GA-32(GA-32) - 药物靶点：AR x GR_在研适应症：去势抵抗性前列腺癌_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

AR x GR

作用机制

AR拮抗剂(雄激素受体拮抗剂)、GR拮抗剂(糖皮质激素受体拮抗剂)

治疗领域

肿瘤泌尿生殖系统疾病

在研适应症

去势抵抗性前列腺癌

非在研适应症-

原研机构

浙江师范大学

在研机构

浙江师范大学

非在研机构-

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)临床前

特殊审评-

关联

100 项与 GA-32 相关的临床结果

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100 项与 GA-32 相关的转化医学

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100 项与 GA-32 相关的专利（医药）

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2

项与 GA-32 相关的文献（医药）

2024-03-14·Journal of Medicinal Chemistry1区 · 医学

Design and Synthesis of Dual-Target Inhibitors Targeting Androgen Receptors and Glucocorticoid Receptors to Overcome Antiandrogen Resistance in Castration-Resistant Prostate Cancer

1区 · 医学

Article

作者: Yan, Qiuxia ; Yang, Fulian ; Yuan, Dazhong ; Wang, Jianlong ; Zhou, Jinming ; Li, Chenfan ; Ji, Yang ; Han, Xiaoli ; Zhang, Rongyu ; Wu, Meng

Androgen receptor (AR) antagonists play important roles in the treatment of castration-resistant prostate cancer (CRPC). The glucocorticoid receptor (GR) upregulation leads to drug resistance for clinically used antiandrogens. Therefore, blocking AR/GR signaling simultaneously has become an efficient strategy to overcome the drug resistance of CRPC. Our previous work indicated that Z19 could inhibit the activity of both AR and GR. Herein, we optimized the structure of Z19 and identified GA32 as a potent AR/GR dual inhibitor. GA32 efficiently reduced the mRNA and protein levels of AR/GR downstream genes. GA32 efficiently inhibited the proliferation of enzalutamide resistance CRPC both in vitro and in vivo. GA32 could directly bind to AR and GR, and the predicted binding modes for GA32 with AR/GR suggested that GA32 binds to the AR or GR hormone binding pocket. This work provides a potential lead compound with dual AR/GR inhibitory activity to conquer the drug resistance of CRPC.

1971-05-21·Science1区 · 综合性期刊

GA ₃₂ : A Polar Gibberellin with High Biological Potency

1区 · 综合性期刊

Article

作者: Coombe, B. G.

A new gibberellin, GA 32 , purified from Prunus seed, has three interesting properties: (i) it is the most polar of the 34 gibberellins presently known, (ii) it is the most potent of all gibberellins tested in the barley endosperm bioassay, and (iii) it is very active in promoting the growth of unpollinated apricot ovaries with a normal ratio of length to diameter.

100 项与 GA-32 相关的药物交易

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