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Small-Molecule Inhibitors of Bruton’s Tyrosine Kinase

  • Chapter
Cancer II

Part of the book series: Topics in Medicinal Chemistry ((TMC,volume 28))

Abstract

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.

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Abbreviations

BCR:

B-cell receptor

BTK:

Bruton’s tyrosine kinase

CLL:

Chronic lymphocytic leukemia

CR:

Complete response

DAG:

Diacylglycerol

DLBCL:

B-cell-like diffuse large B-cell lymphoma

FDA:

Food and Drug Administration

IP3:

Inositol triphosphate

ITAMs:

Immunoreceptor tyrosine kinase activation motifs

LPS:

Bacterial lipopolysaccharide

MCL:

Mantle cell lymphoma

MM:

Multiple myeloma

ORR:

Overall response rate

OS:

Overall survival

PFS:

Progressive-free survival rate

PH:

Pleckstrin homology

PID:

Primary immunologic deficiency

SH:

Src homology

Syk:

Spleen tyrosine kinase

TH:

TEC homology

TLR:

Toll-like receptor

WM:

Waldenström’s macroglobulinemia

XID:

X-linked immunodeficiency

XLA:

X-linked agammaglobulinemia

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Authors and Affiliations

  1. School of Chemical Biology and Biotechnology, Shenzhen Graduate School, Peking University, Shenzhen, China

    Yingying Zuo & Zhengying Pan

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  1. Yingying Zuo
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  2. Zhengying Pan
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Correspondence to Zhengying Pan .

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  1. Northern Institute for Cancer Research, Chemistry, Newcastle University, Newcastle upon Tyne, UK

    Michael J. Waring

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Zuo, Y., Pan, Z. (2017). Small-Molecule Inhibitors of Bruton’s Tyrosine Kinase. In: Waring, M.J. (eds) Cancer II. Topics in Medicinal Chemistry, vol 28. Springer, Cham. https://doi.org/10.1007/7355_2017_6

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