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research Regulation of Receptor Binding Specificity of FGF9 by an Autoinhibitory Homodimerization

24 citations , July 2017 in “Structure”

In this study, researchers found that ligand homodimerization controls the receptor binding specificity of the FGF9 subfamily, preventing off-target activation of FGFR "b" isoforms.

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 Relative binding affinity of novel steroids to androgen receptors in hamster prostate

5 citations , January 2005 in “Journal of Enzyme Inhibition and Medicinal Chemistry”

This study found that certain steroidal compounds, especially 10a–10c, demonstrated strong antiandrogenic activity by binding to the androgen receptor and reducing prostate weight in a hamster model.

Crystallization and Preliminary X-Ray Analysis of the Human Androgen Receptor Ligand-Binding Domain with a Coactivator-Like Peptide and Selective Androgen Receptor Modulators

research Crystallization and preliminary X-ray analysis of the human androgen receptor ligand-binding domain with a coactivator-like peptide and selective androgen receptor modulators

1 citations , November 2008 in “Acta crystallographica”

This study reports the crystallization of the human androgen receptor's ligand-binding domain with nonsteroidal ligands, which may aid in understanding the differences in binding compared to steroidal ligands.

research Discovery of an Androgen Receptor Degrader Featuring a Pyridazinyl Glutarimide CRBN-Binding Motif for Transdermal Treatment of Androgenetic Alopecia

May 2026 in “Journal of Medicinal Chemistry”

In this study, the authors developed a novel PROTAC named dAR-6–1, which demonstrated superior hair regeneration in an AGA mouse model compared to minoxidil, highlighting its promise as a therapy due to potent AR degradation and excellent skin permeability.

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community Bicalutamide effect on androgens?

5 upvotes 5 years ago

Bicalutamide blocks androgen receptors, preventing testosterone and DHT from binding, which can help with hair loss but may cause feminization. It is not recommended for those who do not want feminization effects.

community Why was fluridil abandoned and never made past phase 2?

5 upvotes 4 years ago

Fluridil was abandoned due to its weak effectiveness and low binding affinity to the androgen receptor, making it less competitive against DHT and testosterone. Users discuss its limited results compared to other treatments like pyrilutamide and RU58841.

community How is the GT20029 different to pyrilutamide as an androgenic antagonist

1 year ago

GT20029 and pyrilutamide are both androgen antagonists but work differently; GT20029 degrades the androgen receptor, while pyrilutamide blocks DHT from binding. GT20029 is expected to have similar efficacy to CosmeRNA.

community Having androgen receptor density and sensitivity at wrong f*ing place

in Satire 7 upvotes 1 year ago

The conversation discusses hair loss treatments, focusing on the use of topical minoxidil, microneedling, finasteride, and dutasteride, while debating the role of testosterone and DHT in hair loss. It also touches on the potential liver health impacts of these treatments and the genetic sensitivity of hair follicles to androgens.

community Is there a topical androgen receptor blocker so we don't have to fuck with the enzyme and destroy our allopregnanolone, but go and hit the end target straight?

in Treatment 44 upvotes 2 years ago

The conversation discusses topical androgen receptor blockers for hair loss, mentioning Clascoterone, Pyrilutamide, GT20029, and RU58841. Ketoconazole's effectiveness and application methods are also debated.

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