BM-221(BM-221) - 药物靶点：C5AR1_在研适应症：实体瘤_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

C5AR1

作用机制

C5AR1刺激剂(过敏毒素C5a趋化受体刺激剂)

治疗领域

肿瘤

在研适应症

实体瘤

非在研适应症-

原研机构

苏州百迈生物医药有限公司

在研机构

苏州百迈生物医药有限公司

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 BM-221 相关的临床结果

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100 项与 BM-221 相关的转化医学

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100 项与 BM-221 相关的专利（医药）

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1

项与 BM-221 相关的文献（医药）

2021-11-25·Journal of Medicinal Chemistry1区 · 医学

Development of Potent and Selective Agonists for Complement C5a Receptor 1 with In Vivo Activity

1区 · 医学

Article

作者: Gorman, Declan M. ; Rolfe, Barbara E. ; Lee, Han Siean ; Cui, Cedric S. ; Clark, Richard J. ; Lee, John D. ; Fung, Jenny N. ; Li, Xaria X. ; Woodruff, Trent M.

The anaphylatoxin C5a is a complement peptide associated with immune-related disorders. C5a binds with equal potency to two GPCRs, C5aR1 and C5aR2. Multiple C5a peptide agonists have been developed to interrogate the C5a receptor function but none show selectivity for C5aR1. To address these limitations, we developed potent and stable peptide C5aR1 agonists that display no C5aR2 activity and over 1000-fold selectivity for C5aR1 over C3aR. This includes BM213, which induces C5aR1-mediated calcium mobilization and pERK1/2 signaling but not β-arrestin recruitment, and BM221, which exhibits no signaling bias. Both ligands are functionally similar to C5a in human macrophage cytokine release assays and in a murine in vivo neutrophil mobilization assay. BM213 showed antitumor activity in a mouse model of mammary carcinoma. We anticipate that these C5aR1-selective agonists will be useful research tools to investigate C5aR1 function.

100 项与 BM-221 相关的药物交易

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