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NOVEL NON-PEPTIDE ANTAGONIST OF THE GNRH RECEPTOR

NOVEL NON-PEPTIDE ANTAGONIST OF THE GNRH RECEPTOR
GNRH 受体的新型非肽拮抗剂
批准号:
6073967
负责人:
RICHARD SCOTT STRUTHERS
金额:
$9.99万
依托单位国家:
美国
项目类别:
财政年份:
2000
资助国家:
美国
项目状态:
已结题
起止时间:
2000-04-05 至 2000-10-04

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中文摘要
翻译
描述:(改编自申请人的摘要)。申请人建议 开发一种非肽类口服活性GnRH拮抗剂, 治疗疾病如前列腺癌、乳腺癌、子宫内膜异位症和 子宫肌瘤申请人将采用高通量平行合成 基于三个选择的小的确定的组合化学库, 在筛选内部化学文库中发现的分子框架 合理的设计。合成分子的效力将是 通过使用表达该蛋白的细胞系的膜结合测定来确定。 克隆的人GnRH受体。申请人还将开发一组突变体 GnRH受体和来自几个物种的受体,以确定受体 通过小分子文库的特征分析来确定接触位点。这将 允许申请人汇集来自多个配体家族的信息, 基于对共同受体相互作用的了解。具体目标,在 I期,旨在产生有效的GnRH拮抗剂与 将其开发为II期有效临床候选药物所需的数据。 拟议商业应用:不可用
英文摘要
DESCRIPTION: (adapted from the applicant's abstract). The applicant proposes to develop a non-peptide, orally active GnRH antagonist that may useful in the treatment of diseases such as prostate cancer, breast cancer, endometriosis and uterine fibroids. The applicant will employ high-throughput parallel synthesis of defined combinatorial chemical libraries based upon three selected small molecule frameworks discovered in the screening of in-house chemical libraries and rational design. The potency of the synthesized molecules will be determined by membrane-binding assays using a cell line that expresses the cloned human GnRH receptor. The applicant will also develop a panel of mutant GnRH receptors and receptors from several species to determine the receptor contact sites through profiling of the small molecule libraries. This will allow the applicant to pool information from multiple ligand families based upon knowledge of common receptor interactions. The specific aims, proposed in Phase I, are designed to generate potent GnRH antagonists together with the data necessary to develop them into valid clinical candidates in Phase II. PROPOSED COMMERCIAL APPLICATION: NOT AVAILABLE
期刊论文(13)
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会议论文
Species selectivity of nonpeptide antagonists of the gonadotropin-releasing hormone receptor is determined by residues in extracellular loops II and III and the amino terminus.
促性腺激素释放激素受体的非肽拮抗剂的物种选择性由细胞外环II和III以及氨基末端中的残基决定。
DOI: 10.1074/jbc.m404474200
发表时间: 2004
期刊: The Journal of biological chemistry
影响因子: --
作者: [Reinhart,GregJ, Xie,Qiu, Liu,Xin-Jun, Zhu,Yun-Fei, Fan,Jun, Chen,Chen, Struthers,RScott]
通讯作者: Struthers,RScott
DOI: 10.1016/s0960-894x(03)00619-x
发表时间: 2003-10
期刊: Bioorganic & medicinal chemistry letters
影响因子: 2.7
作者: [F. Tucci;Yun-fei Zhu;Zhiqian Guo;T. Gross;Patrick J. Connors;R. Struthers;Greg J. Reinhart;J. Saunders-J.]
通讯作者: F. Tucci;Yun-fei Zhu;Zhiqian Guo;T. Gross;Patrick J. Connors;R. Struthers;Greg J. Reinhart;J. Saunders-J.
DOI: 10.1016/s0960-894x(02)00745-x
发表时间: 2002-12
期刊: Bioorganic & medicinal chemistry letters
影响因子: 2.7
作者: [F. Tucci;Yun-fei Zhu;Zhiqian Guo;T. Gross;Patrick J. Connors;R. Struthers;Greg J. Reinhart;Xiaochuan Wang;J. Saunders;Chen Chen-Chen]
通讯作者: F. Tucci;Yun-fei Zhu;Zhiqian Guo;T. Gross;Patrick J. Connors;R. Struthers;Greg J. Reinhart;Xiaochuan Wang;J. Saunders;Chen Chen-Chen
Synthesis and structure-activity relationships of (R)-1-alkyl-3-[2-(2-amino)phenethyl]-5-(2-fluorophenyl)-6-methyluracils as human GnRH receptor antagonists.
作为人 GnRH 受体拮抗剂的 (R)-1-烷基-3-[2-(2-氨基)苯乙基]-5-(2-氟苯基)-6-甲基尿嘧啶的合成和构效关系。
DOI: 10.1016/j.bmcl.2004.02.004
发表时间: 2004
期刊: Bioorganic & medicinal chemistry letters.
影响因子: --
作者: [Rowbottom,MartinW, Tucci,FabioC, Zhu,Yun-Fei, Guo,Zhiqiang, Gross,TimothyD, Reinhart,GregJ, Xie,Qui, Struthers,RScott, Saunders,John, Chen,Chen]
通讯作者: Chen,Chen
9
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