Details of the Target

General Information of Target

Target ID LDTP05161
Target Name 11-beta-hydroxysteroid dehydrogenase type 2 (HSD11B2)
Gene Name HSD11B2
Gene ID 3291
Synonyms
HSD11K; SDR9C3; 11-beta-hydroxysteroid dehydrogenase type 2; 11-DH2; 11-beta-HSD2; EC 1.1.1.-; 11-beta-hydroxysteroid dehydrogenase type II; 11-HSD type II; 11-beta-HSD type II; Corticosteroid 11-beta-dehydrogenase isozyme 2; NAD-dependent 11-beta-hydroxysteroid dehydrogenase; Short chain dehydrogenase/reductase family 9C member 3
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MERWPWPSGGAWLLVAARALLQLLRSDLRLGRPLLAALALLAALDWLCQRLLPPPAALAV
LAAAGWIALSRLARPQRLPVATRAVLITGCDSGFGKETAKKLDSMGFTVLATVLELNSPG
AIELRTCCSPRLRLLQMDLTKPGDISRVLEFTKAHTTSTGLWGLVNNAGHNEVVADAELS
PVATFRSCMEVNFFGALELTKGLLPLLRSSRGRIVTVGSPAGDMPYPCLGAYGTSKAAVA
LLMDTFSCELLPWGVKVSIIQPGCFKTESVRNVGQWEKRKQLLLANLPQELLQAYGKDYI
EHLHGQFLHSLRLAMSDLTPVVDAITDALLAARPRRRYYPGQGLGLMYFIHYYLPEGLRR
RFLQAFFISHCLPRALQPGQPGTTPPQDAAQDPNLSPGPSPAVAR
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Short-chain dehydrogenases/reductases (SDR) family
Subcellular location
Microsome
Function
Catalyzes the conversion of biologically active 11beta-hydroxyglucocorticoids (11beta-hydroxysteroid) such as cortisol, to inactive 11-ketoglucocorticoids (11-oxosteroid) such as cortisone, in the presence of NAD(+). Functions as a dehydrogenase (oxidase), thereby decreasing the concentration of active glucocorticoids, thus protecting the nonselective mineralocorticoid receptor from occupation by glucocorticoids. Plays an important role in maintaining glucocorticoids balance during preimplantation and protects the fetus from excessive maternal corticosterone exposure. Catalyzes the oxidation of 11beta-hydroxytestosterone (11beta,17beta-dihydroxyandrost-4-ene-3-one) to 11-ketotestosterone (17beta-hydroxyandrost-4-ene-3,11-dione), a major bioactive androgen. Catalyzes the conversion of 11beta-hydroxyandrostenedione (11beta-hydroxyandrost-4-ene-3,17-dione) to 11-ketoandrostenedione (androst-4-ene-3,11,17-trione), which can be further metabolized to 11-ketotestosterone. Converts 7-beta-25-dihydroxycholesterol to 7-oxo-25-hydroxycholesterol in vitro. 7-beta-25-dihydroxycholesterol (not 7-oxo-25-hydroxycholesterol) acts as a ligand for the G-protein-coupled receptor (GPCR) Epstein-Barr virus-induced gene 2 (EBI2) and may thereby regulate immune cell migration. May protect ovulating oocytes and fertilizing spermatozoa from the adverse effects of cortisol.
