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Volumn 11, Issue 9, 2016, Pages 2499-2505

EPI-001, A Compound Active against Castration-Resistant Prostate Cancer, Targets Transactivation Unit 5 of the Androgen Receptor

Author keywords

[No Author keywords available]

Indexed keywords

ACTIVATION FUNCTION 1 PROTEIN; ANDROGEN RECEPTOR; ANDROGEN RECEPTOR ANTAGONIST; CYTOTOXIC AGENT; EPI 001; GENERAL TRANSCRIPTION FACTOR; TRANSCRIPTION ACTIVATION UNIT 5 PROTEIN; UNCLASSIFIED DRUG; BENZHYDRYL DERIVATIVE; CHLOROHYDRIN DERIVATIVE;

EID: 84987892499     PISSN: 15548929     EISSN: 15548937     Source Type: Journal    
DOI: 10.1021/acschembio.6b00182     Document Type: Article
Times cited : (107)

References (39)
  • 1
    • 0036645414 scopus 로고    scopus 로고
    • Molecular Biology of the Androgen Receptor
    • Gelmann, E. P. (2002) Molecular Biology of the Androgen Receptor J. Clin. Oncol. 20, 3001-3015 10.1200/JCO.2002.10.018
    • (2002) J. Clin. Oncol. , vol.20 , pp. 3001-3015
    • Gelmann, E.P.1
  • 2
    • 68149098902 scopus 로고    scopus 로고
    • Combined androgen blockade with bicalutamide for advanced prostate cancer
    • Akaza, H., Hinotsu, S., Usami, M., Arai, Y., Kanetake, H., Naito, S., and Hirao, Y. (2009) Combined androgen blockade with bicalutamide for advanced prostate cancer Cancer 115, 3437-3445 10.1002/cncr.24395
    • (2009) Cancer , vol.115 , pp. 3437-3445
    • Akaza, H.1    Hinotsu, S.2    Usami, M.3    Arai, Y.4    Kanetake, H.5    Naito, S.6    Hirao, Y.7
  • 3
    • 60149089419 scopus 로고    scopus 로고
    • Androgen deprivation therapy: Progress in understanding mechanisms of resistance and optimizing androgen depletion
    • Harris, W. P., Mostaghel, E. A., Nelson, P. S., and Montgomery, B. (2009) Androgen deprivation therapy: progress in understanding mechanisms of resistance and optimizing androgen depletion Nat. Clin. Pract. Urol. 6, 76-85 10.1038/ncpuro1296
    • (2009) Nat. Clin. Pract. Urol. , vol.6 , pp. 76-85
    • Harris, W.P.1    Mostaghel, E.A.2    Nelson, P.S.3    Montgomery, B.4
  • 4
    • 84890555121 scopus 로고    scopus 로고
    • Prostate cancer progression after androgen deprivation therapy: Mechanisms of castrate resistance and novel therapeutic approaches
    • Karantanos, T., Corn, P. G., and Thompson, T. C. (2013) Prostate cancer progression after androgen deprivation therapy: mechanisms of castrate resistance and novel therapeutic approaches Oncogene 32, 5501-5511 10.1038/onc.2013.206
    • (2013) Oncogene , vol.32 , pp. 5501-5511
    • Karantanos, T.1    Corn, P.G.2    Thompson, T.C.3
  • 5
    • 0037205522 scopus 로고    scopus 로고
    • Conformational analysis of the androgen receptor amino-terminal domain involved in transactivation. Influence of structure-stabilizing solutes and protein-protein interactions
    • Reid, J., Kelly, S. M., Watt, K., Price, N. C., and McEwan, I. J. (2002) Conformational analysis of the androgen receptor amino-terminal domain involved in transactivation. Influence of structure-stabilizing solutes and protein-protein interactions J. Biol. Chem. 277, 20079-20086 10.1074/jbc.M201003200
    • (2002) J. Biol. Chem. , vol.277 , pp. 20079-20086
    • Reid, J.1    Kelly, S.M.2    Watt, K.3    Price, N.C.4    McEwan, I.J.5
  • 6
    • 40849144778 scopus 로고    scopus 로고
    • Structural characterization of the native NH2-terminal transactivation domain of the human androgen receptor: A collapsed disordered conformation underlies structural plasticity and protein-induced folding
