PDBsum entry 3okh

Hormone receptor

PDB id: 3okh

Contents

Protein chain

227 a.a. *

Ligands

HIS-GLN-LEU-LEU-ARG-TYR-LEU-LEU-ASP-LYS

OKH ×2

Waters ×15

* Residue conservation analysis

PDB id:

3okh

Name:

Hormone receptor

Title:

Crystal structure of human fxr in complex with 2-(4-chlorophenyl)-1- [(1s)-1-cyclohexyl-2-(cyclohexylamino)-2-oxoethyl]-1h-benzimidazole- 6-carboxylic acid

Structure:

Bile acid receptor. Chain: a. Fragment: unp residues 258-486. Synonym: fxr, farnesoid x-activated receptor, farnesol receptor hrr- 1, nuclear receptor subfamily 1 group h member 4, retinoid x receptor-interacting protein 14, rxr-interacting protein 14. Engineered: yes. Mutation: yes. Peptide of nuclear receptor coactivator 1.

Source:

Homo sapiens. Human. Organism_taxid: 9606. Gene: nr1h4, hcg_20893. Expressed in: escherichia coli. Expression_system_taxid: 562. Synthetic: yes. Other_details: this sequence occurs naturally in humans

Resolution:

2.50Å R-factor: 0.216 R-free: 0.273

Authors:

M.G.Rudolph

Key ref:

H.G.Richter et al. (2011). Discovery of novel and orally active FXR agonists for the potential treatment of dyslipidemia & diabetes. Bioorg Med Chem Lett, 21, 191-194. PubMed id: 21134747

Date:

25-Aug-10 Release date: 29-Dec-10

Protein chain

Q96RI1  (NR1H4_HUMAN) -  Bile acid receptor from Homo sapiens

Seq: 486 a.a.

Struc: 227 a.a.*

* PDB and UniProt seqs differ at 2 residue positions (black crosses)

Enzyme reactions

• Enzyme class: E.C.?

Bioorg Med Chem Lett 21:191-194 (2011)

PubMed id: 21134747

Discovery of novel and orally active FXR agonists for the potential treatment of dyslipidemia & diabetes.

H.G.Richter, G.M.Benson, D.Blum, E.Chaput, S.Feng, C.Gardes, U.Grether, P.Hartman, B.Kuhn, R.E.Martin, J.M.Plancher, M.G.Rudolph, F.Schuler, S.Taylor, K.H.Bleicher.

ABSTRACT

No abstract given.