3kba

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[[Image:3kba.png|left|200px]]
 
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{{STRUCTURE_3kba| PDB=3kba | SCENE= }}
{{STRUCTURE_3kba| PDB=3kba | SCENE= }}
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===Progesterone receptor bound to sulfonamide pyrrolidine partial agonist===
===Progesterone receptor bound to sulfonamide pyrrolidine partial agonist===
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{{ABSTRACT_PUBMED_19926282}}
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==Function==
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[[http://www.uniprot.org/uniprot/PRGR_HUMAN PRGR_HUMAN]] The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Progesterone receptor isoform B (PRB) is involved activation of c-SRC/MAPK signaling on hormone stimulation.<ref>PMID:15572662</ref> <ref>PMID:15798179</ref> <ref>PMID:17020914</ref> <ref>PMID:17347654</ref> <ref>PMID:17717077</ref> <ref>PMID:17173941</ref> <ref>PMID:18202149</ref> Isoform A is inactive in stimulating c-Src/MAPK signaling on hormone stimulation.<ref>PMID:15572662</ref> <ref>PMID:15798179</ref> <ref>PMID:17020914</ref> <ref>PMID:17347654</ref> <ref>PMID:17717077</ref> <ref>PMID:17173941</ref> <ref>PMID:18202149</ref>
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{{ABSTRACT_PUBMED_19926282}}
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==About this Structure==
==About this Structure==
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==Reference==
==Reference==
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<ref group="xtra">PMID:19926282</ref><references group="xtra"/>
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<ref group="xtra">PMID:019926282</ref><references group="xtra"/><references/>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Kallander, L S.]]
[[Category: Kallander, L S.]]
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[[Category: Washburn, D G.]]
[[Category: Washburn, D G.]]
[[Category: Williams, S P.]]
[[Category: Williams, S P.]]
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[[Category: Nuclear receptor]]
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[[Category: Transcription]]
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[[Category: Transcription regulation]]

Revision as of 02:22, 4 April 2013

Template:STRUCTURE 3kba

Contents

Progesterone receptor bound to sulfonamide pyrrolidine partial agonist

Template:ABSTRACT PUBMED 19926282

Function

[PRGR_HUMAN] The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Progesterone receptor isoform B (PRB) is involved activation of c-SRC/MAPK signaling on hormone stimulation.[1] [2] [3] [4] [5] [6] [7] Isoform A is inactive in stimulating c-Src/MAPK signaling on hormone stimulation.[8] [9] [10] [11] [12] [13] [14]

