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Pharmacological Role and Clinical Applications of 5α-Reductase Inhibitors: Review Article for Pharmacists and Healthcare Professionals

research Pharmacological Role and Clinical Applications of 5α-Reductase Inhibitors-Review Article for Pharmacists and Healthcare Professionals

July 2025

5α-reductase inhibitors help treat prostate enlargement and hair loss but may cause side effects, requiring careful use.

research The use of 5 alpha-reductase in the era of minimally invasive surgical therapies (MISTs): Is it still valuable?

September 2024 in “Uro-Technology Journal”

research OR2AT4, an Ectopic Olfactory Receptor, Suppresses Oxidative Stress-Induced Senescence in Human Keratinocytes

6 citations , November 2022 in “Antioxidants”

OR2AT4 helps reduce aging and cell damage in human skin cells.

research Design, synthesis and biological evaluation of novel 3-oxo-4-oxa-5α-androst-17β-amide derivatives as dual 5α-reductase inhibitors and androgen receptor antagonists

3 citations , May 2017 in “Bioorganic & medicinal chemistry letters”

New compounds were made that are promising for prostate cancer therapy.

research Disruption of P2RY5, an orphan G protein–coupled receptor, underlies autosomal recessive woolly hair

210 citations , February 2008 in “Nature genetics”

Mutations in the P2RY5 gene cause autosomal recessive woolly hair.

research 5 Following the Pattern: Hair Restoration

August 2023

Hair restoration follows a specific pattern.

research 7 Regulation of androgen receptor and 5α-reductase in the skin of normal and hirsute women

35 citations , May 1986 in “Clinics in endocrinology and metabolism”

The exact cause of increased 5α-reductase activity leading to hirsutism in women is still unknown.

research Expression and function of nuclear receptor co-activator 4: evidence of a potential role independent of co-activator activity

26 citations , May 2012 in “Cellular and Molecular Life Sciences”

NcoA4 may have roles beyond helping control gene activity, possibly affecting cell behavior and stability.

MRNA Levels of Aromatase, 5α-Reductase Isozymes, and Prostate Cancer-Related Genes in Plucked Hair from Young Men with Androgenic Alopecia

research mRNA Levels of Aromatase, 5α-Reductase Isozymes, and Prostate Cancer-Related Genes in Plucked Hair from Young Men with Androgenic Alopecia

December 2023 in “International Journal of Molecular Sciences”

Men with early balding showed higher levels of certain genes linked to hair loss and possibly prostate cancer.

research Deletion of an Enhancer in FGF5 is Associated With Ectopic Expression in Goat Hair Follicles and the Cashmere Growth Phenotype

1 citations , October 2020 in “Research Square (Research Square)”

A genetic variant in goats is linked to cashmere growth.

research Fully automated chip-based nanoelectrospray ionization-mass spectrometry as an effective tool for rapid and high-throughput screening of 5α-reductase inhibitors

7 citations , February 2020 in “Analytical and Bioanalytical Chemistry”

research Expression, characterization, and structural analysis of human liver delta4-3-ketosteroid 5beta-reductase (AKR1D1) and its disease-related mutant P133R

January 2009 in “ScholarlyCommons (University of Pennsylvania)”

The P133R mutation in AKR1D1 enzyme causes harmful bile acid buildup, explaining related health issues.

research Determination Method for Steroid 5α-Reductase Activity Using Liquid Chromatography/Atmospheric Pressure Chemical Ionization–Mass Spectrometry

13 citations , October 2005 in “Analytical Sciences”

A new method was developed to measure and assess the activity and inhibition of the enzyme steroid 5α-reductase.

research Four Independent Mutations in the Feline Fibroblast Growth Factor 5 Gene Determine the Long-Haired Phenotype in Domestic Cats

75 citations , September 2007 in “Journal of Heredity”

FGF5 gene mutations cause long hair in domestic cats.

research Molecular Cloning of 5′ Flanking Region of Ovine Keratin Associated Protein 6-1 Gene and Comparison of the Sequences

January 2007 in “Journal of Inner Mongolia University”

The research helps in creating genetically modified animals to study hair growth.

research Androgen receptor-mediated gene activation in prostate cancer cells

1 citations , September 2010 in “UEF eRepo (University of Eastern Finland)”

Androgen receptors help prostate cancer cells grow and resist drugs.

research Synthesis and 5α-Reductase Inhibitory Activity of C21 Steroids Having 1,4-diene or 4,6-diene 20-ones and 4-Azasteroid 20-Oximes

186 citations , December 2011 in “Molecules”

Three specific 4-azasteroid-2-oximes showed strong enzyme inhibition, but less than finasteride.

research Review of Women with Vision: The Presentation Sisters of South Dakota, 1880-1985

January 1990

Knocking out the FGF5 gene in sheep increased wool production and hair-follicle density.

research Identification of xenobiotics interfering with 5 α -reductase (SRD5A2) activity

February 2026 in “Toxicology Letters”

MK-0773 is a moderate inhibitor of the SRD5A2 enzyme.

research Improved 2α-Hydroxylation Efficiency of Steroids by CYP154C2 Using Structure-Guided Rational Design

12 citations , February 2023 in “Applied and Environmental Microbiology”

Mutants of CYP154C2 enzyme significantly improved steroid conversion efficiency.

research Efficacy to hair growth with the combination of 5-aminolevulinic acid and iron.

January 2005 in “FJ. Fragrance journal”

research Δ5-3β-Hydroxysteroid Dehydrogenase Activity in Sebaceous Glands of Scalp in Male-Pattern Baldness

69 citations , August 1988 in “Journal of Investigative Dermatology”

5-Alpha-Reductase Type 2 Deficiency: Is There a Genotype-Phenotype Correlation? A Review

research 5-α-Reductase type 2 deficiency: is there a genotype-phenotype correlation? A review

39 citations , April 2018 in “Hormones”

No consistent link between genotype and phenotype in 5-α-Reductase type 2 deficiency.

research STAT5 Activation in the Dermal Papilla Is Important for Hair Follicle Growth Phase Induction

32 citations , April 2016 in “Journal of Investigative Dermatology”

STAT5 activation is crucial for starting the hair growth phase.

research Intracrine and Myotrophic Roles of 5α-Reductase and Androgens

35 citations , October 2011 in “Medicine and science in sports and exercise”

Muscles can make their own androgens, which may help muscle growth.

research Generation of comparative pharmacophoric model for steroidal 5α-reductase I and II inhibitors: A 3D-QSAR study on 6-azasteroids

13 citations , January 2015 in “Steroids”

The study created a model to help design new inhibitors for steroidal 5α-reductase enzymes.

4-O-Methylhonokiol Protects HaCaT Cells from TGF-β1-Induced Cell Cycle Arrest by Regulating Canonical and Non-Canonical Pathways of TGF-β Signaling

research 4-O-Methylhonokiol Protects HaCaT Cells from TGF-β1-Induced Cell Cycle Arrest by Regulating Canonical and Non-Canonical Pathways of TGF-β Signaling

5 citations , February 2017 in “Biomolecules & Therapeutics”

4-O-Methylhonokiol helps protect skin cells from growth-stopping effects of a protein by regulating growth-related pathways.

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