Prostaglandin F synthase

Revision as of 13:41, 23 September 2014 by Michal Harel (talk | contribs)

<StructureSection load='1s2c' size='350' side='right' caption='Structure of human prostaglandin F synthase complex with cofactor NADP and NSAID drug (PDB entry 1s2c)' scene=>

Prostaglandin F synthase (AKR1C3) catalyzes the conversion of aldehydes and ketones to alcohol using NADH or NADP as cofactor. I catalyzes the isomerization of prostaglandin H2 (PGH2) to prostaglandin F2α (PGF2α) and the formation of 11β-PGF2α from prostaglandin D2 (PGD2). PGH2 is a potent vasoconstrictor; PGF2α is used to treat impotence and abortion. PGD2 is critical in the development of allergic diseases like asthma. Inhibitors of AKR1C3 – mainly non-steroidal anti-inflammatory compounds (NSAID) like flufenamic acid, mefenamic acid, indomethacin, naproxen, ibuprofen are used as drugs. AKR1C3 also catalyzes the NADPH reduction of progesterone, estrone and androstene-dione.

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

Updated on 23-September-2014

AKR1C3AKR1C3

4f40 – LmAKR1C3 – Leishmania major
4fzi – TcAKR1C3 – Trypanosoma cruzi

AKR1C3 binary complex with NADPAKR1C3 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

AKR1C3 ternary complex with NADPAKR1C3 ternary complex with NADP

1s2a, 1s2c, 3r43, 3r58, 3r6i, 3r7m, 3r8g, 3r8h, 3r94, 3ufy, 3ug8, 3ugr, 4dbw – 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

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Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)

Alexander Berchansky, Michal Harel, Joel L. Sussman