PDBsum entry 1e3k

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Human progesterone receptor PDB id
Protein chain
251 a.a. *
R18 ×2
Waters ×1
* Residue conservation analysis
PDB id:
Name: Human progesterone receptor
Title: Human progesteron receptor ligand binding domain in complex with the ligand metribolone (r1881)
Structure: Progesterone receptor. Chain: a, b. Fragment: ligand-binding domain. Engineered: yes
Source: Homo sapiens. Human. Organism_taxid: 9606. Expressed in: escherichia coli. Expression_system_taxid: 511693. Expression_system_cell_line: de3
2.8Å     R-factor:   0.240     R-free:   0.343
Authors: P.M.Matias,P.Donner,R.Coelho,M.Thomaz,C.Peixoto,S.Macedo, N.Otto,S.Joschko,P.Scholz,A.Wegg,S.Basler,M.Schafer, U.Egner,M.A.Carrondo
Key ref:
P.M.Matias et al. (2000). Structural evidence for ligand specificity in the binding domain of the human androgen receptor. Implications for pathogenic gene mutations. J Biol Chem, 275, 26164-26171. PubMed id: 10840043 DOI: 10.1074/jbc.M004571200
19-Jun-00     Release date:   14-Jun-01    
Go to PROCHECK summary

Protein chains
Pfam   ArchSchema ?
P06401  (PRGR_HUMAN) -  Progesterone receptor
933 a.a.
251 a.a.
Key:    PfamA domain  Secondary structure  CATH domain

 Gene Ontology (GO) functional annotation 
  GO annot!
  Cellular component     nucleus   1 term 
  Biological process     steroid hormone mediated signaling pathway   2 terms 
  Biochemical function     DNA binding     3 terms  


DOI no: 10.1074/jbc.M004571200 J Biol Chem 275:26164-26171 (2000)
PubMed id: 10840043  
Structural evidence for ligand specificity in the binding domain of the human androgen receptor. Implications for pathogenic gene mutations.
P.M.Matias, P.Donner, R.Coelho, M.Thomaz, C.Peixoto, S.Macedo, N.Otto, S.Joschko, P.Scholz, A.Wegg, S.Bäsler, M.Schäfer, U.Egner, M.A.Carrondo.
The crystal structures of the human androgen receptor (hAR) and human progesterone receptor ligand-binding domains in complex with the same ligand metribolone (R1881) have been determined. Both three-dimensional structures show the typical nuclear receptor fold. The change of two residues in the ligand-binding pocket between the human progesterone receptor and hAR is most likely the source for the specificity of R1881 to the hAR. The structural implications of the 14 known mutations in the ligand-binding pocket of the hAR ligand-binding domains associated with either prostate cancer or the partial or complete androgen receptor insensitivity syndrome were analyzed. The effects of most of these mutants could be explained on the basis of the crystal structure.
  Selected figure(s)  
Figure 2.
Fig. 2. Numbering scheme of R1881 (top) and progesterone (bottom).
Figure 4.
Fig. 4. Stereo diagrams showing the interactions between the bound ligand and the protein chain in hAR LBD-R1881 (a), hPR LBD-R1881 (molecule A) (b), and hPR LBD-progesterone (c). Residues included are either hydrogen-bonded or have van der Waals contacts (cutoff distance 4.0 Å) with any of the ligands. Residues Val685 and Tyr763 in hAR LBD and corresponding residues Ile^699 and Tyr777 in hPR LBD are hydrogen-bonded to other residues or water molecules near the ligand-binding site and are also included. Bound ligand is colored black; conserved residues are colored gray; different residues in hAR LBD and hPR LBD are colored red. Residue labels with an asterisk denote residues that do not have van der Waals contacts within the specified cutoff distance with the ligand. Hydrogen bond distances for the hPR LBD·progesterone complex were calculated from the Protein Data Bank deposited coordinates of molecule A. Figures were produced with MOLSCRIPT (52).
  The above figures are reprinted by permission from the ASBMB: J Biol Chem (2000, 275, 26164-26171) copyright 2000.  
  Figures were selected by an automated process.  

