Details of the Target

General Information of Target

Target ID LDTP02523
Target Name Retinoic acid receptor beta (RARB)
Gene Name RARB
Gene ID 5915
Synonyms
HAP; NR1B2; Retinoic acid receptor beta; RAR-beta; HBV-activated protein; Nuclear receptor subfamily 1 group B member 2; RAR-epsilon
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MTTSGHACPVPAVNGHMTHYPATPYPLLFPPVIGGLSLPPLHGLHGHPPPSGCSTPSPAT
IETQSTSSEELVPSPPSPLPPPRVYKPCFVCQDKSSGYHYGVSACEGCKGFFRRSIQKNM
IYTCHRDKNCVINKVTRNRCQYCRLQKCFEVGMSKESVRNDRNKKKKETSKQECTESYEM
TAELDDLTEKIRKAHQETFPSLCQLGKYTTNSSADHRVRLDLGLWDKFSELATKCIIKIV
EFAKRLPGFTGLTIADQITLLKAACLDILILRICTRYTPEQDTMTFSDGLTLNRTQMHNA
GFGPLTDLVFTFANQLLPLEMDDTETGLLSAICLICGDRQDLEEPTKVDKLQEPLLEALK
IYIRKRRPSKPHMFPKILMKITDLRSISAKGAERVITLKMEIPGSMPPLIQEMLENSEGH
EPLTPSSSGNTAEHSPSISPSSVENSGVSQSPLVQ
Target Type
Successful
Target Bioclass
Transcription factor
Family
Nuclear hormone receptor family, NR1 subfamily
Subcellular location
Cytoplasm; Nucleus
Function
Receptor for retinoic acid. Retinoic acid receptors bind as heterodimers to their target response elements in response to their ligands, all-trans or 9-cis retinoic acid, and regulate gene expression in various biological processes. The RXR/RAR heterodimers bind to the retinoic acid response elements (RARE) composed of tandem 5'-AGGTCA-3' sites known as DR1-DR5. In the absence or presence of hormone ligand, acts mainly as an activator of gene expression due to weak binding to corepressors. The RXRA/RARB heterodimer can act as a repressor on the DR1 element and as an activator on the DR5 element. In concert with RARG, required for skeletal growth, matrix homeostasis and growth plate function.
TTD ID
T61657
Uniprot ID
P10826
DrugMap ID
TTISP28
Ensemble ID
ENST00000330688.9
HGNC ID
HGNC:9865
ChEMBL ID
CHEMBL2008

