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WALTHAM, Mass.--(BUSINESS WIRE)--Avilar Therapeutics, a biopharmaceutical company focused on extracellular protein degradation, today announced it will present preclinical proof-of-concept data for the company’s MTAC (M6PR Targeting Chimera) protein degrader platform at IMMUNOLOGY™ 2024, the American Association of Immunologists annual meeting taking place May 3-7 in Chicago, Illinois..
马萨诸塞州沃尔瑟姆市(商业新闻短讯)--专注于细胞外蛋白质降解的生物制药公司Avilar Therapeutics今天宣布,将于5月3日至7日在伊利诺伊州芝加哥举行的美国免疫学家协会年会IMMUNOLOGY™2024上,为该公司的MTAC(靶向M6PR的嵌合体)蛋白质降解平台提供临床前概念验证数据。。
MTACs are novel bifunctional molecules containing a proprietary Avilar ligand to the mannose 6‑phosphate receptor (M6PR) conjugated to a second ligand that binds to a protein of interest for degradation. MTACs represent an expansion of Avilar’s capabilities for extracellular protein degradation, building on the company’s ATAC (ASGPR Targeting Chimera) platform, which utilizes the asialoglycoprotein receptor (ASGPR) for degradation of proteins in the hepatocyte endolysosome.
MTAC是一种新型的双功能分子,含有与甘露糖6-磷酸受体(M6PR)结合的专有Avilar配体,该配体与第二配体结合,该配体与目标蛋白质结合以降解。MTAC代表了Avilar细胞外蛋白质降解能力的扩展,建立在该公司的ATAC(ASGPR靶向嵌合体)平台上,该平台利用去唾液酸糖蛋白受体(ASGPR)降解肝细胞内溶酶体中的蛋白质。
As a complementary approach, MTACs harness the M6P receptor and work by degrading pathogenic proteins in the endolysosome of M6PR-expressing cells, which include hepatocytes but also encompass multiple additional cell types..
作为一种补充方法,MTAC利用M6P受体并通过降解表达M6PR的细胞(包括肝细胞,但也包括多种其他细胞类型)的内溶酶体中的致病蛋白来发挥作用。。
Avilar scientists invented novel high affinity ligands to both ASGPR and M6PR, and these ligands form the chemistry backbone for ATACs and MTACs, respectively. In both cases, Avilar’s chemistry enables the design of highly efficient degraders with more streamlined monovalent designs, lower molecular weight, and improved physicochemical properties versus previous approaches.
Avilar科学家发明了针对ASGPR和M6PR的新型高亲和力配体,这些配体分别形成ATAC和MTAC的化学骨架。在这两种情况下,与以前的方法相比,Avilar的化学方法能够设计出高效的降解剂,具有更简化的单价设计,更低的分子量和改进的理化性质。
While Avilar leverages ATACs for degrading circulating proteins and hepatocyte membrane proteins, MTACs offer a new and complementary technology for degrading non-hepatocyte membrane proteins involved in the pathogenesis of human diseases..
虽然Avilar利用ATAC降解循环蛋白和肝细胞膜蛋白,但MTAC为降解参与人类疾病发病机制的非肝细胞膜蛋白提供了一种新的补充技术。。
“We are building multiple technologies for protein degradation and have successfully demonstrated in vivo proof-of-concept for ATACs as potent degraders of extracellular proteins,” said Effie Tozzo, PhD, Chief Scientific Officer of Avilar. “While our primary focus continues to be on ATACs as we advance a pipeline of first-in-class degrader medicines, MTACs represent an additional strategy with expanded target reach for extracellular protein degradation.”.
Avilar首席科学官Effie Tozzo博士说:“我们正在建立多种蛋白质降解技术,并成功证明了ATAC作为细胞外蛋白质有效降解剂的体内概念验证。”。“虽然随着我们推进一流降解药物的管道,我们的主要重点仍然是ATAC,但MTAC代表了一种额外的策略,扩大了细胞外蛋白质降解的目标范围。”。
Highlights from the MTAC data to be presented at the conference include:
将在会议上介绍的MTAC数据要点包括:
Development of novel M6PR ligands with enhanced affinity for M6PR through structure-based computational design methods
通过基于结构的计算设计方法开发对M6PR具有增强亲和力的新型M6PR配体
Demonstration that monovalent MTACs containing these high affinity M6PR ligands achieve robust ternary complex formation and efficient uptake and degradation
证明含有这些高亲和力M6PR配体的单价MTAC可实现强大的三元复合物形成以及有效的吸收和降解
Benchmarking the performance of monovalent MTACs versus tridentate and monodentate bifunctional molecules containing ligands with weaker affinity for M6PR
基准测试单价MTAC与含有对M6PR亲和力较弱的配体的三齿和单齿双功能分子的性能
Details of the poster presentation are as follows:
海报展示详情如下:
Title: In Vitro and In Vivo Proof-of-Concept Studies of Extracellular Protein Degradation Using Novel M6PR-Targeting Chimeras (MTACs)
标题:使用新型M6PR靶向嵌合体(MTAC)进行细胞外蛋白降解的体外和体内概念验证研究
Session Date and Time: Saturday, May 4, 2024, 3:15 p.m. – 4:30 p.m. CT
会议日期和时间:2024年5月4日星期六下午3:15–4:30
Poster #: 848
海报#:848
Presenter: Lisa Molz, PhD, Vice President, Research
主持人:Lisa Molz博士,研究副总裁
The poster will be available on the publications page of the Avilar website following the presentation.
演示后,海报将在Avilar网站的出版物页面上提供。
About Avilar Therapeutics
关于Avilar Therapeutics
Avilar Therapeutics is a biopharmaceutical company pioneering the discovery and development of extracellular protein degraders, a new frontier in targeted protein degradation. Avilar develops ATACs (ASGPR Targeting Chimeras), a new class of protein degraders that shuttle disease-causing proteins from circulation to the endolysosome where the unwanted proteins are degraded.
Avilar Therapeutics是一家生物制药公司,率先发现和开发细胞外蛋白质降解剂,这是靶向蛋白质降解的新前沿。Avilar开发了ATACs(靶向ASGPR的嵌合体),这是一类新的蛋白质降解剂,可将致病蛋白质从循环中穿梭到不需要的蛋白质降解的内溶酶体。
Avilar has built a proprietary discovery platform that includes novel, high-affinity, small molecule ASGPR ligands and advanced modeling of the biophysics, pharmacokinetics, and pharmacodynamics of ATAC mediated endocytosis and degradation. This platform enables the modular design and synthesis of ATACs extendable across the extracellular proteome to a wide range of proteins involved in the pathogenesis of human diseases.
Avilar建立了一个专有的发现平台,其中包括新颖的高亲和力小分子ASGPR配体,以及ATAC介导的内吞和降解的生物物理学,药代动力学和药效学的高级建模。该平台使ATAC的模块化设计和合成能够在细胞外蛋白质组中扩展到与人类疾病发病机理有关的多种蛋白质。
Avilar is leveraging its ATAC platform to create a broad and diverse pipeline of first-in-class extracellular protein degraders. Avilar is based in Waltham, MA. For more information, please visit www.avilar-tx.com and follow us on LinkedIn..
Avilar正在利用其ATAC平台创建广泛多样的一流细胞外蛋白降解剂管道。Avilar位于马萨诸塞州沃尔瑟姆。有关更多信息,请访问www.Avilar-tx.com并在LinkedIn上关注我们。。