Inhibition of Human Steroid 5β-Reductase (AKR1D1) by Finasteride and Structure of the Enzyme-Inhibitor Complex

July 2009 in “ Journal of Biological Chemistry ”

Jason E. Drury, Ugo Caruso, Trevor M. Penning, David W. Christianson

finasteride steroid 5β-reductase AKR1D1 NADP+ progesterone Propecia

TLDR Finasteride helps treat hair loss and prostate enlargement by blocking a specific enzyme.

The study investigated the inhibition of human steroid 5β-reductase (AKR1D1) by finasteride and the structure of the enzyme-inhibitor complex. Finasteride was found to be a competitive inhibitor of AKR1D1 with low micromolar affinity. The crystal structure of the AKR1D1-NADP+ finasteride complex showed that finasteride binds perpendicular to the NADP+ cofactor and is rotated by ~12° with respect to progesterone. The study provides insight into the mechanism of action of finasteride, which is used to treat hair loss and prostate enlargement.

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Research cited in this study

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research Structural Characterization of Polymorphs and Molecular Complexes of Finasteride

17 citations, January 1999 in “Journal of Molecular Structure”

Finasteride's molecular and crystal structures help develop new drug formulations.

Mechanism-Based Inhibition of Human Steroid 5α-Reductase by Finasteride: Enzyme-Catalyzed Formation of NADP-Dihydrofinasteride, a Potent Bisubstrate Analog Inhibitor

research Mechanism-Based Inhibition of Human Steroid 5α-Reductase by Finasteride: Enzyme-Catalyzed Formation of NADP-Dihydrofinasteride, a Potent Bisubstrate Analog Inhibitor

136 citations, March 1996 in “Journal of the American Chemical Society”

Finasteride effectively blocks enzyme causing male pattern baldness.

research The Clinical Development of a 5α-Reductase Inhibitor, Finasteride

211 citations, November 1990 in “The Journal of Steroid Biochemistry and Molecular Biology”

Finasteride effectively treats BPH, but needs more trials to understand potential.

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community Trying to understand finasteride side effects and post finasteride syndrome

in Finasteride/Dutasteride 74 upvotes 4 years ago

The conversation discusses the side effects of finasteride, including low libido and erectile dysfunction, and the possibility of these effects being permanent, known as post-finasteride syndrome (PFS). Some users report personal experiences with PFS and debate whether the condition is real, with varying opinions on the reversibility of side effects and the role of individual biology.

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The conversation discusses the potential of long-chain unsaturated fatty acids, like oleic and linoleic acid, as an additional treatment for hair loss, which may inhibit the enzyme responsible for converting testosterone to DHT and promote hair growth. Users humorously suggest using oils topically and discuss other hair loss treatments, but the main focus is on the science behind fatty acids and their role in hair health.

community Using Fin and Alfatradiol in conjunction?

in Finasteride/Dutasteride 5 upvotes 2 years ago

User considers adding Alfatradiol to their topical finasteride treatment for hair loss. Others discuss Alfatradiol as a weak estrogen and 5α-reductase inhibitor used for pattern hair loss in men and women.

community Completely defeated after trying so hard with topical finasteride.

in Finasteride/Dutasteride 24 upvotes 1 year ago

A user who has tried multiple treatments for hair loss, including oral and topical finasteride and liposomal finasteride, but experienced severe side effects in each case; the user is considering trying RU58841 or aromatise inhibitors as alternatives.

community A meta analysis of 18 popular hair loss treatments. An 2022 guide on efficacy. From finasteride and minoxidil to caffeine shampoo, saw palmetto and biotin. 96 Scientific References included.

in Research/Science 101 upvotes 2 years ago

Most hair loss treatments are ineffective; only finasteride, dutasteride, and minoxidil show effectiveness.

community The truth about Dutasteride (w/ sources)

in Finasteride/Dutasteride 52 upvotes 1 year ago

The effectiveness of Dutasteride compared to Finasteride in treating hair loss, with evidence given such as studies and experiences, as well as discussion around whether one should switch from Finasteride to Dutasteride. There is also a discussion on post-Dutasteride syndrome.

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research Effect of Finasteride, a 5 Alpha-Reductase Inhibitor, on Serum Gonadotropins in Normal Men

30 citations, August 1992 in “The Journal of Clinical Endocrinology and Metabolism”

Finasteride doesn't affect hormone levels in normal men.