Bruton’s tyrosine kinase (BTK) is a non-receptor kinase that plays a crucial role in oncogenic signaling that is critical for proliferation and survival of leukemic cells in many B cell malignancies. BTK was initially shown to be defective in the ...

与第一代BTK抑制剂依鲁替尼（ibrutinib）相比，Acalabrutinib具有更好的选择性和靶向特异性，在人全血CD69B细胞激活试验中，其对BTK的IC50和EC50值分别为3、8nmol/L，对ERBB2、ERBB4、JAK3、BLK、FGR、FYN、HCK、LCK、LYN、SRC和YES1等受体的IC50值均在1000nmol·L－1以上。

2024年2月22日 · Bruton酪氨酸激酶（BTK）是一种非受体激酶，在许多B细胞恶性肿瘤中扮演关键的致癌信号传导作用，对白血病细胞的增殖和存活至关重要。 BTK最初在 X连锁遗传无球蛋白血病 （XLA）中被发现缺陷，对B细胞的发育和成熟B细胞的功能均至关重要。 在被发现后不久，BTK被放置在B细胞抗原受体（BCR）下游的信号传导途径中。 最近，针对该激酶的小分子抑制剂已经在动物模型中展现出出色的抗肿瘤活性，并随后在临床研究中得到证实。 特别是口服的不可 …

Bruton’s tyrosine kinase (BTK) was discovered due to its importance in B cell development, and it has a critical role in signal transduction downstream of the B cell receptor (BCR). Targeting of BTK with small molecule inhibitors has proven to be efficacious in several B cell malignancies.

Bruton's tyrosine kinase (BTK) is a TEC kinase with a multifaceted role in B-cell biology and function, highlighted by its position as a critical component of the B-cell receptor signalling pathway. Due to its role as a therapeutic target in several …

The cytoplasmic protein-tyrosine kinase BTK plays an essential role for differentiation and survival of B-lineage cells and, hence, represents a suitable drug target. The number of BTK inhibitors (BTKis) in the clinic has increased considerably and ...

当抗原与 B 细胞表面的 BCR 结合后，一系列的信号分子被激活，其中 BTK 是关键的信号转导分子。 BTK 抑制剂能够阻止 BTK 的磷酸化和活化，从而切断 BCR 信号传导。 这就抑制了 B 细胞的进一步活化、增殖和分化，减少了自身抗体的产生。 例如，在 系统性红斑狼疮 （SLE）等自免疾病中，异常活化的 B 细胞会产生大量的抗核抗体等自身抗体，BTK 抑制剂可以在源头上抑制这种异常的抗体产生。 调节细胞因子产生：B 细胞还可以分泌多种细胞因子，在自身免疫反应的炎症 …

2024年7月9日 · Bruton’s tyrosine kinase (BTK) is a non-receptor tyrosine kinase representing a crucial signaling node in the B cell receptor (BCR) signaling pathway and plays a pivotal role in B-cell development, activation, and proliferation. BTK belongs to the Tec kinase family and serves as a linchpin in BCR signal transduction.

2018年2月19日 · Bruton's tyrosine kinase (BTK) is a non-receptor kinase that plays a crucial role in oncogenic signaling that is critical for proliferation and survival of leukemic cells in many B cell malignancies. BTK was initially shown to be defective in the primary immunodeficiency X-linked agammaglobulinemia …

Bruton's tyrosine kinase (BTK) is an intracellular signaling molecule first identified as the molecule affected in X-linked agammaglobulinemia (XLA) patients, who almost completely lack peripheral B cells and serum immunoglobulins. BTK is crucial for …