About this Structure

3kba is a 2 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

  • Kallander LS, Washburn DG, Hoang TH, Frazee JS, Stoy P, Johnson L, Lu Q, Hammond M, Barton LS, Patterson JR, Azzarano LM, Nagilla R, Madauss KP, Williams SP, Stewart EL, Duraiswami C, Grygielko ET, Xu X, Laping NJ, Bray JD, Thompson SK. Improving the developability profile of pyrrolidine progesterone receptor partial agonists. Bioorg Med Chem Lett. 2010 Jan 1;20(1):371-4. Epub 2009 Oct 25. PMID:19926282 doi:10.1016/j.bmcl.2009.10.092
  1. ↑ Pierson-Mullany LK, Lange CA. Phosphorylation of progesterone receptor serine 400 mediates ligand-independent transcriptional activity in response to activation of cyclin-dependent protein kinase 2. Mol Cell Biol. 2004 Dec;24(24):10542-57. PMID:15572662 doi:10.1128/MCB.24.24.10542-10557.2004
  2. ↑ Narayanan R, Edwards DP, Weigel NL. Human progesterone receptor displays cell cycle-dependent changes in transcriptional activity. Mol Cell Biol. 2005 Apr;25(8):2885-98. PMID:15798179 doi:25/8/2885
  3. ↑ Man JH, Li HY, Zhang PJ, Zhou T, He K, Pan X, Liang B, Li AL, Zhao J, Gong WL, Jin BF, Xia Q, Yu M, Shen BF, Zhang XM. PIAS3 induction of PRB sumoylation represses PRB transactivation by destabilizing its retention in the nucleus. Nucleic Acids Res. 2006;34(19):5552-66. Epub 2006 Oct 4. PMID:17020914 doi:gkl691
  4. ↑ Zhang PJ, Zhao J, Li HY, Man JH, He K, Zhou T, Pan X, Li AL, Gong WL, Jin BF, Xia Q, Yu M, Shen BF, Zhang XM. CUE domain containing 2 regulates degradation of progesterone receptor by ubiquitin-proteasome. EMBO J. 2007 Apr 4;26(7):1831-42. Epub 2007 Mar 8. PMID:17347654 doi:7601602
  5. ↑ Daniel AR, Faivre EJ, Lange CA. Phosphorylation-dependent antagonism of sumoylation derepresses progesterone receptor action in breast cancer cells. Mol Endocrinol. 2007 Dec;21(12):2890-906. Epub 2007 Aug 23. PMID:17717077 doi:me.2007-0248
  6. ↑ Daniel AR, Qiu M, Faivre EJ, Ostrander JH, Skildum A, Lange CA. Linkage of progestin and epidermal growth factor signaling: phosphorylation of progesterone receptors mediates transcriptional hypersensitivity and increased ligand-independent breast cancer cell growth. Steroids. 2007 Feb;72(2):188-201. Epub 2006 Dec 14. PMID:17173941 doi:S0039-128X(06)00225-X
  7. ↑ Faivre EJ, Daniel AR, Hillard CJ, Lange CA. Progesterone receptor rapid signaling mediates serine 345 phosphorylation and tethering to specificity protein 1 transcription factors. Mol Endocrinol. 2008 Apr;22(4):823-37. Epub 2008 Jan 17. PMID:18202149 doi:me.2007-0437
  8. ↑ Pierson-Mullany LK, Lange CA. Phosphorylation of progesterone receptor serine 400 mediates ligand-independent transcriptional activity in response to activation of cyclin-dependent protein kinase 2. Mol Cell Biol. 2004 Dec;24(24):10542-57. PMID:15572662 doi:10.1128/MCB.24.24.10542-10557.2004
  9. ↑ Narayanan R, Edwards DP, Weigel NL. Human progesterone receptor displays cell cycle-dependent changes in transcriptional activity. Mol Cell Biol. 2005 Apr;25(8):2885-98. PMID:15798179 doi:25/8/2885
  10. ↑ Man JH, Li HY, Zhang PJ, Zhou T, He K, Pan X, Liang B, Li AL, Zhao J, Gong WL, Jin BF, Xia Q, Yu M, Shen BF, Zhang XM. PIAS3 induction of PRB sumoylation represses PRB transactivation by destabilizing its retention in the nucleus. Nucleic Acids Res. 2006;34(19):5552-66. Epub 2006 Oct 4. PMID:17020914 doi:gkl691
  11. ↑ Zhang PJ, Zhao J, Li HY, Man JH, He K, Zhou T, Pan X, Li AL, Gong WL, Jin BF, Xia Q, Yu M, Shen BF, Zhang XM. CUE domain containing 2 regulates degradation of progesterone receptor by ubiquitin-proteasome. EMBO J. 2007 Apr 4;26(7):1831-42. Epub 2007 Mar 8. PMID:17347654 doi:7601602
  12. ↑ Daniel AR, Faivre EJ, Lange CA. Phosphorylation-dependent antagonism of sumoylation derepresses progesterone receptor action in breast cancer cells. Mol Endocrinol. 2007 Dec;21(12):2890-906. Epub 2007 Aug 23. PMID:17717077 doi:me.2007-0248
  13. ↑ Daniel AR, Qiu M, Faivre EJ, Ostrander JH, Skildum A, Lange CA. Linkage of progestin and epidermal growth factor signaling: phosphorylation of progesterone receptors mediates transcriptional hypersensitivity and increased ligand-independent breast cancer cell growth. Steroids. 2007 Feb;72(2):188-201. Epub 2006 Dec 14. PMID:17173941 doi:S0039-128X(06)00225-X
  14. ↑ Faivre EJ, Daniel AR, Hillard CJ, Lange CA. Progesterone receptor rapid signaling mediates serine 345 phosphorylation and tethering to specificity protein 1 transcription factors. Mol Endocrinol. 2008 Apr;22(4):823-37. Epub 2008 Jan 17. PMID:18202149 doi:me.2007-0437

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