
减脂增肌靶点 —— ActRII - 知乎 - 知乎专栏
在皮下脂肪和内脏脂肪中,肥胖/肥胖小鼠的myostatin和 ActRIIB mRNA 水平比野生型小鼠高 50 到 100 倍。 在Bimagrumab包涵体肌炎的临床研究中,接受治疗的患者只表现出肌肉质量的增加,但并未有功能性改善。
ActRII-减脂增肌减肥药新兴靶点 - 专注肿瘤免疫
2024年4月11日 · Luspatercept(罗特西普)是由BMS开发的一款ActRIIB-Fc融合蛋白,由人免疫球蛋白G1(IgG1)的Fc结构域与活化素受体IIB(ActRIIB)的细胞外结构域融合而成。2014年7月和8月,Luspatercept分别获得治疗β-地中海贫血中间型和重度和骨髓增生异常综合征(MDS)的孤 …
ACVR2B - Wikipedia
Activin receptor type-2B is a protein that in humans is encoded by the ACVR2B gene. [5][6][7] ACVR2B is an activin type 2 receptor. Activins are dimeric growth and differentiation factors which belong to the transforming growth factor-beta (TGF-beta) superfamily of structurally related signaling proteins.
下一代高质量减肥“种子选手”:ActRII靶点 - 健康界
2024年6月20日 · 激活素Ⅱ型受体(Activin type Ⅱ Receptor,即ActRⅡ)是转化生长因子β(TGF-β)受体家族的成员,是 包括活化素 A (Activin A)和 活化素B (Activin B)及BMP7、BMP9、BMP10、GDF1、GDF8 (myostatin)、 GDF11和Nodal在内的其他TGF-β家族成员的II型受体。 ActRⅡ存在于脂肪和肌肉细胞中。 在脂肪细胞中,激活素通过ActRⅡ进行脂质存储,这是肥胖的重要驱动因素,阻断该信号通路,则可促进脂肪代谢;在肌肉细胞中,ActRⅡ受体传导的 …
Blocking ActRIIB and restoring appetite reverses cachexia and …
2022年8月8日 · We identify Activin A as a purported driver of cachexia and treat with ActRIIB-Fc, a decoy ligand for TGF-β/activin family members, together with anamorelin (Ana), a ghrelin receptor agonist, to...
Principles of the activin receptor signaling pathway and its …
2021年8月1日 · Activin type IIB decoy receptor (ActRIIB-Fc) is based on a fusion of the ligand binding domain of ActRIIB and the Fc of an immunoglobulin. Native ActRIIB has a high affinity to activins, myostatin, and selected GDFs and BMPs, including GDF11, BMP9, and …
Characterization of the Ligand Binding Functionality of the ...
The single transmembrane domain serine/threonine kinase activin receptor type IIB (ActRIIB) has been proposed to bind key regulators of skeletal muscle mass development, including the ligands GDF-8 (myostatin) and GDF-11 (BMP-11).
Molecular characteristic of activin receptor IIB and its functions in ...
2020年9月1日 · Activin receptor IIB (ActRIIB) is a serine/threonine-kinase receptor binding with transforming growth factor-β (TGF-β) superfamily ligands to participate in the regulation of muscle mass in vertebrates. However, its structure and function in crustaceans remain unknown.
Structures of an ActRIIB:activin A complex reveal a novel binding …
2003年4月1日 · We have solved the crystal structure of activin A bound to the extracellular domain of a type II receptor, ActRIIB, revealing the details of this interaction. ActRIIB binds to the outer edges of the activin finger regions, with the two receptors juxtaposed in close proximity, in a mode that differs from TGF‐β3 binding to type II receptors.
ActRIIB:ALK4-Fc alleviates muscle dysfunction and ... - PubMed
2021年2月15日 · Here, we introduce as a potential therapeutic agent a heterodimeric ligand-trapping fusion protein, ActRIIB:ALK4-Fc, which comprises extracellular domains of activin-like kinase 4 (ALK4) and activin receptor type IIB (ActRIIB), a naturally occurring pair of type I and II receptors belonging to the TGF-β superfamily.