TTD ID
T43721
Uniprot ID
P80365
DrugMap ID
TT9H85R
Ensemble ID
ENST00000326152.6
HGNC ID
HGNC:5209
ChEMBL ID
CHEMBL3746

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
IPM
 Probe Info  		N.A.  LDD0241  [1]
DBIA
 Probe Info  		C264(1.37)  LDD0533  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0216  AC100 HCT 116 C264(1.37)  LDD0533  [2]
 LDCM0217  AC101 HCT 116 C264(1.39)  LDD0534  [2]
 LDCM0218  AC102 HCT 116 C264(1.14)  LDD0535  [2]
 LDCM0219  AC103 HCT 116 C264(1.45)  LDD0536  [2]
 LDCM0220  AC104 HCT 116 C264(1.02)  LDD0537  [2]
 LDCM0221  AC105 HCT 116 C264(1.29)  LDD0538  [2]
 LDCM0222  AC106 HCT 116 C264(1.50)  LDD0539  [2]
 LDCM0223  AC107 HCT 116 C264(1.32)  LDD0540  [2]
 LDCM0224  AC108 HCT 116 C264(1.38)  LDD0541  [2]
 LDCM0225  AC109 HCT 116 C264(1.13)  LDD0542  [2]
 LDCM0227  AC110 HCT 116 C264(1.46)  LDD0544  [2]
 LDCM0228  AC111 HCT 116 C264(1.53)  LDD0545  [2]
 LDCM0229  AC112 HCT 116 C264(1.31)  LDD0546  [2]
 LDCM0230  AC113 HCT 116 C264(1.02)  LDD0547  [2]
 LDCM0231  AC114 HCT 116 C264(1.06)  LDD0548  [2]
 LDCM0232  AC115 HCT 116 C264(1.00)  LDD0549  [2]
 LDCM0233  AC116 HCT 116 C264(1.06)  LDD0550  [2]
 LDCM0234  AC117 HCT 116 C264(1.00)  LDD0551  [2]
 LDCM0235  AC118 HCT 116 C264(1.03)  LDD0552  [2]
 LDCM0236  AC119 HCT 116 C264(1.18)  LDD0553  [2]
 LDCM0238  AC120 HCT 116 C264(1.18)  LDD0555  [2]
 LDCM0239  AC121 HCT 116 C264(1.12)  LDD0556  [2]
 LDCM0240  AC122 HCT 116 C264(1.17)  LDD0557  [2]
 LDCM0241  AC123 HCT 116 C264(1.05)  LDD0558  [2]
 LDCM0242  AC124 HCT 116 C264(1.09)  LDD0559  [2]
 LDCM0243  AC125 HCT 116 C264(1.26)  LDD0560  [2]
 LDCM0244  AC126 HCT 116 C264(1.15)  LDD0561  [2]
 LDCM0245  AC127 HCT 116 C264(1.05)  LDD0562  [2]
 LDCM0285  AC25 HCT 116 C264(1.06)  LDD0602  [2]
 LDCM0286  AC26 HCT 116 C264(1.19)  LDD0603  [2]
 LDCM0287  AC27 HCT 116 C264(1.16)  LDD0604  [2]
 LDCM0288  AC28 HCT 116 C264(1.28)  LDD0605  [2]
 LDCM0289  AC29 HCT 116 C264(1.30)  LDD0606  [2]
 LDCM0291  AC30 HCT 116 C264(1.49)  LDD0608  [2]
 LDCM0292  AC31 HCT 116 C264(1.18)  LDD0609  [2]
 LDCM0293  AC32 HCT 116 C264(1.65)  LDD0610  [2]
 LDCM0294  AC33 HCT 116 C264(1.06)  LDD0611  [2]
 LDCM0295  AC34 HCT 116 C264(0.82)  LDD0612  [2]
 LDCM0308  AC46 HCT 116 C264(1.22)  LDD0625  [2]
 LDCM0309  AC47 HCT 116 C264(1.13)  LDD0626  [2]
 LDCM0310  AC48 HCT 116 C264(1.32)  LDD0627  [2]
 LDCM0311  AC49 HCT 116 C264(1.25)  LDD0628  [2]
 LDCM0313  AC50 HCT 116 C264(1.47)  LDD0630  [2]
 LDCM0314  AC51 HCT 116 C264(1.26)  LDD0631  [2]
 LDCM0315  AC52 HCT 116 C264(1.12)  LDD0632  [2]
 LDCM0316  AC53 HCT 116 C264(1.14)  LDD0633  [2]
 LDCM0317  AC54 HCT 116 C264(1.30)  LDD0634  [2]
