Progesterone receptor
From Proteopedia
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'''Progesterone receptor''' (PR) binds to DNA and inhibits transcription. It is [[Nuclear receptors|nuclear receptor]]. The inhibition terminates when progesterone binds to PR. The ovarian steroid progesterone which is essential for breast development and reproductive behavior, is mediated by PR<ref>PMID:19072517</ref>. | '''Progesterone receptor''' (PR) binds to DNA and inhibits transcription. It is [[Nuclear receptors|nuclear receptor]]. The inhibition terminates when progesterone binds to PR. The ovarian steroid progesterone which is essential for breast development and reproductive behavior, is mediated by PR<ref>PMID:19072517</ref>. | ||
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| + | See also [[Intracellular receptors]] | ||
== Relevance == | == Relevance == | ||
| - | The response to hormone therapy in breast cancer correlates with PR. PR absence in breast tumor cells predicts resistance to hormone therapy <ref>PMID:16234531</ref>. | + | The response to hormone therapy in breast cancer correlates with PR. PR absence in breast tumor cells predicts resistance to hormone therapy <ref>PMID:16234531</ref>. [[Mometasone]] is a potent agonist of PR<ref>PMID:15189034</ref>. |
== Structural highlights == | == Structural highlights == | ||
| - | The structure of the complex of the ligand-binding domain of PR with RU486 - an abortion-inducing drug - shows the ligand bound at a similar location to other agonists or partial agonists with a flexible loop of PR being a possible entry route to the <scene name='78/780972/Cv/4'>binding site and several PR-RU486 interactions</scene><ref>PMID:19372222</ref>. Water molecules are shown as red spheres. | + | The structure of the complex of the ligand-binding domain of PR with RU486 - an abortion-inducing drug - shows the ligand bound at a similar location to other agonists or partial agonists with a flexible loop of PR being a possible entry route to the <scene name='78/780972/Cv/4'>binding site and several PR-RU486 interactions</scene><ref>PMID:19372222</ref>. Water molecules are shown as red spheres. <scene name='89/895670/Cv/8'>Human progesterone receptor ligand-binding domain bound with progesterone</scene> ([[1a28]]). |
</StructureSection> | </StructureSection> | ||
== 3D Structures of progesterone receptor == | == 3D Structures of progesterone receptor == | ||
Current revision
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3D Structures of progesterone receptor
Updated on 18-January-2024
References
- ↑ Lange CA, Yee D. Progesterone and breast cancer. Womens Health (Lond). 2008 Mar;4(2):151-62. doi: 10.2217/17455057.4.2.151. PMID:19072517 doi:http://dx.doi.org/10.2217/17455057.4.2.151
- ↑ Cui X, Schiff R, Arpino G, Osborne CK, Lee AV. Biology of progesterone receptor loss in breast cancer and its implications for endocrine therapy. J Clin Oncol. 2005 Oct 20;23(30):7721-35. doi: 10.1200/JCO.2005.09.004. PMID:16234531 doi:http://dx.doi.org/10.1200/JCO.2005.09.004
- ↑ Madauss KP, Deng SJ, Austin RJ, Lambert MH, McLay I, Pritchard J, Short SA, Stewart EL, Uings IJ, Williams SP. Progesterone receptor ligand binding pocket flexibility: crystal structures of the norethindrone and mometasone furoate complexes. J Med Chem. 2004 Jun 17;47(13):3381-7. PMID:15189034 doi:http://dx.doi.org/10.1021/jm030640n
- ↑ Raaijmakers HC, Versteegh JE, Uitdehaag JC. The X-ray structure of RU486 bound to the progesterone receptor in a destabilized agonistic conformation. J Biol Chem. 2009 Jul 17;284(29):19572-9. Epub 2009 Apr 16. PMID:19372222 doi:http://dx.doi.org/10.1074/jbc.M109.007872
