减脂增肌靶点 —— ActRII - 知乎 - 知乎专栏
2023年11月6日 · 与 ActRII 结合后，配体和ActRII 与ActRI形成复合物，刺激细胞质中 Smad2 和 Smad3 转录因子的磷酸化。 磷酸化的Smad2/3随后转运至细胞核，并调节包括MyoD在内的靶基因的转录。
Characterization of the Extracellular Ligand-Binding Domain of …
To study the structural basis that underlies the transmembrane signaling mechanism, we have overexpressed the soluble extracellular domain of the type II activin receptor from mouse (ActRII-ECD). We used the methylotrophic yeast Pichia pastoris as an expression host to produce a large quantity of ActRII-ECD.
The BMP7/ActRII Extracellular Domain Complex Provides New
2002年10月30日 · Activins and bone morphogenetic proteins (BMPs) elicit diverse biological responses by signaling through two pairs of structurally related type I and type II receptors. Here we report the crystal structure of BMP7 in complex with the extracellular domain (ECD) of the activin type II receptor.
The interaction of BMP-7 and ActRII implicates a new mode of …
Both types of receptor consist of a small extracellular domain that is linked to the membrane-spanning segment by a short peptide and a cytoplasmic part that contains a Ser/Thr-kinase domain. Signalling by BMP-7 is mediated through a sequential binding mechanism; in the first step, BMP-7 is bound to its high-affinity type II receptor.
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.
Activin type II receptor (ActRII) is crucial for the assembly of the ligand/receptor complex and the activation of downstream cascades in activin signaling pathway. In this study, we identified six variants of grass carp ActRIIA which can be generated through three alternative splicing events (defined as AS1, AS2 and AS3).
Activin and Inhibin Binding to the Soluble Extracellular Domain of ...
1999年4月1日 · The extracellular domain of type II mouse activin receptor (ActRII ECD) was expressed in the baculovirus system, purified in three steps by lectin affinity, anion exchange, and reverse phase chromatography, and further characterized by mass spectrometry.
ActRII - A Novel Drug Target that Preserves ... - DIMA Biotechnology
2024年4月10日 · Both types of Activin receptors have approximately 500 amino acid residues, are single-pass transmembrane serine/threonine kinases, and consist of an extracellular domain rich in Cys residues (approximately 110 amino acid residues) with ligand-binding activity, a transmembrane domain (approximately 26 amino acid residues), and an intracellular ...
Novel factors in regulation of activin signaling - ScienceDirect
2004年10月15日 · ARIP2 interacts with both ActRIIs and RalBP1 (Ral binding protein 1) through different domains to dramatically change the localization of ActRIIs. Overexpression of ARIP2 enhances endocytosis of ActRIIs. These data indicate that ARIP2 is a novel factor regulating cell surface ActRII expression and activin function.
ACTRIIA-Fc rebalances activin/GDF versus BMP signaling in
2020年5月13日 · ACTRIIA-Fc, a potent GDF8/11 and activin ligand trap, was used to test the roles of these ligands in animal and cellular models of PH. By blocking GDF8/11- and activin-mediated SMAD2/3 activation in vascular cells, ACTRIIA-Fc attenuated proliferation of pulmonary arterial smooth muscle cells and pulmonary microvascular endothelial cells.