SEN-177(SEN-177) - 药物靶点：QPCT x QPCTL_在研适应症：亨廷顿舞蹈病_专利_临床

概要

基本信息

药物类型

小分子化药

别名-

靶点

QPCT x QPCTL

作用机制

谷氨酰胺酰肽环转移酶抑制剂、QPCTL抑制剂(glutaminyl-peptide cyclotransferase like inhibitors)

治疗领域

神经系统疾病遗传病与畸形其他疾病

在研适应症

亨廷顿舞蹈病

非在研适应症

肿瘤

原研机构

Netherlands Cancer Insitute

在研机构

Siena Biotech SpA

University of Cambridge

Cenix BioScience GmbH

非在研机构

Netherlands Cancer Insitute

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 SEN-177 相关的临床结果

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100 项与 SEN-177 相关的转化医学

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100 项与 SEN-177 相关的专利（医药）

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1

项与 SEN-177 相关的文献（医药）

2018-12-01·JBIC Journal of Biological Inorganic Chemistry3区 · 化学

The structure of the human glutaminyl cyclase–SEN177 complex indicates routes for developing new potent inhibitors as possible agents for the treatment of neurological disorders

3区 · 化学

Article

作者: Benvenuti, Manuela ; Pozzi, Cecilia ; Mangani, Stefano ; Di Pisa, Flavio

Recent evidence links the role of human glutaminyl cyclase (hQC) to the amyloidogenic process involved in Alzheimer's disease (AD). hQC is a zinc enzyme present in neuronal tissue and its activity is responsible for the cyclization of N-terminal Gln or Glu β-amyloid peptides, leading to N-pyroglutamic acid peptides (pE-Aβ) that is probably a crucial event in the initiation and progress of the disease. Indeed, pE-containing peptides exhibit an elevated neurotoxicity and a tendency to aggregate. These observations render hQC inhibition an attractive strategy for developing new molecules active against AD. We present here the crystal structure of hQC in complex with SEN177, a newly designed molecule. The SEN177-binding mode to hQC differs from that of the known hQC inhibitors. SEN177 K_i on hQC is 20 nM, comparable or better than that of the most potent known hQC inhibitors PBD150 and PQ912. In addition, SEN177 already demonstrated relevant pharmacological properties in in vivo models of Huntington's disease. All these properties make SEN177 an important scaffold for developing molecules acting on AD and related diseases.

100 项与 SEN-177 相关的药物交易

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研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
肿瘤	临床1期	荷兰	Netherlands Cancer Insitute	2019-03-31
亨廷顿舞蹈病	临床前	英国	University of Cambridge	2015-04-06
亨廷顿舞蹈病	临床前	德国	Cenix BioScience GmbH	2015-04-06
亨廷顿舞蹈病	临床前	意大利	Siena Biotech SpA	2015-04-06