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PDBsum entry 1e3k

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Human progesterone receptor PDB id
1e3k
Jmol
Contents
Protein chain
251 a.a. *
Ligands
R18 ×2
Waters ×1
* Residue conservation analysis
PDB id:
1e3k
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
Resolution:
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
Date:
19-Jun-00     Release date:   14-Jun-01    
PROCHECK
Go to PROCHECK summary
 Headers
 References

Protein chains
Pfam   ArchSchema ?
P06401  (PRGR_HUMAN) -  Progesterone receptor
Seq:
Struc:
 
Seq:
Struc:
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.
 
  ABSTRACT  
 
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
21274273 D.N.Lavery, and C.L.Bevan (2011).
Androgen receptor signalling in prostate cancer: the functional consequences of acetylation.
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20333619 A.S.Veleiro, L.D.Alvarez, S.L.Eduardo, and G.Burton (2010).
Structure of the glucocorticoid receptor, a flexible protein that can adapt to different ligands.
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21031218 M.Huxley, C.Sanchez-Cano, M.J.Browning, C.Navarro-Ranninger, A.G.Quiroga, A.Rodger, and M.J.Hannon (2010).
An androgenic steroid delivery vector that imparts activity to a non-conventional platinum(ii) metallo-drug.
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20148675 P.Huang, V.Chandra, and F.Rastinejad (2010).
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21318111 R.Hu, S.R.Denmeade, and J.Luo (2010).
Molecular processes leading to aberrant androgen receptor signaling and castration resistance in prostate cancer.
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20624985 T.Friscić, R.W.Lancaster, L.Fábián, and P.G.Karamertzanis (2010).
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20708648 W.Gao (2010).
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19995608 X.E.Zhou, K.Suino-Powell, P.L.Ludidi, D.P.McDonnell, and H.E.Xu (2010).
Expression, purification and primary crystallographic study of human androgen receptor in complex with DNA and coactivator motifs.
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20011049 A.T.Szafran, S.Hartig, H.Sun, I.P.Uray, M.Szwarc, Y.Shen, S.N.Mediwala, J.Bell, M.J.McPhaul, M.A.Mancini, and M.Marcelli (2009).
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19427329 A.di Masi, E.De Marinis, P.Ascenzi, and M.Marino (2009).
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19171919 C.Féau, L.A.Arnold, A.Kosinski, and R.K.Guy (2009).
A high-throughput ligand competition binding assay for the androgen receptor and other nuclear receptors.
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19721807 G.N.Brooke, and C.L.Bevan (2009).
The role of androgen receptor mutations in prostate cancer progression.
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19389631 J.D.Norris, J.D.Joseph, A.B.Sherk, D.Juzumiene, P.S.Turnbull, S.W.Rafferty, H.Cui, E.Anderson, D.Fan, D.A.Dye, X.Deng, D.Kazmin, C.Y.Chang, T.M.Willson, and D.P.McDonnell (2009).
Differential presentation of protein interaction surfaces on the androgen receptor defines the pharmacological actions of bound ligands.
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19557178 M.E.Baker, D.J.Chang, and C.Chandsawangbhuwana (2009).
3D model of lamprey estrogen receptor with estradiol and 15alpha-hydroxy-estradiol.
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19861292 M.Tóth (2009).
[Myoanabolic steroids and selective androgen receptor modulators: mechanism of action and perspectives]
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19666041 R.Kumar, and G.Litwack (2009).
Structural and functional relationships of the steroid hormone receptors' N-terminal transactivation domain.
  Steroids, 74, 877-883.  
19178528 R.Tadokoro, T.Bunch, J.W.Schwabe, I.A.Hughes, and J.C.Murphy (2009).
Comparison of the molecular consequences of different mutations at residue 754 and 690 of the androgen receptor (AR) and androgen insensitivity syndrome (AIS) phenotype.
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20009327 S.B.Kim, Y.Umezawa, and H.Tao (2009).
Determination of the androgenicity of ligands using a single-chain probe carrying androgen receptor N-terminal peptides.