    • Lavery, D. N. and McEwan, I. J. (2008) Structural characterization of the native NH2-terminal transactivation domain of the human androgen receptor: a collapsed disordered conformation underlies structural plasticity and protein-induced folding Biochemistry 47, 3360-3369 10.1021/bi702221e
    • (2008) Biochemistry , vol.47 , pp. 3360-3369
    • Lavery, D.N.1    McEwan, I.J.2
  • 7
    • 33846609681 scopus 로고    scopus 로고
    • Androgen receptor decoy molecules block the growth of prostate cancer
    • Quayle, S. N., Mawji, N. R., Wang, J., and Sadar, M. D. (2007) Androgen receptor decoy molecules block the growth of prostate cancer Proc. Natl. Acad. Sci. U. S. A. 104, 1331-1336 10.1073/pnas.0606718104
    • (2007) Proc. Natl. Acad. Sci. U. S. A. , vol.104 , pp. 1331-1336
    • Quayle, S.N.1    Mawji, N.R.2    Wang, J.3    Sadar, M.D.4
  • 10
    • 77955327536 scopus 로고    scopus 로고
    • Intrinsically disordered proteins are potential drug targets
    • Metallo, S. J. (2010) Intrinsically disordered proteins are potential drug targets Curr. Opin. Chem. Biol. 14, 481-488 10.1016/j.cbpa.2010.06.169
    • (2010) Curr. Opin. Chem. Biol. , vol.14 , pp. 481-488
    • Metallo, S.J.1
  • 11
    • 84940467045 scopus 로고    scopus 로고
    • Targeting disordered proteins with small molecules using entropy
    • Heller, G. T., Sormanni, P., and Vendruscolo, M. (2015) Targeting disordered proteins with small molecules using entropy Trends Biochem. Sci. 40, 491-496 10.1016/j.tibs.2015.07.004
    • (2015) Trends Biochem. Sci. , vol.40 , pp. 491-496
    • Heller, G.T.1    Sormanni, P.2    Vendruscolo, M.3
  • 15
    • 82655180375 scopus 로고    scopus 로고
    • Intrinsic disorder in the androgen receptor: Identification, characterisation and drugability
    • McEwan, I. J. (2012) Intrinsic disorder in the androgen receptor: identification, characterisation and drugability Mol. BioSyst. 8, 82-90 10.1039/C1MB05249G
    • (2012) Mol. BioSyst. , vol.8 , pp. 82-90
    • McEwan, I.J.1
  • 18
    • 0028904382 scopus 로고
    • Identification of two transcription activation units in the N-terminal domain of the human androgen receptor
    • Jenster, G., van der Korput, H. A. G. M., Trapman, J., and Brinkmann, A. O. (1995) Identification of two transcription activation units in the N-terminal domain of the human androgen receptor J. Biol. Chem. 270, 7341-7346 10.1074/jbc.270.13.7341
    • (1995) J. Biol. Chem. , vol.270 , pp. 7341-7346
    • Jenster, G.1    Van Der Korput, H.A.G.M.2    Trapman, J.3    Brinkmann, A.O.4
  • 19
    • 31544451068 scopus 로고    scopus 로고
    • Interplay between two hormone-independent activation domains in the androgen receptor
    • Callewaert, L., Van Tilborgh, N., and Claessens, F. (2006) Interplay between two hormone-independent activation domains in the androgen receptor Cancer Res. 66, 543-553 10.1158/0008-5472.CAN-05-2389
    • (2006) Cancer Res. , vol.66 , pp. 543-553
    • Callewaert, L.1    Van Tilborgh, N.2    Claessens, F.3
  • 20
    • 35448947810 scopus 로고    scopus 로고
    • Selective role of an NH2-terminal WxxLF motif for aberrant androgen receptor activation in androgen depletion independent prostate cancer cells
    • Dehm, S. M., Regan, K. M., Schmidt, L. J., and Tindall, D. J. (2007) Selective role of an NH2-terminal WxxLF motif for aberrant androgen receptor activation in androgen depletion independent prostate cancer cells Cancer Res. 67, 10067-10077 10.1158/0008-5472.CAN-07-1267
    • (2007) Cancer Res. , vol.67 , pp. 10067-10077
    • Dehm, S.M.1    Regan, K.M.2    Schmidt, L.J.3    Tindall, D.J.4
  • 21
    • 0037439106 scopus 로고    scopus 로고
    • A novel inducible transactivation domain in the androgen receptor: Implications for PRK in prostate cancer
