Progesterone receptor: Difference between revisions
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== Function == | == Function == | ||
'''Progesterone receptor''' (PR) binds to DNA and inhibits transcription. | '''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>. | ||
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 == | ||
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Updated on {{REVISIONDAY2}}-{{MONTHNAME|{{REVISIONMONTH}}}}-{{REVISIONYEAR}} | Updated on {{REVISIONDAY2}}-{{MONTHNAME|{{REVISIONMONTH}}}}-{{REVISIONYEAR}} | ||
{{#tree:id=OrganizedByTopic|openlevels=0| | {{#tree:id=OrganizedByTopic|openlevels=0| | ||
* Progesterone receptor residues 1-125 | |||
**[[1ejf]] – hPR - human<br /> | |||
* Progesterone receptor residues 72-195 | * Progesterone receptor residues 72-195 | ||
**[[4x8y]] – hPR | **[[4x8y]] – hPR<br /> | ||
* Progesterone receptor DNA-binding domain residues 399-476 | * Progesterone receptor DNA-binding domain residues 399-476 | ||
Latest revision as of 12:29, 18 January 2024
FunctionProgesterone receptor (PR) binds to DNA and inhibits transcription. It is 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[1]. See also Intracellular receptors RelevanceThe response to hormone therapy in breast cancer correlates with PR. PR absence in breast tumor cells predicts resistance to hormone therapy [2]. Mometasone is a potent agonist of PR[3]. Structural highlightsThe 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 [4]. Water molecules are shown as red spheres. (1a28). |
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3D Structures of progesterone receptor3D Structures of progesterone receptor
Updated on 18-January-2024
ReferencesReferences
- ↑ 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