Details of the Target

General Information of Target

Target ID LDTP07597
Target Name Inactive rhomboid protein 2 (RHBDF2)
Gene Name RHBDF2
Gene ID 79651
Synonyms
IRHOM2; RHBDL5; RHBDL6; Inactive rhomboid protein 2; iRhom2; Rhomboid 5 homolog 2; Rhomboid family member 2; Rhomboid veinlet-like protein 5; Rhomboid veinlet-like protein 6
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MASADKNGGSVSSVSSSRLQSRKPPNLSITIPPPEKETQAPGEQDSMLPEGFQNRRLKKS
QPRTWAAHTTACPPSFLPKRKNPAYLKSVSLQEPRSRWQESSEKRPGFRRQASLSQSIRK
GAAQWFGVSGDWEGQRQQWQRRSLHHCSMRYGRLKASCQRDLELPSQEAPSFQGTESPKP
CKMPKIVDPLARGRAFRHPEEMDRPHAPHPPLTPGVLSLTSFTSVRSGYSHLPRRKRMSV
AHMSLQAAAALLKGRSVLDATGQRCRVVKRSFAFPSFLEEDVVDGADTFDSSFFSKEEMS
SMPDDVFESPPLSASYFRGIPHSASPVSPDGVQIPLKEYGRAPVPGPRRGKRIASKVKHF
AFDRKKRHYGLGVVGNWLNRSYRRSISSTVQRQLESFDSHRPYFTYWLTFVHVIITLLVI
CTYGIAPVGFAQHVTTQLVLRNKGVYESVKYIQQENFWVGPSSIDLIHLGAKFSPCIRKD
GQIEQLVLRERDLERDSGCCVQNDHSGCIQTQRKDCSETLATFVKWQDDTGPPMDKSDLG
QKRTSGAVCHQDPRTCEEPASSGAHIWPDDITKWPICTEQARSNHTGFLHMDCEIKGRPC
CIGTKGSCEITTREYCEFMHGYFHEEATLCSQVHCLDKVCGLLPFLNPEVPDQFYRLWLS
LFLHAGVVHCLVSVVFQMTILRDLEKLAGWHRIAIIFILSGITGNLASAIFLPYRAEVGP
AGSQFGLLACLFVELFQSWPLLERPWKAFLNLSAIVLFLFICGLLPWIDNIAHIFGFLSG
LLLAFAFLPYITFGTSDKYRKRALILVSLLAFAGLFAALVLWLYIYPINWPWIEHLTCFP
FTSRFCEKYELDQVLH
Target Type
Literature-reported
Target Bioclass
Enzyme
Family
Peptidase S54 family
Subcellular location
Endoplasmic reticulum membrane
Function
Regulates ADAM17 protease, a sheddase of the epidermal growth factor (EGF) receptor ligands and TNF, thereby plays a role in sleep, cell survival, proliferation, migration and inflammation. Does not exhibit any protease activity on its own.
TTD ID
T93711
Uniprot ID
Q6PJF5
DrugMap ID
TTH1ZOP
Ensemble ID
ENST00000313080.8
HGNC ID
HGNC:20788

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 9 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
STPyne
 Probe Info  		K358(10.00)  LDD0277  [1]
BTD
 Probe Info  		C476(0.83)  LDD2117  [2]
IPM
 Probe Info  		C476(1.77)  LDD1702  [2]
DBIA
 Probe Info  		C499(0.95); C508(0.95)  LDD0078  [3]
5E-2FA
 Probe Info  		N.A.  LDD2235  [4]
IA-alkyne
 Probe Info  		N.A.  LDD0162  [5]
VSF
 Probe Info  		N.A.  LDD0007  [6]
Phosphinate-6
 Probe Info  		C147(0.00); C158(0.00)  LDD0018  [7]
NAIA_5
 Probe Info  		C516(0.00); C549(0.00)  LDD2223  [8]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C476(0.83)  LDD2117  [2]
 LDCM0026  4SU-RNA+native RNA HEK-293T C181(2.03)  LDD0372  [9]
 LDCM0020  ARS-1620 HCC44 C499(0.95); C508(0.95)  LDD0078  [3]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C476(1.77)  LDD1702  [2]
 LDCM0625  F8 Ramos C181(0.62)  LDD2187  [10]
 LDCM0572  Fragment10 Ramos C181(1.82)  LDD2189  [10]
 LDCM0573  Fragment11 Ramos C181(2.04); C147(1.51)  LDD2190  [10]
 LDCM0574  Fragment12 Ramos C181(1.04)  LDD2191  [10]
 LDCM0575  Fragment13 Ramos C181(0.95)  LDD2192  [10]
 LDCM0576  Fragment14 Ramos C181(0.50); C147(0.54)  LDD2193  [10]
 LDCM0579  Fragment20 Ramos C181(1.55)  LDD2194  [10]
 LDCM0580  Fragment21 Ramos C181(0.77)  LDD2195  [10]
 LDCM0582  Fragment23 Ramos C181(0.97)  LDD2196  [10]
 LDCM0578  Fragment27 Ramos C181(0.83)  LDD2197  [10]
 LDCM0586  Fragment28 Ramos C181(0.88)  LDD2198  [10]
 LDCM0588  Fragment30 Ramos C181(0.97)  LDD2199  [10]
 LDCM0589  Fragment31 Ramos C181(0.84)  LDD2200  [10]
 LDCM0590  Fragment32 Ramos C181(2.00)  LDD2201  [10]
 LDCM0468  Fragment33 Ramos C181(1.14)  LDD2202  [10]
 LDCM0596  Fragment38 Ramos C181(0.77)  LDD2203  [10]
 LDCM0566  Fragment4 Ramos C181(1.09); C147(1.13)  LDD2184  [10]
 LDCM0610  Fragment52 Ramos C181(1.19)  LDD2204  [10]
 LDCM0614  Fragment56 Ramos C181(1.06)  LDD2205  [10]
 LDCM0569  Fragment7 Ramos C181(1.41); C147(0.44)  LDD2186  [10]
 LDCM0571  Fragment9 Ramos C181(1.44)  LDD2188  [10]
 LDCM0022  KB02 Ramos C181(1.67); C147(0.56)  LDD2182  [10]
 LDCM0023  KB03 Ramos C181(1.09); C147(0.68)  LDD2183  [10]
 LDCM0024  KB05 COLO792 C549(2.64)  LDD3310  [11]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Sulforaphane . D0X4IO

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 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
3 Reimagining high-throughput profiling of reactive cysteines for cell-based screening of large electrophile libraries. Nat Biotechnol. 2021 May;39(5):630-641. doi: 10.1038/s41587-020-00778-3. Epub 2021 Jan 4.
4 Global profiling of functional histidines in live cells using small-molecule photosensitizer and chemical probe relay labelling. Nat Chem. 2024 Jun 4. doi: 10.1038/s41557-024-01545-6. Online ahead of print.
Mass spectrometry data entry: PXD042377
5 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
6 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
7 DFT-Guided Discovery of Ethynyl-Triazolyl-Phosphinates as Modular Electrophiles for Chemoselective Cysteine Bioconjugation and Profiling. Angew Chem Int Ed Engl. 2022 Oct 10;61(41):e202205348. doi: 10.1002/anie.202205348. Epub 2022 Aug 22.
Mass spectrometry data entry: PXD033004
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
9 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
10 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
11 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