Prostaglandin F synthase

Function Prostaglandin F synthase (AKR1C3) catalyzes the conversion of aldehydes and ketones to alcohol using NADH or NADP as cofactor. It catalyzes the isomerization of prostaglandin H2 (PGH2) to prostaglandin F2α (PGF2α) and the formation of 11β-PGF2α from prostaglandin D2 (PGD2). AKR1C3 also catalyzes the NADPH reduction of progesterone, estrone and androstene-dione. Relevance Since PGH2 is a potent vasoconstrictor, PGF2α is used to treat impotence and abortion. PGD2 is critical in the development of allergic diseases like asthma, hence inhibitors of AKR1C3 – mainly non-steroidal anti-inflammatory compounds (NSAID) like flufenamic acid, mefenamic acid, indomethacin, naproxen, ibuprofen are used as drugs. Structural highlights Human AKR1C3 active site contains NADP and interacts with NSAID drug inhibitor.

spinqualitylabelsall models Structure of human prostaglandin F synthase complex with cofactor NADP and NSAID drug (PDB entry 1s2c) Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image

3D structures of prostaglandin F synthase3D structures of prostaglandin F synthase

Updated on 13-July-2016

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• Prostaglandin F synthase
  • 4f40 – LmAKR1C3 – Leishmania major
    
  • 4fzi – TcAKR1C3 – Trypanosoma cruzi
    
• Prostaglandin F synthase binary complex with NADP
  • 1s1p, 1s1r, 2fgb – hAKR1C3 + NADP - human
    
  • 4dz5 – hAKR1C3 (mutant) + NADP
    
  • 1vbj – AKR1C3 + NADP – Trypanosoma brucei
    
  • 4g5d – LmAKR1C3 + NADP
    
  • 4gie – TcAKR1C3 + NADP
    
• Prostaglandin F synthase ternary complex with NADP
  • 1s2a, 1s2c, 3r43, 3r58, 3r6i, 3r7m, 3r8g, 3r8h, 3r94, 3ufy, 3ug8, 3ugr, 4dbw, 4xve, 4xvd, 4wrh, 4wdx, 4wdw, 4wdt, 4wdu, 4hmn, 4h7c – hAKR1C3 + NADP + NSAID drug
    
  • 1xf0 – hAKR1C3 + NADP + androstene-dione
    
  • 1ry0 – hAKR1C3 + NADP + PGD2
    
  • 1ry8, 1zq5, 4dbs, 4dbu, 4fa3, 4fal, 4fam, 4h7c – hAKR1C3 + NADP + inhibitor
    
  • 2f38 – hAKR1C3 + NADP + glaucoma drug
    
  • 3uwe – hAKR1C3 + NADP + phenoxybenzoic acid