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 5 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
TH211
 Probe Info  		Y208(16.87)  LDD0257  [1]
DBIA
 Probe Info  		C203(1.27)  LDD0532  [2]
IA-alkyne
 Probe Info  		C124(0.00); C148(0.00)  LDD0165  [3]
IPM
 Probe Info  		N.A.  LDD2156  [4]
YN-1
 Probe Info  		N.A.  LDD0446  [5]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0215  AC10 HCT 116 C203(1.27)  LDD0532  [2]
 LDCM0226  AC11 HCT 116 C203(1.30)  LDD0543  [2]
 LDCM0230  AC113 HCT 116 C203(0.94)  LDD0547  [2]
 LDCM0231  AC114 HCT 116 C203(1.01)  LDD0548  [2]
 LDCM0232  AC115 HCT 116 C203(1.06)  LDD0549  [2]
 LDCM0233  AC116 HCT 116 C203(1.19)  LDD0550  [2]
 LDCM0234  AC117 HCT 116 C203(1.04)  LDD0551  [2]
 LDCM0235  AC118 HCT 116 C203(1.06)  LDD0552  [2]
 LDCM0236  AC119 HCT 116 C203(1.13)  LDD0553  [2]
 LDCM0237  AC12 HCT 116 C203(1.22)  LDD0554  [2]
 LDCM0238  AC120 HCT 116 C203(1.12)  LDD0555  [2]
 LDCM0239  AC121 HCT 116 C203(0.93)  LDD0556  [2]
 LDCM0240  AC122 HCT 116 C203(1.00)  LDD0557  [2]
 LDCM0241  AC123 HCT 116 C203(0.97)  LDD0558  [2]
 LDCM0242  AC124 HCT 116 C203(0.90)  LDD0559  [2]
 LDCM0243  AC125 HCT 116 C203(0.96)  LDD0560  [2]
 LDCM0244  AC126 HCT 116 C203(1.15)  LDD0561  [2]
 LDCM0245  AC127 HCT 116 C203(1.07)  LDD0562  [2]
 LDCM0259  AC14 HCT 116 C203(1.19)  LDD0576  [2]
 LDCM0263  AC143 HCT 116 C203(1.02)  LDD0580  [2]
 LDCM0264  AC144 HCT 116 C203(1.14)  LDD0581  [2]
 LDCM0265  AC145 HCT 116 C203(1.06)  LDD0582  [2]
 LDCM0266  AC146 HCT 116 C203(1.33)  LDD0583  [2]
 LDCM0267  AC147 HCT 116 C203(1.19)  LDD0584  [2]
 LDCM0268  AC148 HCT 116 C203(1.68)  LDD0585  [2]
 LDCM0269  AC149 HCT 116 C203(1.68)  LDD0586  [2]
 LDCM0270  AC15 HCT 116 C203(1.23)  LDD0587  [2]
 LDCM0271  AC150 HCT 116 C203(1.17)  LDD0588  [2]
 LDCM0272  AC151 HCT 116 C203(1.01)  LDD0589  [2]
 LDCM0273  AC152 HCT 116 C203(1.16)  LDD0590  [2]
 LDCM0274  AC153 HCT 116 C203(1.67)  LDD0591  [2]
 LDCM0621  AC154 HCT 116 C203(1.35)  LDD2158  [2]
 LDCM0622  AC155 HCT 116 C203(1.49)  LDD2159  [2]
 LDCM0623  AC156 HCT 116 C203(1.07)  LDD2160  [2]
 LDCM0624  AC157 HCT 116 C203(0.96)  LDD2161  [2]
 LDCM0320  AC57 HCT 116 C203(1.24)  LDD0637  [2]
 LDCM0321  AC58 HCT 116 C203(1.26)  LDD0638  [2]
 LDCM0322  AC59 HCT 116 C203(1.61)  LDD0639  [2]
 LDCM0323  AC6 HCT 116 C203(1.28)  LDD0640  [2]
 LDCM0324  AC60 HCT 116 C203(1.45)  LDD0641  [2]
 LDCM0325  AC61 HCT 116 C203(1.29)  LDD0642  [2]
 LDCM0326  AC62 HCT 116 C203(1.25)  LDD0643  [2]
 LDCM0327  AC63 HCT 116 C203(1.35)  LDD0644  [2]
 LDCM0328  AC64 HCT 116 C203(1.55)  LDD0645  [2]
 LDCM0329  AC65 HCT 116 C203(1.54)  LDD0646  [2]
 LDCM0330  AC66 HCT 116 C203(1.55)  LDD0647  [2]
 LDCM0331  AC67 HCT 116 C203(1.47)  LDD0648  [2]
 LDCM0334  AC7 HCT 116 C203(0.87)  LDD0651  [2]
 LDCM0345  AC8 HCT 116 C203(1.11)  LDD0662  [2]
 LDCM0349  AC83 HCT 116 C203(1.01)  LDD0666  [2]
 LDCM0350  AC84 HCT 116 C203(0.98)  LDD0667  [2]
 LDCM0351  AC85 HCT 116 C203(1.07)  LDD0668  [2]
 LDCM0352  AC86 HCT 116 C203(1.00)  LDD0669  [2]
 LDCM0353  AC87 HCT 116 C203(0.87)  LDD0670  [2]
 LDCM0354  AC88 HCT 116 C203(0.94)  LDD0671  [2]
 LDCM0355  AC89 HCT 116 C203(0.92)  LDD0672  [2]
 LDCM0357  AC90 HCT 116 C203(0.89)  LDD0674  [2]
 LDCM0358  AC91 HCT 116 C203(1.02)  LDD0675  [2]
 LDCM0359  AC92 HCT 116 C203(1.02)  LDD0676  [2]
 LDCM0360  AC93 HCT 116 C203(1.00)  LDD0677  [2]
 LDCM0361  AC94 HCT 116 C203(1.16)  LDD0678  [2]
 LDCM0362  AC95 HCT 116 C203(0.85)  LDD0679  [2]
 LDCM0363  AC96 HCT 116 C203(1.09)  LDD0680  [2]
 LDCM0364  AC97 HCT 116 C203(1.11)  LDD0681  [2]
 LDCM0248  AKOS034007472 HCT 116 C203(1.05)  LDD0565  [2]
 LDCM0356  AKOS034007680 HCT 116 C203(1.16)  LDD0673  [2]
 LDCM0275  AKOS034007705 HCT 116 C203(1.78)  LDD0592  [2]
 LDCM0370  CL101 HCT 116 C203(1.52)  LDD0687  [2]
 LDCM0371  CL102 HCT 116 C203(1.07)  LDD0688  [2]
 LDCM0372  CL103 HCT 116 C203(1.35)  LDD0689  [2]
 LDCM0373  CL104 HCT 116 C203(1.20)  LDD0690  [2]
 LDCM0396  CL125 HCT 116 C203(1.01)  LDD0713  [2]
 LDCM0397  CL126 HCT 116 C203(0.93)  LDD0714  [2]
 LDCM0398  CL127 HCT 116 C203(1.04)  LDD0715  [2]
 LDCM0399  CL128 HCT 116 C203(1.36)  LDD0716  [2]
 LDCM0469  CL76 HCT 116 C203(1.39)  LDD0786  [2]
 LDCM0470  CL77 HCT 116 C203(1.10)  LDD0787  [2]
 LDCM0471  CL78 HCT 116 C203(1.03)  LDD0788  [2]
 LDCM0472  CL79 HCT 116 C203(1.50)  LDD0789  [2]
 LDCM0474  CL80 HCT 116 C203(1.12)  LDD0791  [2]
 LDCM0475  CL81 HCT 116 C203(1.18)  LDD0792  [2]
 LDCM0476  CL82 HCT 116 C203(1.67)  LDD0793  [2]
 LDCM0477  CL83 HCT 116 C203(1.86)  LDD0794  [2]
 LDCM0478  CL84 HCT 116 C203(2.24)  LDD0795  [2]
 LDCM0479  CL85 HCT 116 C203(1.27)  LDD0796  [2]
 LDCM0480  CL86 HCT 116 C203(1.03)  LDD0797  [2]
 LDCM0481  CL87 HCT 116 C203(1.49)  LDD0798  [2]
 LDCM0482  CL88 HCT 116 C203(1.43)  LDD0799  [2]
 LDCM0483  CL89 HCT 116 C203(1.95)  LDD0800  [2]
 LDCM0485  CL90 HCT 116 C203(1.48)  LDD0802  [2]
 LDCM0022  KB02 A101D C78(1.19)  LDD2250  [6]
 LDCM0023  KB03 A101D C78(2.17)  LDD2667  [6]
 LDCM0024  KB05 HMCB C78(1.62)  LDD3312  [6]