 LDCM0318  AC55 HCT 116 C264(1.02)  LDD0635  [2]
 LDCM0319  AC56 HCT 116 C264(1.11)  LDD0636  [2]
 LDCM0349  AC83 HCT 116 C264(1.46)  LDD0666  [2]
 LDCM0350  AC84 HCT 116 C264(1.38)  LDD0667  [2]
 LDCM0351  AC85 HCT 116 C264(1.56)  LDD0668  [2]
 LDCM0352  AC86 HCT 116 C264(1.61)  LDD0669  [2]
 LDCM0353  AC87 HCT 116 C264(1.56)  LDD0670  [2]
 LDCM0354  AC88 HCT 116 C264(1.54)  LDD0671  [2]
 LDCM0355  AC89 HCT 116 C264(1.45)  LDD0672  [2]
 LDCM0357  AC90 HCT 116 C264(1.46)  LDD0674  [2]
 LDCM0358  AC91 HCT 116 C264(1.21)  LDD0675  [2]
 LDCM0359  AC92 HCT 116 C264(1.50)  LDD0676  [2]
 LDCM0360  AC93 HCT 116 C264(1.49)  LDD0677  [2]
 LDCM0361  AC94 HCT 116 C264(1.13)  LDD0678  [2]
 LDCM0362  AC95 HCT 116 C264(1.49)  LDD0679  [2]
 LDCM0363  AC96 HCT 116 C264(1.01)  LDD0680  [2]
 LDCM0364  AC97 HCT 116 C264(1.51)  LDD0681  [2]
 LDCM0365  AC98 HCT 116 C264(1.43)  LDD0682  [2]
 LDCM0366  AC99 HCT 116 C264(1.38)  LDD0683  [2]
 LDCM0367  CL1 HCT 116 C264(1.07)  LDD0684  [2]
 LDCM0368  CL10 HCT 116 C264(0.94)  LDD0685  [2]
 LDCM0379  CL11 HCT 116 C264(1.58)  LDD0696  [2]
 LDCM0382  CL112 HCT 116 C264(2.15)  LDD0699  [2]
 LDCM0383  CL113 HCT 116 C264(1.28)  LDD0700  [2]
 LDCM0384  CL114 HCT 116 C264(2.51)  LDD0701  [2]
 LDCM0385  CL115 HCT 116 C264(1.31)  LDD0702  [2]
 LDCM0386  CL116 HCT 116 C264(1.02)  LDD0703  [2]
 LDCM0390  CL12 HCT 116 C264(0.98)  LDD0707  [2]
 LDCM0392  CL121 HCT 116 C264(1.36)  LDD0709  [2]
 LDCM0393  CL122 HCT 116 C264(1.19)  LDD0710  [2]
 LDCM0394  CL123 HCT 116 C264(1.44)  LDD0711  [2]
 LDCM0395  CL124 HCT 116 C264(2.00)  LDD0712  [2]
 LDCM0400  CL13 HCT 116 C264(0.95)  LDD0717  [2]
 LDCM0401  CL14 HCT 116 C264(0.92)  LDD0718  [2]
 LDCM0402  CL15 HCT 116 C264(1.24)  LDD0719  [2]
 LDCM0407  CL2 HCT 116 C264(0.97)  LDD0724  [2]
 LDCM0418  CL3 HCT 116 C264(0.88)  LDD0735  [2]
 LDCM0420  CL31 HCT 116 C264(1.37)  LDD0737  [2]
 LDCM0421  CL32 HCT 116 C264(1.07)  LDD0738  [2]
 LDCM0422  CL33 HCT 116 C264(1.30)  LDD0739  [2]
 LDCM0423  CL34 HCT 116 C264(3.68)  LDD0740  [2]
 LDCM0424  CL35 HCT 116 C264(1.12)  LDD0741  [2]
 LDCM0425  CL36 HCT 116 C264(2.64)  LDD0742  [2]
 LDCM0426  CL37 HCT 116 C264(1.19)  LDD0743  [2]
 LDCM0428  CL39 HCT 116 C264(1.15)  LDD0745  [2]
 LDCM0429  CL4 HCT 116 C264(3.95)  LDD0746  [2]
 LDCM0430  CL40 HCT 116 C264(1.83)  LDD0747  [2]
 LDCM0431  CL41 HCT 116 C264(1.96)  LDD0748  [2]
 LDCM0432  CL42 HCT 116 C264(1.26)  LDD0749  [2]
 LDCM0433  CL43 HCT 116 C264(1.18)  LDD0750  [2]
 LDCM0434  CL44 HCT 116 C264(1.15)  LDD0751  [2]
 LDCM0435  CL45 HCT 116 C264(6.07)  LDD0752  [2]
 LDCM0436  CL46 HCT 116 C264(1.26)  LDD0753  [2]
