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ANTIANDROGEN OLIGONUCLEOTIDES USABLE FOR THE TREATMENT OF DERMATOLOGICAL ANDROGEN-RELATED DISORDERS RELATING TO ANDROGEN METABOLISM, THEIR PHARMACEUTICAL COMPOSITIONS, THEIR USES AND TREATMENT METHOD
ANTIANDROGEN OLIGONUCLEOTIDES USABLE FOR THE TREATMENT OF DERMATOLOGICAL ANDROGEN-RELATED DISORDERS RELATING TO ANDROGEN METABOLISM, THEIR PHARMACEUTICAL COMPOSITIONS, THEIR USES AND TREATMENT METHOD
Antiandrogen oligonucleotides suitable for the treatment of hair loss and androgen-metabolism related skin disorders. The oligonucleotides having the sequences:;
INN-18.1(SEQ ID No 1):5′ CATTGGTGAAGGATCGCC 3′INN-24(SEQ ID No 2):5′ CAATCATTTCTGCTGGCG 3′INN-71(SEQ ID No 3):5′ GGCCTTCTTCGGCTGTGAAG 3′INN-72(SEQ ID No 4):5′ CACACGGTCCATACAACTGG 3′INN-18.2(SEQ ID No 5):5′ GGCGAAGTAGAGCATCCT 3INN-24.1(SEQ ID No 6):5′ TGG CGC ACA GGT ACT TCT 3′INN-73(SEQ ID No 7):5′ CCA CCA CCA CCA CAC GG 3′INN-76(SEQ ID No 8):5′ GCC GCC ACC ACC CCC ACC 3′
;These anti-androgenic active principles are specific to reach their molecular target, which is circumscribed to the site of application. The oligonucleotides described inhibit the androgen receptor (AR) expression at very low concentrations in skin and hair follicle primary cell cultures, through a mechanism implying the reaching of, and the hibridizing with, specific regions of the AR mRNA, thereby triggering the RNAse H digestion of the AR mRNA and thus inhibiting the AR translation.
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机译：适用于治疗脱发和雄激素代谢相关的皮肤疾病的抗雄激素寡核苷酸。具有以下序列的寡核苷酸：
<标题/> <行> INN-18.1 <行> （SEQ ID N o 1）： 5'CATTGGTGAAGGATCGCC 3' <行> <行> INN-24 <行> （SEQ ID N o 2）： 5'CAATCATTTCTGCTGGCG 3' <行> <行> INN-71 <行> （SEQ ID N o 3）： 5'GGCCTTCTTCGGCTGTGAAG 3' <行> <行> INN-72 <行> （SEQ ID N o 4）： 5'CACACGGTCCATACAACTGG 3' <行> <行> INN-18.2 <行> （SEQ ID N o 5）： 5'GGCGAAGTAGAGCATCCT 3 <行> <行> INN-24.1 <行> （SEQ ID N o 6）： 5'TGG CGC ACA GGT ACT TCT 3' <行> <行> INN-73 <行> （SEQ ID N o 7）： 5'CCA CCA CCA CCA CAC GG 3' <行> <行> INN-76 <行> （SEQ ID N o 8）： 5'GCC GCC ACC ACC CCC ACC 3' ;这些抗雄激素活性成分特定于达到其分子靶标，该靶标已限制在应用部位。所描述的寡核苷酸通过一种暗示AR mRNA特定区域到达并与之杂交的机制，以极低的浓度抑制皮肤和毛囊原代细胞培养物中的雄激素受体（AR）表达，从而触发RNA酶H消化。 AR mRNA的表达，因此抑制AR翻译。
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