    • Metzger, E., Müller, J. M., Ferrari, S., Buettner, R., and Schüle, R. (2003) A novel inducible transactivation domain in the androgen receptor: implications for PRK in prostate cancer EMBO J. 22, 270-280 10.1093/emboj/cdg023
    • (2003) EMBO J. , vol.22 , pp. 270-280
    • Metzger, E.1    Müller, J.M.2    Ferrari, S.3    Buettner, R.4    Schüle, R.5
  • 22
    • 1542743970 scopus 로고    scopus 로고
    • Induced alpha-helix structure in AF1 of the androgen receptor upon binding transcription factor TFIIF
    • Kumar, R., Betney, R., Li, J., Thompson, E. B., and McEwan, I. J. (2004) Induced alpha-helix structure in AF1 of the androgen receptor upon binding transcription factor TFIIF Biochemistry 43, 3008-3013 10.1021/bi035934p
    • (2004) Biochemistry , vol.43 , pp. 3008-3013
    • Kumar, R.1    Betney, R.2    Li, J.3    Thompson, E.B.4    McEwan, I.J.5
  • 23
    • 78650615363 scopus 로고    scopus 로고
    • Sequence-specific random coil chemical shifts of intrinsically disordered proteins
    • Tamiola, K., Acar, B., and Mulder, F. A. A. (2010) Sequence-specific random coil chemical shifts of intrinsically disordered proteins J. Am. Chem. Soc. 132, 18000-18003 10.1021/ja105656t
    • (2010) J. Am. Chem. Soc. , vol.132 , pp. 18000-18003
    • Tamiola, K.1    Acar, B.2    Mulder, F.A.A.3
  • 24
    • 33751552347 scopus 로고    scopus 로고
    • Sensitivity of secondary structure propensities to sequence differences between alpha- and gamma-synuclein: Implications for fibrillation
    • Marsh, J. A., Singh, V. K., Jia, Z., and Forman-Kay, J. D. (2006) Sensitivity of secondary structure propensities to sequence differences between alpha- and gamma-synuclein: implications for fibrillation Protein Sci. 15, 2795-2804 10.1110/ps.062465306
    • (2006) Protein Sci. , vol.15 , pp. 2795-2804
    • Marsh, J.A.1    Singh, V.K.2    Jia, Z.3    Forman-Kay, J.D.4
  • 29
    • 3142672066 scopus 로고    scopus 로고
    • An androgen receptor NH2-terminal conserved motif interacts with the COOH terminus of the Hsp70-interacting protein (CHIP)
    • He, B., Bai, S., Hnat, A. T., Kalman, R. I., Minges, J. T., Patterson, C., and Wilson, E. M. (2004) An androgen receptor NH2-terminal conserved motif interacts with the COOH terminus of the Hsp70-interacting protein (CHIP) J. Biol. Chem. 279, 30643-30653 10.1074/jbc.M403117200
    • (2004) J. Biol. Chem. , vol.279 , pp. 30643-30653
    • He, B.1    Bai, S.2    Hnat, A.T.3    Kalman, R.I.4    Minges, J.T.5    Patterson, C.6    Wilson, E.M.7
  • 30
    • 77955428685 scopus 로고    scopus 로고
    • Cross talk between epidermal growth factor (EGF) receptor and extra nuclear steroid receptors in cell lines
    • Migliaccio, A., Castoria, G., Giovannelli, P., and Auricchio, F. (2010) Cross talk between epidermal growth factor (EGF) receptor and extra nuclear steroid receptors in cell lines Mol. Cell. Endocrinol. 327, 19-24 10.1016/j.mce.2010.06.014
    • (2010) Mol. Cell. Endocrinol. , vol.327 , pp. 19-24
    • Migliaccio, A.1    Castoria, G.2    Giovannelli, P.3    Auricchio, F.4
  • 32
    • 84878259928 scopus 로고    scopus 로고
    • Polyproline-II helix in proteins: Structure and function
    • Adzhubei, A. A., Sternberg, M. J. E., and Makarov, A. A. (2013) Polyproline-II helix in proteins: structure and function J. Mol. Biol. 425, 2100-2132 10.1016/j.jmb.2013.03.018
    • (2013) J. Mol. Biol. , vol.425 , pp. 2100-2132
    • Adzhubei, A.A.1    Sternberg, M.J.E.2    Makarov, A.A.3
  • 33
    • 0034725648 scopus 로고    scopus 로고
    • FXXLF and WXXLF sequences mediate the NH2-terminal interaction with the ligand binding domain of the androgen receptor
