Binding Site Information of Target

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Target General Information
Drug Binding Sites of Target
References
Target General Information  Top
Target ID T60077 Target Info
Target Name Retinoic acid receptor RXR-beta (RXRB)
Synonyms Retinoid X receptor beta; Nuclear receptor subfamily 2 group B member 2; NR2B2
Target Type Successful Target
Gene Name RXRB
Biochemical Class Nuclear hormone receptor
UniProt ID
RXRB_HUMAN
Drug Binding Sites of Target  Top
Ligand Name: Methoprene acid Ligand Info
Structure Description Crystal structure of the LXRalfa-RXRbeta LBD heterodimer PDB:1UHL
Method X-ray diffraction Resolution 2.90 Å Mutation No [1]
PDB Sequence
EMPVDRILEA
307
ELAVEQSPND
334
PVTNICQAAD
344
KQLFTLVEWA
354
KRIPHFSSLP
364

LDDQVILLRA
374
GWNELLIASF
384
SHRSIDVRDG
394
ILLATGLHVH
404
RNSAHSAGVG
414

AIFDRVLTEL
424
VSKMRDMRMD
434
KTELGCLRAI
444
ILFNPDAKGL
454
SNPSEVEVLR
464

EKVYASLETY
474
CKQKYPEQQG
484
RFAKLLLRLP
494
ALRSIGLKCL
504
EHLFFFKLIG
514

DTPIDTFLME
524
MLEA
Residue
Distance (Å)
ILE339
3.512
ALA342
3.146
ALA343
3.224
GLN346
3.770
TRP376
4.273
ASN377
3.759
LEU380
3.522
ILE381
3.721
PHE384
3.606
ARG387
2.693
Residue
Distance (Å)
LEU397
3.990
ALA398
3.307
VAL413
3.450
ILE416
4.010
PHE417
4.487
CYS503
3.354
HIS506
3.930
LEU507
3.662
PHE510
4.849
Ligand Name: LG100268 Ligand Info
Structure Description The structure of the human retinoid-X-receptor beta ligand binding domain in complex with the specific synthetic agonist LG100268 PDB:1H9U
Method X-ray diffraction Resolution 2.70 Å Mutation No [2]
PDB Sequence
MPVDRILEAE
308
LAVPVTNICQ
341
AADKQLFTLV
351
EWAKRIPHFS
361
SLPLDDQVIL
371

LRAGWNELLI
381
ASFSHRSIDV
391
RDGILLATGL
401
HVHRNSAHSA
411
GVGAIFDRVL
421

TELVSKMRDM
431
RMDKTELGCL
441
RAIILFNPDA
451
KGLSNPSEVE
461
VLREKVYASL
471

ETYCKQKYPE
481
QQGRFAKLLL
491
RLPALRSIGL
501
KCLEHLFFFK
511
LIGDTPIDTF
521

L
Residue
Distance (Å)
VAL336
4.193
ILE339
3.503
CYS340
4.234
ALA342
2.849
ALA343
3.514
GLN346
3.604
TRP376
3.669
ASN377
3.914
LEU380
3.230
ILE381
3.404
PHE384
3.384
ARG387
2.940
LEU396
4.788
Residue
Distance (Å)
LEU397
3.171
ALA398
2.646
THR399
4.573
VAL413
4.092
ILE416
3.680
PHE417
4.448
VAL420
3.973
ILE499
4.644
CYS503
3.470
HIS506
3.645
LEU507
4.112
PHE510
4.920
References  Top
REF 1 Crystal structure of the heterodimeric complex of LXRalpha and RXRbeta ligand-binding domains in a fully agonistic conformation. EMBO J. 2003 Sep 15;22(18):4625-33.
REF 2 The structural basis for the specificity of retinoid-X receptor-selective agonists: new insights into the role of helix H12. J Biol Chem. 2002 Mar 29;277(13):11385-91.

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