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Synthesis, Biological Evaluation, and Molecular Docking of 4-Amino-2H-benzo[h]chromen-2-one Analogs Containing the Piperazine Moiety

research Synthesis, biological evaluation and molecular docking of 4-Amino-2H-benzo[h]chromen-2-one (ABO) analogs containing the piperazine moiety

7 citations , August 2019 in “Bioorganic & medicinal chemistry”

This study identified novel 4-Amino-2H-benzo[h]chromen-2-one analogs as potent androgen receptor antagonists that show strong antiproliferative activity against prostate cancer cells, suggesting them as potential lead compounds for therapy development.

A Novel Point Mutation in the Ligand-Binding Domain of the Human Glucocorticoid Receptor Causing Generalized Glucocorticoid Resistance: The Importance of the C Terminus in Conferring Transactivational Activity

research A Novel Point Mutation in the Ligand-Binding Domain (LBD) of the Human Glucocorticoid Receptor (hGR) Causing Generalized Glucocorticoid Resistance: The Importance of the C Terminus of hGR LBD in Conferring Transactivational Activity

91 citations , May 2005 in “The Journal of Clinical Endocrinology & Metabolism”

In this study, a novel mutation in the glucocorticoid receptor gene was identified in a young woman, impairing glucocorticoid signaling and leading to generalized glucocorticoid resistance.

research In Vitroandin VivoStructure-Activity Relationships of Novel Androgen Receptor Ligands with Multiple Substituents in the B-Ring

20 citations , September 2005 in “Endocrinology”

This study identified novel selective androgen receptor modulators with enhanced in vivo pharmacological activity through structure-activity relationship analysis in castrated rats.

research Androgen Receptor Ligands: Agonists and Antagonists

2 citations , November 2017 in “Elsevier eBooks”

This article discusses the role of the androgen receptor in regulating development and homeostasis, and reviews treatment approaches for conditions related to hormone imbalances, without reporting new clinical findings.

research Structural perspectives on the androgen receptor, the elusive shape-shifter

August 2024 in “Steroids”

This review summarizes structural insights into androgen receptor dynamics, highlighting its flexibility in binding numerous partners, which may explain adaptive resistance mutations in cancer and loss of function in androgen insensitivity syndrome.

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community Bile Acid-Mediated DHT Dysregulation Hypothesis

in Research/Science 13 upvotes 1 year ago

Elevated bile acids can inhibit the enzyme AKR1C2, leading to increased DHT levels, which may accelerate hair loss in those predisposed to androgenetic alopecia. Treatments mentioned include topical minoxidil and finasteride.

community Why Fin/Dut Isn't Working for You GPR133: a new hairloss mechanism + Steroid Hair Loss Deep Dive

6 upvotes 1 month ago

Hair loss may be linked to the GPR133 receptor, independent of the androgen receptor pathway. Treatments like finasteride, dutasteride, minoxidil, RU58841, and KX-826 show varying results, with hair loss persisting due to high testosterone and GPR133's role.

community KX-826: Long-Term Safety Results are out!

159 upvotes 1 year ago

KX-826 initially improves hair growth but declines after 24 weeks, with mild itching as a side effect. Combining it with minoxidil and finasteride may improve results, but long-term effectiveness is uncertain.

community Study: There is 70x Higher Unconjugated DHT in Feces Compared To Blood Levels in Young Adults - Gut Microbiota Manages DHT Recycling and Metabolism

in Research/Science 194 upvotes 1 year ago

Gut microbiota significantly influences androgen metabolism, impacting hair loss treatments like finasteride. Probiotics, dietary changes, and fecal microbiota transplants may help manage DHT levels and improve hair health.

community The Real Cause Of Androgenetic Alopecia

675 upvotes 1 year ago

Androgenetic alopecia is caused by DHT affecting hair growth. Finasteride and minoxidil are used to manage hair loss by blocking DHT and promoting hair growth.

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Hair Transplant Surgeon
Dr. Shashikiran AR, MD, MBBS, FRGHS
Mysuru, Karnataka, India

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Dr. Shashikiran AR, MD, MBBS, FRGHS