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

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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