Literature references that cite this PDB file's key reference

  PubMed id Reference
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19178528 R.Tadokoro, T.Bunch, J.W.Schwabe, I.A.Hughes, and J.C.Murphy (2009).
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20009327 S.B.Kim, Y.Umezawa, and H.Tao (2009).
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18612376 F.Claessens, S.Denayer, N.Van Tilborgh, S.Kerkhofs, C.Helsen, and A.Haelens (2008).
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18037956 G.N.Brooke, M.G.Parker, and C.L.Bevan (2008).
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18502379 J.Zhang, and D.S.Geller (2008).
Helix 3-helix 5 interactions in steroid hormone receptor function.
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18160712 K.Suino-Powell, Y.Xu, C.Zhang, Y.G.Tao, W.D.Tolbert, S.S.Simons, and H.E.Xu (2008).
Doubling the size of the glucocorticoid receptor ligand binding pocket by deacylcortivazol.
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PDB code: 3bqd
18981605 K.Tachibana, I.Imaoka, T.Shiraishi, H.Yoshino, M.Nakamura, M.Ohta, H.Kawata, K.Taniguchi, N.Ishikura, T.Tsunenari, H.Saito, M.Nagamuta, T.Nakagawa, K.Takanashi, E.Onuma, and H.Sato (2008).
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18852122 M.C.Hodgson, H.C.Shen, A.N.Hollenberg, and S.P.Balk (2008).
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19094205 V.Douard, F.Brunet, B.Boussau, I.Ahrens, V.Vlaeminck-Guillem, B.Haendler, V.Laudet, and Y.Guiguen (2008).
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PDB code: 2oz7
17137423 D.L.Bain, A.F.Heneghan, K.D.Connaghan-Jones, and M.T.Miura (2007).
Nuclear receptor structure: implications for function.
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The evolution of progesterone receptor ligands.
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Structural analysis of the evolution of steroid specificity in the mineralocorticoid and glucocorticoid receptors.
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Androgen receptor coregulators and their involvement in the development and progression of prostate cancer.
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Phenotypic heterogeneity of mutations in androgen receptor gene.
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Androgen and estrogen receptors: potential of crystallography in the fight against cancer.
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Expanding the therapeutic use of androgens via selective androgen receptor modulators (SARMs).
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Discovery of antiandrogen activity of nonsteroidal scaffolds of marketed drugs.
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Androgen receptor genotyping in a large Australasian cohort with androgen insensitivity syndrome; identification of four novel mutations.
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16892386 J.T.Moore, J.L.Collins, and K.H.Pearce (2006).
The nuclear receptor superfamily and drug discovery.
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Comparison of crystal structures of human androgen receptor ligand-binding domain complexed with various agonists reveals molecular determinants responsible for binding affinity.
  Protein Sci, 15, 987-999.
PDB codes: 2am9 2ama 2amb
16682621 L.Xin, M.A.Teitell, D.A.Lawson, A.Kwon, I.K.Mellinghoff, and O.N.Witte (2006).
Progression of prostate cancer by synergy of AKT with genotropic and nongenotropic actions of the androgen receptor.
  Proc Natl Acad Sci U S A, 103, 7789-7794.  
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A fluorescent indicator to visualize activities of the androgen receptor ligands in single living cells.
  Angew Chem Int Ed Engl, 45, 2707-2712.  
16759873 P.Marwah, A.Marwah, H.A.Lardy, H.Miyamoto, and C.Chang (2006).
C19-steroids as androgen receptor modulators: design, discovery, and structure-activity relationship of new steroidal androgen receptor antagonists.
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16474655 A.S.Singh, C.H.Chau, D.K.Price, and W.D.Figg (2005).
Mechanisms of disease: Polymorphisms of androgen regulatory genes in the development of prostate cancer.
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Structural basis for accommodation of nonsteroidal ligands in the androgen receptor.
  J Biol Chem, 280, 37747-37754.
PDB codes: 2ax6 2ax7 2ax8 2ax9 2axa
15833816 C.E.Bohl, W.Gao, D.D.Miller, C.E.Bell, and J.T.Dalton (2005).
Structural basis for antagonism and resistance of bicalutamide in prostate cancer.
  Proc Natl Acad Sci U S A, 102, 6201-6206.
PDB code: 1z95
15860367 C.Y.Chang, and D.P.McDonnell (2005).
Androgen receptor-cofactor interactions as targets for new drug discovery.
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Androgen receptor mutants detected in recurrent prostate cancer exhibit diverse functional characteristics.
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Mutation of the androgen receptor causes oncogenic transformation of the prostate.
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In vitro and in vivo structure-activity relationships of novel androgen receptor ligands with multiple substituents in the B-ring.
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Crystal structure of a mutant mineralocorticoid receptor responsible for hypertension.
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PDB codes: 1y9r 1ya3
15789554 R.Maltais, C.Mercier, F.Labrie, and D.Poirier (2005).
Solid-phase synthesis of model libraries of 3alpha,17beta-dihydroxy-16alpha-(aminoethyl-N-substituted)-5alpha-androstanes for the development of steroidal therapeutic agents.
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16159155 W.Gao, C.E.Bohl, and J.T.Dalton (2005).
Chemistry and structural biology of androgen receptor.
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16061183 Y.Li, K.Suino, J.Daugherty, and H.E.Xu (2005).
Structural and biochemical mechanisms for the specificity of hormone binding and coactivator assembly by mineralocorticoid receptor.