 LDCM0437  CL47 HCT 116 C264(1.06)  LDD0754  [2]
 LDCM0438  CL48 HCT 116 C264(1.53)  LDD0755  [2]
 LDCM0439  CL49 HCT 116 C264(1.28)  LDD0756  [2]
 LDCM0440  CL5 HCT 116 C264(0.99)  LDD0757  [2]
 LDCM0441  CL50 HCT 116 C264(1.91)  LDD0758  [2]
 LDCM0442  CL51 HCT 116 C264(2.82)  LDD0759  [2]
 LDCM0443  CL52 HCT 116 C264(1.44)  LDD0760  [2]
 LDCM0444  CL53 HCT 116 C264(1.18)  LDD0761  [2]
 LDCM0445  CL54 HCT 116 C264(1.16)  LDD0762  [2]
 LDCM0446  CL55 HCT 116 C264(0.94)  LDD0763  [2]
 LDCM0447  CL56 HCT 116 C264(0.92)  LDD0764  [2]
 LDCM0448  CL57 HCT 116 C264(1.08)  LDD0765  [2]
 LDCM0449  CL58 HCT 116 C264(1.08)  LDD0766  [2]
 LDCM0450  CL59 HCT 116 C264(1.05)  LDD0767  [2]
 LDCM0451  CL6 HCT 116 C264(0.96)  LDD0768  [2]
 LDCM0452  CL60 HCT 116 C264(1.12)  LDD0769  [2]
 LDCM0462  CL7 HCT 116 C264(1.42)  LDD0779  [2]
 LDCM0473  CL8 HCT 116 C264(0.94)  LDD0790  [2]
 LDCM0484  CL9 HCT 116 C264(1.12)  LDD0801  [2]
 LDCM0427  Fragment51 HCT 116 C264(7.71)  LDD0744  [2]
 LDCM0022  KB02 BRX29 C248(1.49); C90(1.58); C264(3.19)  LDD2270  [3]
 LDCM0023  KB03 BRX29 C248(2.37); C90(2.27); C264(8.39)  LDD2687  [3]
 LDCM0024  KB05 SK-HEP1 C90(2.17)  LDD3424  [3]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 14 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Dexamethasone Small molecular drug DB01234
Fludrocortisone Small molecular drug DB00687
Fluoxymesterone Small molecular drug DB01185
Hydrocortisone Small molecular drug DB00741
Methylprednisolone Small molecular drug DB00959
Nadh Small molecular drug DB00157
Dexamethasone Acetate . DB14649
Hydrocortisone Acetate . DB14539
Hydrocortisone Butyrate . DB14540
Hydrocortisone Cypionate . DB14541
Hydrocortisone Phosphate . DB14542
Hydrocortisone Probutate . DB14543
Hydrocortisone Valerate . DB14544
Prednisolone Phosphate . DB14631
Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Rg-7234 . D04ZNL
Investigative
Click To Hide/Show 6 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
11-keto-beta-boswellicacid Small molecular drug D09VYW
3-acetyl-11-keto-beta-boswellic Acid Small molecular drug D02XEX
Corticosterone Small molecular drug DB04652
Ganoderic Acid A Small molecular drug D03NPA
[(125)I] Rb129 Small molecular drug D0U8IF
Hydrocortisone Aceponate . DB14538
Discontinued
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Formebolone . DB01569

References

1 Oxidant-Induced Bioconjugation for Protein Labeling in Live Cells. ACS Chem Biol. 2023 Jan 20;18(1):112-122. doi: 10.1021/acschembio.2c00740. Epub 2022 Dec 21.
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 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