Ramos C130(1.41); C7(0.84); C108(1.77); C151(1.52)  LDD2186  [4]
 LDCM0571  Fragment9 Ramos C130(1.69); C7(0.99); C108(2.20); C165(2.10)  LDD2188  [4]
 LDCM0022  KB02 Ramos 4.58  LDD0431  [5]
 LDCM0023  KB03 Jurkat C130(77.28)  LDD0209  [1]
 LDCM0024  KB05 MONO-MAC-6 C165(1.57)  LDD3335  [6]
 LDCM0131  RA190 MM1.R C108(1.42)  LDD0304  [7]

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
Sulfite oxidase, mitochondrial (SUOX) . P51687
Transporter and channel
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Metaxin-2 (MTX2) Metaxin family O75431
Sortilin-related receptor (SORL1) VPS10-related sortilin family Q92673
Integrin beta-1-binding protein 1 (ITGB1BP1) . O14713
Sodium channel modifier 1 (SCNM1) . Q9BWG6
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Transcription factor 19 (TCF19) . Q9Y242
Other
Click To Hide/Show 5 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Cyclin-H (CCNH) Cyclin family P51946
Protein FAM90A1 (FAM90A1) FAM90 family Q86YD7
Protein ripply1 (RIPPLY1) Ripply family Q0D2K3
IQ motif and ubiquitin-like domain-containing protein (IQUB) . Q8NA54
KN motif and ankyrin repeat domain-containing protein 2 (KANK2) . Q63ZY3

References

1 Covalent Inhibition by a Natural Product-Inspired Latent Electrophile. J Am Chem Soc. 2023 May 24;145(20):11097-11109. doi: 10.1021/jacs.3c00598. Epub 2023 May 15.
2 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
3 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.
4 Site-specific quantitative cysteine profiling with data-independent acquisition-based mass spectrometry. Methods Enzymol. 2023;679:295-322. doi: 10.1016/bs.mie.2022.07.037. Epub 2022 Sep 7.
Mass spectrometry data entry: PXD027578
5 2-Sulfonylpyridines as Tunable, Cysteine-Reactive Electrophiles. J Am Chem Soc. 2020 May 13;142(19):8972-8979. doi: 10.1021/jacs.0c02721. Epub 2020 Apr 29.
6 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
7 Physical and Functional Analysis of the Putative Rpn13 Inhibitor RA190. Cell Chem Biol. 2020 Nov 19;27(11):1371-1382.e6. doi: 10.1016/j.chembiol.2020.08.007. Epub 2020 Aug 27.