  Anal Sci, 25, 1415-1420.  
19796750 Y.Chen, N.J.Clegg, and H.I.Scher (2009).
Anti-androgens and androgen-depleting therapies in prostate cancer: new agents for an established target.
  Lancet Oncol, 10, 981-991.  
18421785 A.A.Ramos, and J.C.Varela (2008).
Biochemistry and molecular biology in Portugal: an overview of past and current contributions.
  IUBMB Life, 60, 265-269.  
18612376 F.Claessens, S.Denayer, N.Van Tilborgh, S.Kerkhofs, C.Helsen, and A.Haelens (2008).
Diverse roles of androgen receptor (AR) domains in AR-mediated signaling.
  Nucl Recept Signal, 6, e008.  
18037956 G.N.Brooke, M.G.Parker, and C.L.Bevan (2008).
Mechanisms of androgen receptor activation in advanced prostate cancer: differential co-activator recruitment and gene expression.
  Oncogene, 27, 2941-2950.  
18502379 J.Zhang, and D.S.Geller (2008).
Helix 3-helix 5 interactions in steroid hormone receptor function.
  J Steroid Biochem Mol Biol, 109, 279-285.  
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.
  Mol Cell Biol, 28, 1915-1923.
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).
Discovery of an orally-active nonsteroidal androgen receptor pure antagonist and the structure-activity relationships of its derivatives.
  Chem Pharm Bull (Tokyo), 56, 1555-1561.  
18852122 M.C.Hodgson, H.C.Shen, A.N.Hollenberg, and S.P.Balk (2008).
Structural basis for nuclear receptor corepressor recruitment by antagonist-liganded androgen receptor.
  Mol Cancer Ther, 7, 3187-3194.  
19079612 R.Narayanan, M.L.Mohler, C.E.Bohl, D.D.Miller, and J.T.Dalton (2008).
Selective androgen receptor modulators in preclinical and clinical development.
  Nucl Recept Signal, 6, e010.  
18593950 S.M.Dehm, L.J.Schmidt, H.V.Heemers, R.L.Vessella, and D.J.Tindall (2008).
Splicing of a novel androgen receptor exon generates a constitutively active androgen receptor that mediates prostate cancer therapy resistance.
  Cancer Res, 68, 5469-5477.  
18330543 T.Harada, K.Yamagishi, T.Nakano, K.Kitaura, and H.Tokiwa (2008).
Ab initio fragment molecular orbital study of ligand binding to human progesterone receptor ligand-binding domain.
  Naunyn Schmiedebergs Arch Pharmacol, 377, 607-615.  
19094205 V.Douard, F.Brunet, B.Boussau, I.Ahrens, V.Vlaeminck-Guillem, B.Haendler, V.Laudet, and Y.Guiguen (2008).
The fate of the duplicated androgen receptor in fishes: a late neofunctionalization event?
  BMC Evol Biol, 8, 336.  
18637017 Y.D.Li, Y.Lu, G.C.Chen, and J.Lu (2008).
An S296R mutation in the human androgen receptor causes activation of the receptor by non-androgenic steroids and stronger inhibition by the nuclear receptor corepressor N-coR.
  Clin Exp Pharmacol Physiol, 35, 1252-1257.  
17164529 A.M.Hassell, G.An, R.K.Bledsoe, J.M.Bynum, H.L.Carter, S.J.Deng, R.T.Gampe, T.E.Grisard, K.P.Madauss, R.T.Nolte, W.J.Rocque, L.Wang, K.L.Weaver, S.P.Williams, G.B.Wisely, R.Xu, and L.M.Shewchuk (2007).
Crystallization of protein-ligand complexes.
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17311914 C.E.Bohl, Z.Wu, D.D.Miller, C.E.Bell, and J.T.Dalton (2007).
Crystal structure of the T877A human androgen receptor ligand-binding domain complexed to cyproterone acetate provides insight for ligand-induced conformational changes and structure-based drug design.
  J Biol Chem, 282, 13648-13655.