    • He, B., Kemppainen, J. A., and Wilson, E. M. (2000) FXXLF and WXXLF sequences mediate the NH2-terminal interaction with the ligand binding domain of the androgen receptor J. Biol. Chem. 275, 22986-22994 10.1074/jbc.M002807200
    • (2000) J. Biol. Chem. , vol.275 , pp. 22986-22994
    • He, B.1    Kemppainen, J.A.2    Wilson, E.M.3
  • 34
    • 19344376991 scopus 로고    scopus 로고
    • Recognition and accommodation at the androgen receptor coactivator binding interface
    • Hur, E., Pfaff, S. J., Payne, E. S., Grøn, H., Buehrer, B. M., and Fletterick, R. J. (2004) Recognition and accommodation at the androgen receptor coactivator binding interface PLoS Biol. 2, E274 10.1371/journal.pbio.0020274
    • (2004) PLoS Biol. , vol.2 , pp. E274
    • Hur, E.1    Pfaff, S.J.2    Payne, E.S.3    Grøn, H.4    Buehrer, B.M.5    Fletterick, R.J.6
  • 35
    • 84859485587 scopus 로고    scopus 로고
    • Androgen receptor exon 1 mutation causes androgen insensitivity by creating phosphorylation site and inhibiting melanoma antigen-A11 activation of NH2- and carboxyl-terminal interaction-dependent transactivation
    • Lagarde, W. H., Blackwelder, A. J., Minges, J. T., Hnat, A. T., French, F. S., and Wilson, E. M. (2012) Androgen receptor exon 1 mutation causes androgen insensitivity by creating phosphorylation site and inhibiting melanoma antigen-A11 activation of NH2- and carboxyl-terminal interaction-dependent transactivation J. Biol. Chem. 287, 10905-10915 10.1074/jbc.M111.336081
    • (2012) J. Biol. Chem. , vol.287 , pp. 10905-10915
    • Lagarde, W.H.1    Blackwelder, A.J.2    Minges, J.T.3    Hnat, A.T.4    French, F.S.5    Wilson, E.M.6
  • 36
    • 0028447768 scopus 로고
    • Elucidating the folding problem of helical peptides using empirical parameters
    • Muñoz, V. and Serrano, L. (1994) Elucidating the folding problem of helical peptides using empirical parameters Nat. Struct. Biol. 1, 399-409 10.1038/nsb0694-399
    • (1994) Nat. Struct. Biol. , vol.1 , pp. 399-409
    • Muñoz, V.1    Serrano, L.2
  • 37
    • 77955839695 scopus 로고    scopus 로고
    • Cooperative formation of native-like tertiary contacts in the ensemble of unfolded states of a four-helix protein
    • Bruun, S. W., Iešmantavičius, V., Danielsson, J., and Poulsen, F. M. (2010) Cooperative formation of native-like tertiary contacts in the ensemble of unfolded states of a four-helix protein Proc. Natl. Acad. Sci. U. S. A. 107, 13306-13311 10.1073/pnas.1003004107
    • (2010) Proc. Natl. Acad. Sci. U. S. A. , vol.107 , pp. 13306-13311
    • Bruun, S.W.1    Iešmantavičius, V.2    Danielsson, J.3    Poulsen, F.M.4
  • 38
    • 82455179494 scopus 로고    scopus 로고
    • Understanding biomolecular motion, recognition, and allostery by use of conformational ensembles
    • Fenwick, R. B., Esteban-Martín, S., and Salvatella, X. (2011) Understanding biomolecular motion, recognition, and allostery by use of conformational ensembles Eur. Biophys. J. 40, 1339-1355 10.1007/s00249-011-0754-8
    • (2011) Eur. Biophys. J. , vol.40 , pp. 1339-1355
    • Fenwick, R.B.1    Esteban-Martín, S.2    Salvatella, X.3
  • 39
    • 1842637389 scopus 로고    scopus 로고
    • Structural basis of androgen receptor binding to selective androgen response elements
    • Shaffer, P. L., Jivan, A., Dollins, D. E., Claessens, F., and Gewirth, D. T. (2004) Structural basis of androgen receptor binding to selective androgen response elements Proc. Natl. Acad. Sci. U. S. A. 101, 4758-4763 10.1073/pnas.0401123101
    • (2004) Proc. Natl. Acad. Sci. U. S. A. , vol.101 , pp. 4758-4763
    • Shaffer, P.L.1    Jivan, A.2    Dollins, D.E.3    Claessens, F.4    Gewirth, D.T.5


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