Syk抑制剂是什么？ 这是一个什么样的新药呢？ 有研究发现， 脾酪氨酸激酶 (Syk)在B细胞受体信号转导、B细胞活化和自身抗体产生中起着关键作用，活化的Syk通过B细胞受体介导B淋巴细胞的激活并分化为能分泌抗体的浆细胞等。

2018年5月30日 · The FDA approved Rigel Pharmaceuticals' first-in-class SYK inhibitor fostamatinib for the treatment of adult patients with chronic immune thrombocytopenia (ITP) who have had an insufficient...

2025年1月1日 · This review covers the structure and regulatory pathways of SYK, as well as its links to various diseases. It also highlights key small-molecule SYK inhibitors, their design strategies and their potential therapeutic benefits, aiming to enhance our understanding and aid in the discovery of more-effective SYK inhibitors.

Gusacitinib (ASN-002) 是一种口服有效的 SYK/JAK 激酶双重抑制剂，其抑制 SYK、JAK1、JAK2、JAK3 和 TYK2 的 IC 50 值分别为 5, 46, 4, 11 和 8 nM。Gusacitinib 能快速且显著抑制与特应性皮炎发病机制有关的关键炎症通路。

2017年7月28日 · Syk inhibitors are a new group of small molecule inhibitors targeting BCR-mediated signaling pathways. The second generation compound, entospletinib, showed promising results in clinical trials against B-cell malignancies, mainly CLL.

Recently, researchers revealed that SYK enhances the activation of HSCs via facilitating the generation of reactive oxygen species (ROS) and autophagy in liver, and the combinational application of Silybin (ROS inhibitor) and GS-9973 (SYK inhibitor) hold promising therapeutic action against mouse liver fibrosis and liver cirrhosis . However ...

2023年12月15日 · Spleen tyrosine kinase (SYK) is a non-receptor tyrosine kinase. The dysregulation of SYK is closely related to the occurrence and development of allergic diseases, autoimmune diseases and cancer. SYK has become an attractive target for drug discovery due to its important biological functions.

2022年10月13日 · In this study, we developed a new inhibitor for Syk targeting lipid binding of its SH2 domain. It was not only more specific and potent against AML cells than currently available...

2025年2月17日 · These results suggested that Syk inhibitor (fostamatinib) improved the severity of lupus caused by FcγRIIb defect partly through Syk-p38MAPK anti-inflammation that inhibited both ET formation...

2024年11月5日 · TQB3473 is a novel, potent and highly selective oral Syk inhibitor designed to target immune-mediated B cell receptor (BCR) pathways and Fcγ receptors downstream signals. Here we report the initial phase 1 results of TQB3473 in patients with relapsed/refractory ITP enrolled in TQB3473-I-02.