Progesterone 5 3-reductase

Egerer-Sieber et al. (2006) reported on the purification and crystallization of recombinant 5p-POR from D. lanata. Later on, Gavidia et al. (2007) predicted that the 5p-POR belongs to the SDR family (Oppermann et al, 1997). Finally, Thorn et al. (2008) fully characterized the crystal structure and found that the progesterone reductase from D. lanata defines a novel class of short-chain dehydrogenases / reductases. 

Anti-androgens and hormones 5a-Reductase inhibitors Progesterone and estrogen Recreational drugs Ethanol Cocaine Marijuana... 

Cyproterone acetate6 Progesterones 5-a-reductase inhibition Finasteride6... 

Fig. 9.8 Examples of rule-of-three compliant molecules that have biological activity better than 10 nM. Under each molecule, the following information is included molecule name, MW, ClogP, the biological activity type, value and target. Target names are as follows D3 and D4 - dopaminergic receptor types 2 and 3 AChE and BChE - acetyl- and butyryl-choline esterases PRa and PRb - progesterone receptor types A and B H] and H3, histamine receptor types 1 and 3 5-HT2a, 5-HT2b, 5-HT2c, 5-HT3, 5-HT4 - serotonin receptor subtypes 2A, 2B, 2C, and types 3 and 4 DAT, NET, 5-HTT - dopamine, norepinephrine and serotonin transporter proteins /X], /x.2, S, ki, ks - opioid receptor types mu-1, mu-2, delta, kappa-1 and kappa-3 5a-Rl and 5o -R2 - 5-alpha-reductase isozymes 1 and 2 Flt-1-fms-like tyrosine kinase receptor.

Figure 9.85 Normal phase HPLC profiles of the reaction product of the cholesterol side chain cleavage system. Peaks were identified on the basis of their retention times. (i4) Without cholesterol oxidase treatment. Cholesterol (100 nmol) was incubated with cytochrome P450scc (70 pmol) in the presence of adrenodoxin, adrenodoxin reductase, and an NADPH-generating system. Monitoring was at 214 nm. Peaks 1, cholesterol 2, pregnenolone 3, deoxycorticosterone acetate (internal standard) (B) The reaction mixture of (A) was further incubated with cholesterol oxidase at 37°C for 10 minutes. Monitoring was at 240 nm. Peaks 1, cholestenone 2, progesterone 3, deoxycorticosterone acetate (internal standard). (From Sugano et al., 1989.)...

Egerer-Sieber, C., Herl, V., Miiller-Uri, R, Kreis, W. and Muller, Y.A. (2006) Crystallization and preliminary crystallographic analysis of selenomethionine-labelled progesterone 5p-reductase from Digitalis lanata Ehrh. Acta Crystallogr. Sect. F Struct. Biol. Cryst. Commun., 62, 186-8. 

Gartner, D., Keilholz, W. and Seitz, H. (1994) Purification, characterization and partial peptide microsequencing of progesterone 5fJ-reductase from shoot cultures of Digitalis purpurea. Eur.. Biochem., 225,1125-32. 

Gartner, D., Wendroth, S. and Seitz, H. (1990) A stereospecific enzyme of the putative biosynthetic pathway of cardenolides characterization of a progesterone 5p-reductase from leaves of Digitalis purpurea. FEBS Lett., 271, 239-42. 

Gavidia, L, Tarrio, R., Rodriguez-Trelles, R, Perez-Bermudez, P. and Seitz, H.U. (2007) Plant progesterone 5p-reductase is not homologous to the animal enzyme. Molecular evolutionary characterization of P5fJR from Digitalis purpurea. Phytochemistry, 68, 853-64. 

Herl, V., Albach, D., Mueller-Uri, R, Braeuchler, C., Heubl, G. and Kreis, W. (2008) Using progesterone 5p-reductase, a gene encoding a key enzyme in the cardenolide biosynthesis, to infer the phylogeny of the genus Digitalis. Plant Syst. Evol., 271, 65-78. 

Herl, V., Fischer, G., Botsch, R., Miiller-Uri, F. and Kreis, W. (2006b) Molecular cloning and expression of progesterone 5fJ-reductase (5p-POR) from Isoplexis canariensis. Planta Med., 72,1163-5. 

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