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
26S proteasome regulatory subunit 8 (PSMC5) AAA ATPase family P62195
Transcription factor
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Retinoic acid receptor RXR-beta (RXRB) Nuclear hormone receptor family P28702
Retinoic acid receptor RXR-gamma (RXRG) Nuclear hormone receptor family P48443
Homeobox protein MOX-2 (MEOX2) . P50222
Other
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Cyclin-D1-binding protein 1 (CCNDBP1) CCNDBP1 family O95273
Peroxisome proliferator-activated receptor gamma coactivator 1-alpha (PPARGC1A) . Q9UBK2

The Drug(s) Related To This Target

Approved
Click To Hide/Show 6 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Acitretin Small molecular drug DB00459
Adapalene Small molecular drug DB00210
Alitretinoin Small molecular drug D0G3PI
Tazarotene Small molecular drug DB00799
Tretinoin Small molecular drug DB00755
Trifarotene Small molecular drug DB12808
Phase 3
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Tamibarotene Small molecular drug D02GTY
Investigative
Click To Hide/Show 8 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ac261066 Small molecular drug D09RRF
Ac55649 Small molecular drug D05QYR
Agn193109 Small molecular drug D0Q0IR
Arotinoid Acid Small molecular drug DB02877
Bms641 Small molecular drug D09RNF
Cd666 Small molecular drug D0F8CC
Ttnpb Small molecular drug D0G6JM
Lgd-1550 . DB05785
Patented
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pmid27336223-compound-10 Small molecular drug D0E2AD
Pmid27336223-compound-7 Small molecular drug D0PU1L
Pmid27336223-compound-8 Small molecular drug D0M5EC
Discontinued
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Etretinate Small molecular drug DB00926

References

1 Chemoproteomic profiling of kinases in live cells using electrophilic sulfonyl triazole probes. Chem Sci. 2021 Jan 21;12(9):3295-3307. doi: 10.1039/d0sc06623k.
2 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.
3 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
4 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
5 Ynamide Electrophile for the Profiling of Ligandable Carboxyl Residues in Live Cells and the Development of New Covalent Inhibitors. J Med Chem. 2022 Aug 11;65(15):10408-10418. doi: 10.1021/acs.jmedchem.2c00272. Epub 2022 Jul 26.
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