  Mol Cell, 19, 367-380.
PDB code: 2a3i
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Molecular Basis of Steroid Action in the Prostate.
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15239655 C.E.Bohl, C.Chang, M.L.Mohler, J.Chen, D.D.Miller, P.W.Swaan, and J.T.Dalton (2004).
A ligand-based approach to identify quantitative structure-activity relationships for the androgen receptor.
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15328534 E.Hur, S.J.Pfaff, E.S.Payne, H.Grøn, B.M.Buehrer, and R.J.Fletterick (2004).
Recognition and accommodation at the androgen receptor coactivator binding interface.
  PLoS Biol, 2, E274.
PDB codes: 1t73 1t74 1t76 1t79 1t7f 1t7m 1t7r 1t7t
15264248 G.Buchanan, P.S.Craft, M.Yang, A.Cheong, J.Prescott, L.Jia, G.A.Coetzee, and W.D.Tilley (2004).
PC-3 cells with enhanced androgen receptor signaling: a model for clonal selection in prostate cancer.
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Androgen receptor: a key molecule in the progression of prostate cancer to hormone independence.
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Electrostatic modulation in steroid receptor recruitment of LXXLL and FXXLF motifs.
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Key structural features of nonsteroidal ligands for binding and activation of the androgen receptor.
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16604181 G.F.Allan, and Z.Sui (2003).
Therapeutic androgen receptor ligands.
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Interaction of organophosphate pesticides and related compounds with the androgen receptor.
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14635106 J.H.Wu, B.Gottlieb, G.Batist, T.Sulea, E.O.Purisima, L.K.Beitel, and M.Trifiro (2003).
Bridging structural biology and genetics by computational methods: an investigation into how the R774C mutation in the AR gene can result in complete androgen insensitivity syndrome.
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Beta-catenin binds to the activation function 2 region of the androgen receptor and modulates the effects of the N-terminal domain and TIF2 on ligand-dependent transcription.
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Interactions of androgens, green tea catechins and the antiandrogen flutamide with the external glucose-binding site of the human erythrocyte glucose transporter GLUT1.
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R726L androgen receptor mutation is uncommon in prostate cancer families in the united states.
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Structure-function relationships of vitamin D including ligand recognition by the vitamin D receptor.
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12616628 T.Mordasini, A.Curioni, R.Bursi, and W.Andreoni (2003).
The binding mode of progesterone to its receptor deduced from molecular dynamics simulations.
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A novel point mutation of the androgen receptor (F804L) in an Egyptian newborn with complete androgen insensitivity associated with congenital glaucoma and hypertrophic pyloric stenosis.
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12220494 G.B.Wisely, A.B.Miller, R.G.Davis, A.D.Thornquest, R.Johnson, T.Spitzer, A.Sefler, B.Shearer, J.T.Moore, A.B.Miller, T.M.Willson, and S.P.Williams (2002).
Hepatocyte nuclear factor 4 is a transcription factor that constitutively binds fatty acids.
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PDB code: 1lv2
12223047 I.K.Mellinghoff, and C.L.Sawyers (2002).
The emergence of resistance to targeted cancer therapeutics.
  Pharmacogenomics, 3, 603-623.  
12115546 K.Steketee, L.Timmerman, A.C.Ziel-van der Made, P.Doesburg, A.O.Brinkmann, and J.Trapman (2002).
Broadened ligand responsiveness of androgen receptor mutants obtained by random amino acid substitution of H874 and mutation hot spot T877 in prostate cancer.
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11971970 M.Fu, C.Wang, J.Wang, X.Zhang, T.Sakamaki, Y.G.Yeung, C.Chang, T.Hopp, S.A.Fuqua, E.Jaffray, R.T.Hay, J.J.Palvimo, O.A.Jänne, and R.G.Pestell (2002).
Androgen receptor acetylation governs trans activation and MEKK1-induced apoptosis without affecting in vitro sumoylation and trans-repression function.
  Mol Cell Biol, 22, 3373-3388.  
11849240 S.F.Ahmed, and I.A.Hughes (2002).
The genetics of male undermasculinization.
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Formation of the androgen receptor transcription complex.
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11793469 Z.Q.Yuan, B.Gottlieb, L.K.Beitel, N.Wong, P.H.Gordon, Q.Wang, A.Puisieux, W.D.Foulkes, and M.Trifiro (2002).
Polymorphisms and HNPCC: PMS2-MLH1 protein interactions diminished by single nucleotide polymorphisms.
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Participation of critical residues from the extreme C-terminal end of the human androgen receptor in the ligand binding function.
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11396657 C.J.Loy, and E.L.Yong (2001).
Sex, infertility and the molecular biology of the androgen receptor.
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11320241 J.S.Sack, K.F.Kish, C.Wang, R.M.Attar, S.E.Kiefer, Y.An, G.Y.Wu, J.E.Scheffler, M.E.Salvati, S.R.Krystek, R.Weinmann, and H.M.Einspahr (2001).
Crystallographic structures of the ligand-binding domains of the androgen receptor and its T877A mutant complexed with the natural agonist dihydrotestosterone.
  Proc Natl Acad Sci U S A, 98, 4904-4909.
PDB codes: 1i37 1i38
11607933 U.Egner, N.Heinrich, M.Ruff, M.Gangloff, A.Mueller-Fahrnow, and J.M.Wurtz (2001).
Different ligands-different receptor conformations: modeling of the hER alpha LBD in complex with agonists and antagonists.
  Med Res Rev, 21, 523-539.  
11358696 Y.Shi, and J.T.Koh (2001).
Selective regulation of gene expression by an orthogonal estrogen receptor-ligand pair created by polar-group exchange.
  Chem Biol, 8, 501-510.  
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