December 2016 in “University of Birmingham Institutional Research Archive (University of Birmingham)” This study found that manipulating 5αR2 activity in human hepatocytes in vitro can regulate lipogenesis, with potential clinical implications for patients taking 5αR inhibitors.
11 citations
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January 2000 in “The Journal of Steroid Biochemistry and Molecular Biology” This study found that LY320236 is a competitive inhibitor of type I and a non-competitive inhibitor of type II steroid 5alpha-reductase, indicating its potential as a dual inhibitor with differing modes of activity.
2 citations
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March 2010 in “Acta Biochimica Polonica” This study observed that conjugates of the anticancer drug raltitrexed with dextran and albumin were more cytotoxic than the free drug at high concentrations, altering cell cycle effects.
This study synthesized new heterocyclic steroid derivatives and reported their promising antiproliferative activity against breast and prostate cancer cell lines, highlighting selectivity and impact on signaling pathways even in cells resistant to certain treatments.
6 citations
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March 1996 in “Journal of Investigative Dermatology” 5 citations
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August 2021 in “Journal of biological chemistry/The Journal of biological chemistry” This study observed sexually dimorphic effects of reduced Rdh10 on energy metabolism and muscle function in mice, with males experiencing decreased endurance and females showing increased endurance on a high-fat diet.
December 2010 in “TSpace” In this study, selective overexpression of androgen receptors in muscle cells increased lean muscle mass and reduced fat mass in transgenic rodents, suggesting a potential target for drug development.
December 2023 in “Biointerface Research in Applied Chemistry” This study used molecular docking to identify stiripentol as a potential new inhibitor of the SRD5A2 enzyme, which is targeted for treating androgen-related diseases; however, in vivo trials are needed to validate its efficacy.
2 citations
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October 2023 in “Philosophical Transactions of the Royal Society B Biological Sciences” This study identified novel isoforms of the PADI2 and PADI3 proteins, showing that PADI2β inhibits oligodendrocyte differentiation, possibly by opposing the effect of canonical PADI2, while PADI3β modulates the activity of PADI3α, suggesting new regulatory mechanisms of citrullination in tissue development.
15 citations
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January 2014 in “Medicinal chemistry” This study conducted molecular docking and ADME property analysis on 144 newly designed isatin analogs, suggesting they exhibit lead-like properties for targeting EGFR enzymes.
18 citations
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December 2005 in “Journal of Medicinal Chemistry” In this study, novel substituted benzoyl benzoic acids and phenylacetic acids were potent and selective inhibitors of human steroid 5alpha-reductase type 2, with one compound showing promising bioavailability in rats for potential clinical evaluation.
January 2002 in “映像情報メディア学会技術報告” This study found that 60% of examined prostate tumors had new somatic substitutions in the SRD5A2 gene, affecting enzyme activity and potentially influencing prostate cancer progression.
December 2005 in “Science s STKE” This study reports that localized Rho GTPase activity and ROS production play a critical role in polarized growth and movement in both migrating endothelial cells and developing plant root hairs.
January 2016 in “Munich Personal RePEc Archive (Ludwig Maximilian University of Munich)” This study demonstrated that a light-activated RNAi approach using hollow gold nanoshells effectively targets human prostate cancer cells with reduced off-target toxicity and material use compared to standard methods.
305 citations
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March 2008 in “AJP Endocrinology and Metabolism” This article reviews the regulation and roles of spermidine/spermine-N(1)-acetyltransferase (SSAT) in polyamine metabolism and its potential as a target in cancer and other diseases, without reporting new experimental results.
38 citations
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October 2005 in “Expert opinion on therapeutic patents” This review discusses nonsteroidal selective androgen receptor modulators and their potential therapeutic applications but reports no new clinical findings.
3 citations
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February 2021 in “Molecules” In this study, researchers developed a sensitive assay to measure the inhibition of steroid 5-α reductase (5AR) by chemicals like finasteride and dutasteride, revealing species-specific differences in inhibitor efficacy between human and fish cell lines.
30 citations
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October 2020 in “Nature Communications” This study provides the first crystal structure of the human SRD5A2 enzyme, revealing key insights into its function and inhibition which may aid future drug development.
153 citations
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November 2004 in “Current Medicinal Chemistry” This article updates a prior work on pharmacophore modeling and highlights the advances in 3D database searching technologies for drug design, without presenting new research findings.
56 citations
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July 2014 in “PloS one” This study found that selective androgen receptor modulators (SARMs) significantly inhibited tumor growth and metastasis-promoting factors in AR-positive triple-negative breast cancer models.
58 citations
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June 2000 in “The Journal of Steroid Biochemistry and Molecular Biology” This study found that Atlantic croaker nuclear androgen receptors AR1 and AR2 have different binding affinities for androgens, suggesting that they may mediate distinct physiological actions in teleosts.
October 2016 in “Letters in Drug Design & Discovery” 30 citations
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June 2010 in “Endocrine Related Cancer” In this study, dutasteride more effectively reduced prostate cancer cell viability than finasteride in vitro, but did not significantly alter the angiogenic response.
In this study, researchers developed a computational method called iEdgePathDDA that prioritizes anticancer drug candidates by analyzing changes in gene interactions, demonstrating superior performance compared to existing methods across colorectal, breast, and lung cancer datasets.
15 citations
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April 2008 in “Steroids” This study found that pregnane derivatives with higher lipophilicity, like compound 9d, had stronger androgen receptor binding and greater antiandrogenic effects in rats, correlating relative binding affinity with log P values.
88 citations
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January 2004 in “Journal of Neuroscience” This study found that inhibiting neurosteroidogenesis affected GABA A receptor-mediated synaptic inhibition in immature rats but not in adults, suggesting age-dependent modulation of synaptic strength in the spinal dorsal horn.
13 citations
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June 2024 in “Asian Pacific Journal of Cancer Prevention” The researchers reported that the ethyl ester group in YH239-EE may enhance its ability to induce cell death, making the (+) enantiomer a potentially promising therapy for breast cancer reflected in MCF7 cell studies.
5 citations
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July 2014 in “Acta Crystallographica Section D-biological Crystallography” This study reports that mutations in human L-PGDS affect the entrance and exit of ligands in its binding cavity, suggesting these residues play a role in ligand interaction processes.
16 citations
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October 1994 in “The Journal of Steroid Biochemistry and Molecular Biology” Two non-steroidal antiandrogens, RU 58841 and RU 56187, form a common metabolite at different rates, which may influence their effects; RU 56187 could be used for prostate cancer treatment and RU 58841 for acne treatment.
54 citations
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May 2015 in “Endocrinology” In this study, manipulation of the enzyme 5α-reductase type 2 in human hepatocytes altered lipogenesis, suggesting clinical implications for patients using 5α-reductase inhibitors by affecting glucocorticoid action on hepatic lipid metabolism.