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.
  Annu Rev Physiol, 69, 201-220.  
  18007998 J.K.Hess-Wilson, S.L.Webb, H.K.Daly, Y.K.Leung, J.Boldison, C.E.Comstock, M.A.Sartor, S.M.Ho, and K.E.Knudsen (2007).
Unique bisphenol A transcriptome in prostate cancer: novel effects on ERbeta expression that correspond to androgen receptor mutation status.
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17013809 K.P.Madauss, E.L.Stewart, and S.P.Williams (2007).
The evolution of progesterone receptor ligands.
  Med Res Rev, 27, 374-400.  
17306029 M.E.Baker, C.Chandsawangbhuwana, and N.Ollikainen (2007).
Structural analysis of the evolution of steroid specificity in the mineralocorticoid and glucocorticoid receptors.
  BMC Evol Biol, 7, 24.  
17163421 R.Chmelar, G.Buchanan, E.F.Need, W.Tilley, and N.M.Greenberg (2007).
Androgen receptor coregulators and their involvement in the development and progression of prostate cancer.
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17334586 S.Rajender, L.Singh, and K.Thangaraj (2007).
Phenotypic heterogeneity of mutations in androgen receptor gene.
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17300979 V.Nahoum, and W.Bourguet (2007).
Androgen and estrogen receptors: potential of crystallography in the fight against cancer.
  Int J Biochem Cell Biol, 39, 1280-1287.  
17331889 W.Gao, and J.T.Dalton (2007).
Expanding the therapeutic use of androgens via selective androgen receptor modulators (SARMs).
  Drug Discov Today, 12, 241-248.  
17606915 W.H.Bisson, A.V.Cheltsov, N.Bruey-Sedano, B.Lin, J.Chen, N.Goldberger, L.T.May, A.Christopoulos, J.T.Dalton, P.M.Sexton, X.K.Zhang, and R.Abagyan (2007).
Discovery of antiandrogen activity of nonsteroidal scaffolds of marketed drugs.
  Proc Natl Acad Sci U S A, 104, 11927-11932.  
  17937062 Y.W.Jeske, I.N.McGown, D.M.Cowley, C.Oley, M.J.Thomsett, C.S.Choong, and A.M.Cotterill (2007).
Androgen receptor genotyping in a large Australasian cohort with androgen insensitivity syndrome; identification of four novel mutations.
  J Pediatr Endocrinol Metab, 20, 893-908.  
16892386 J.T.Moore, J.L.Collins, and K.H.Pearce (2006).
The nuclear receptor superfamily and drug discovery.
  ChemMedChem, 1, 504-523.  
16641486 K.Pereira de Jésus-Tran, P.L.Côté, L.Cantin, J.Blanchet, F.Labrie, and R.Breton (2006).
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.  
16555356 M.Awais, M.Sato, X.Lee, and Y.Umezawa (2006).
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.
  Bioorg Med Chem, 14, 5933-5947.  
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.
  Nat Clin Pract Urol, 2, 101-107.  
16129672 C.E.Bohl, D.D.Miller, J.Chen, C.E.Bell, and J.T.Dalton (2005).
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.
  Trends Pharmacol Sci, 26, 225-228.  
15617028 G.Chen, X.Wang, S.Zhang, Y.Lu, Y.Sun, J.Zhang, Z.Li, and J.Lu (2005).
Androgen receptor mutants detected in recurrent prostate cancer exhibit diverse functional characteristics.
  Prostate, 63, 395-406.  
15657128 G.Han, G.Buchanan, M.Ittmann, J.M.Harris, X.Yu, F.J.Demayo, W.Tilley, and N.M.Greenberg (2005).
Mutation of the androgen receptor causes oncogenic transformation of the prostate.
  Proc Natl Acad Sci U S A, 102, 1151-1156.  
16166218 J.Chen, D.J.Hwang, K.Chung, C.E.Bohl, S.J.Fisher, D.D.Miller, and J.T.Dalton (2005).
In vitro and in vivo structure-activity relationships of novel androgen receptor ligands with multiple substituents in the B-ring.
