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Nuclear receptor structure is composed of 5 domains -

A/B: N-terminal regulatory domain contains activation function 1 (residues 101-370), activation function 5 (residues 360-485) and dimerization surface (residues 1-36 and 370-494).
C: DNA binding domain (DBD)
D: Hinge region between DBD and LBD
E: Ligand binding domain (LBD) containing an which binds intramolecularly the N-terminal FXXFL motif or coactivators with the same motif (Human androgen receptor ligand-binding domain complex with modulator; PDB code 3b5r).[1] Water molecules are shown as red spheres.
F: C-terminal domain

Thyroid Hormone Receptor-like

Thyroid hormone receptor

Retinoic acid receptor

Peroxisome Proliferator-Activated Receptors

PPARγ

Vitamin D receptor-like

Vitamin D receptor

Estrogen Receptor-like

Estrogen receptor

Estrogen receptor alpha

Estrogen receptor beta

Estrogen-related receptor

3-Ketosteroid receptors

Androgen receptor

Glucocorticoid receptor

Human androgen receptor ligand-binding domain complex with modulator (PDB code 3b5r)

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ReferencesReferences

  1. Bohl CE, Wu Z, Chen J, Mohler ML, Yang J, Hwang DJ, Mustafa S, Miller DD, Bell CE, Dalton JT. Effect of B-ring substitution pattern on binding mode of propionamide selective androgen receptor modulators. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5567-70. Epub 2008 Sep 5. PMID:18805694 doi:10.1016/j.bmcl.2008.09.002
  2. Li MJ, Greenblatt HM, Dym O, Albeck S, Pais A, Gunanathan C, Milstein D, Degani H, Sussman JL. Structure of estradiol metal chelate and estrogen receptor complex: The basis for designing a new class of selective estrogen receptor modulators. J Med Chem. 2011 Apr 7. PMID:21473635 doi:10.1021/jm200192y

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Alexander Berchansky, Michal Harel