1116 Novel androgen receptor degrader for androgenetic alopecia (AGA) application
نویسندگان
چکیده
Androgenetic alopecia (AGA) is the most common form of hair loss disorder in men and women all races worldwide. Loss scalp a distressing condition that dampens patient’s self-esteem lowers quality life, but options for effective safe treatment are still limited. In patients with AGA, level dihydrotestosterone (DHT) androgen receptor (AR) protein increased, excessive DHT-AR signaling plays an essential role development progression AGA. this study, we design synthesize series novel degraders can specifically degrade AR AGA treatment. The activity degrader (AR-degrader) was evaluated LNCaP cells demonstrated low nanomolar range DC50. Then DHT-induced regrowth inhibition mouse model which simulates established to evaluate efficacy AR-degrader vivo. After daily administration topically, delay reversed as compared vehicle control. addition, detected amount AR-PROTAC serum close lower limit quantification, suggesting only very limited topically administered enters circulation. This could greatly reduce potential adverse side effects observed finasteride, oral antiandrogen drug Collectively, provides novel, efficient, strategy great therapeutic treating
منابع مشابه
Increased androgen receptor messenger RNA in frontal-parietal hair follicles of women with androgenetic alopecia.
Normal testosterone levels are frequently observed in women with androgenetic alopecia (AGA), suggesting the involvement of androgen sensitivity in this condition. Androgen sensitivity is related to androgen receptor (AR) messenger RNA (mRNA) production in hair follicles and is negatively related to the number of CAG repeats present in exon 1 of the AR gene. The aim of this study was to compare...
متن کاملTitle: Association of Premature Androgenetic Alopecia and Metabolic Syndrome in a Young Indian Population ABSTRACT Context: Although evidences for association of androgenetic alopecia (AGA) with metabolic syndrome
Materials and Methods: The Norwood–Hamilton classification was used to assess the grade of AGA. MetS was defined according to the National Cholesterol Education Program Adult TreatmentPanel III criteria. Blood pressure, blood glucose, lipid parameters, and body mass index along with anthropometric measurements were assessed in all study participants. Statistical Analysis Used: Chi ‐square test ...
متن کاملAndrogen Receptor Copy Number Variation and Androgenetic Alopecia: A Case-Control Study
BACKGROUND The functional polymorphism that explains the established association of the androgen receptor (AR) with androgenetic alopecia (AGA) remains unidentified, but Copy Number Variation (CNV) might be relevant. CNV involves changes in copy number of large segments of DNA, leading to the altered dosage of gene regulators or genes themselves. Two recent reports indicate regions of CNV in an...
متن کاملInflammation in androgenetic alopecia
Years of research have led to the conclusion that androgenetic alopecia may be a result of an alteration in the hair growth cycle and/or a premature aging of the pilosebaceous unit. The etiology of androgenetic alopecia has been defined as multifactorial or even polygenic in nature. The fact that the success rate of treatment with either antihypertensive agents or modulators of androgen metabol...
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ژورنال
عنوان ژورنال: Journal of Investigative Dermatology
سال: 2023
ISSN: ['1523-1747', '0022-202X']
DOI: https://doi.org/10.1016/j.jid.2023.03.1128