  Endocrinology, 146, 5444-5454.  
15908963 J.Fagart, J.Huyet, G.M.Pinon, M.Rochel, C.Mayer, and M.E.Rafestin-Oblin (2005).
Crystal structure of a mutant mineralocorticoid receptor responsible for hypertension.
  Nat Struct Mol Biol, 12, 554-555.
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.
  Chem Rev, 105, 3352-3370.  
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
  16971966 Y.S.Zhu (2005).
Molecular Basis of Steroid Action in the Prostate.
  Cellscience, 1, 27-55.  
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.
  J Med Chem, 47, 3765-3776.  
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.
  Prostate, 60, 352-366.  
14755679 M.E.Taplin, and S.P.Balk (2004).
Androgen receptor: a key molecule in the progression of prostate cancer to hormone independence.
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12612084 B.He, and E.M.Wilson (2003).
Electrostatic modulation in steroid receptor recruitment of LXXLL and FXXLF motifs.
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12488554 D.Yin, Y.He, M.A.Perera, S.S.Hong, C.Marhefka, N.Stourman, L.Kirkovsky, D.D.Miller, and J.T.Dalton (2003).
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.
  Nucl Recept Signal, 1, e009.  
  12676613 H.Tamura, H.Yoshikawa, K.W.Gaido, S.M.Ross, R.K.DeLisle, W.J.Welsh, and A.M.Richard (2003).
Interaction of organophosphate pesticides and related compounds with the androgen receptor.
  Environ Health Perspect, 111, 545-552.  
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.
  Hum Mutat, 22, 465-475.  
12588987 L.N.Song, R.Herrell, S.Byers, S.Shah, E.M.Wilson, and E.P.Gelmann (2003).
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.
  Mol Cell Biol, 23, 1674-1687.  
12970085 R.J.Naftalin, I.Afzal, P.Cunningham, M.Halai, C.Ross, N.Salleh, and S.R.Milligan (2003).
Interactions of androgens, green tea catechins and the antiandrogen flutamide with the external glucose-binding site of the human erythrocyte glucose transporter GLUT1.
  Br J Pharmacol, 140, 487-499.  
12539229 S.B.Gruber, H.Chen, L.P.Tomsho, N.Lee, E.E.Perrone, and K.A.Cooney (2003).
R726L androgen receptor mutation is uncommon in prostate cancer families in the united states.
  Prostate, 54, 306-309.  
12424754 S.Yamada, M.Shimizu, and K.Yamamoto (2003).
Structure-function relationships of vitamin D including ligand recognition by the vitamin D receptor.
  Med Res Rev, 23, 89.  
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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12519373 Y.Z.Gad, I.Mazen, S.Lumbroso, S.A.Temtamy, and C.Sultan (2003).
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.
  Clin Genet, 63, 59-63.  
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.
  Structure, 10, 1225-1234.
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.
  Int J Cancer, 100, 309-317.  
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.
  Clin Endocrinol (Oxf), 56, 1.  
11931767 Y.Shang, M.Myers, and M.Brown (2002).
Formation of the androgen receptor transcription complex.
  Mol Cell, 9, 601-610.  
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.
  Hum Mutat, 19, 108-113.  
11456479 B.Tahiri, G.Auzou, J.C.Nicolas, C.Sultan, and B.Lupo (2001).
Participation of critical residues from the extreme C-terminal end of the human androgen receptor in the ligand binding function.
  Biochemistry, 40, 8431-8437.  
11396657 C.J.Loy, and E.L.Yong (2001).
Sex, infertility and the molecular biology of the androgen receptor.
  Curr Opin Obstet Gynecol, 13, 315-321.  
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.  
The most recent references are shown first. Citation data come partly from CiteXplore and partly from an automated harvesting procedure. Note that this is likely to be only a partial list as not all journals are covered by either method. However, we are continually building up the citation data so more and more references will be included with time. Where a reference describes a PDB structure, the PDB code is shown on the right.