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| <StructureSection load='2w8y' size='350' side='right' caption='Structure of human progesterone receptor ligand-binding domain complex with RU486 and sulfate (PDB entry [[2w8y]])' scene='78/780972/Cv/2'> | | <StructureSection load='2w8y' size='350' side='right' caption='Structure of human progesterone receptor ligand-binding domain complex with RU486 and sulfate (PDB entry [[2w8y]])' scene='78/780972/Cv/2'> |
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| | See also [[Intracellular receptors]] |
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| == Function == | | == Function == |
Revision as of 09:47, 12 January 2023
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See also Intracellular receptors
Function
Progesterone 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].
Relevance
The response to hormone therapy in breast cancer correlates with PR. PR absence in breast tumor cells predicts resistance to hormone therapy [2].
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 binding site and several PR-RU486 interactions[3]. Water molecules are shown as red spheres. Human progesterone receptor ligand-binding domain bound with progesterone (1a28).
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3D Structures of progesterone receptor
Updated on 12-January-2023
{"openlevels":0}
- Progesterone receptor residues 1-125
- Progesterone receptor residues 72-195
- Progesterone receptor DNA-binding domain residues 399-476
- Progesterone receptor ligand-binding domain residues 673-933
- 3g8o, 3hq5, 3kba, 4a2j, 4apu – hPR LBD + partial agonist
- 1zuc – hPR LBD + agonist
- 1sqn, 3d90 – hPR LBD + contraceptive
- 2w8y – hPR LBD + RU486
- 1a28 – hPR LBD + progesterone
- 1e3k – hPR LBD + metribolone
- 1sr7 – hPR LBD + skin inflammation drug
- 3zr7, 3zra, 3zrb – hPR LBD + modulator
- 2ovh, 2ovm – hPR LBD + modulator + co-repressor peptide
- 4oar – hPR LBD + contraceptive + co-repressor peptide
References
proteopedia link