Cancer II pp 75-104 | Cite as

Small-Molecule Inhibitors of Bruton’s Tyrosine Kinase

  • Yingying Zuo
  • Zhengying PanEmail author
Part of the Topics in Medicinal Chemistry book series (TMC, volume 28)


Bruton’s tyrosine kinase has emerged as a promising drug target for multiple diseases, particularly hematopoietic malignancies. As a result of intensive efforts, many inhibitors have been developed to target BTK. Among them, considerable progress has been made in covalent inhibitors. In this chapter, example compounds will be discussed to highlight our current understanding of the functional and structural features of BTK inhibitors.


B-cell malignancies BTK Inhibitors Signaling pathway Tec family kinase 



B-cell receptor


Bruton’s tyrosine kinase


Chronic lymphocytic leukemia


Complete response




B-cell-like diffuse large B-cell lymphoma


Food and Drug Administration


Inositol triphosphate


Immunoreceptor tyrosine kinase activation motifs


Bacterial lipopolysaccharide


Mantle cell lymphoma


Multiple myeloma


Overall response rate


Overall survival


Progressive-free survival rate


Pleckstrin homology


Primary immunologic deficiency


Src homology


Spleen tyrosine kinase


TEC homology


Toll-like receptor


Waldenström’s macroglobulinemia


X-linked immunodeficiency


X-linked agammaglobulinemia


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© Springer International Publishing AG 2017

Authors and Affiliations

  1. 1.School of Chemical Biology and Biotechnology, Shenzhen Graduate SchoolPeking UniversityShenzhenChina

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