Introduction
BTK inhibition blocks B cell signaling and proliferation1
Acalabrutinib: a next-generation BTK inhibitor that delivers focused kinase inhibition and limited off-target activity2,3
Visualization of Kinase Selectivity2,3
| Number of Kinases Bound | |||
| Compounda | >65% Bound | >90% Bound | >99% Bound |
| Acalabrutinib | 7 | 4 | 1b |
| Ibrutinib | 37 | 25 | 13 |
| Zanubrutinib | 19 | 13 | 4 |
Abbreviations
AGC = protein kinase A, G, and C families
;AKT = protein kinase B
;BCL-10 = B-cell lymphoma/leukemia 10
;BCR = B-cell receptor
;BLNK = B-cell linker protein
;BTK = Bruton tyrosine kinase
;CAMK = calmodulin/calcium-regulated kinases
;CARD11 = caspase recruitment domain-containing protein 11
;CBM = CARD11–BCL‑10–MALT1
;CD = cluster of differentiation
;CK1 = casein kinase 1
;CIN85 = Cbl-interacting protein of 85 kDa
;CMGC = CDK, MAPK, GSK3, and CLK
;DAG = diacylglycerol
;IgH = immunoglobulin heavy chain
;IgL = immunoglobulin light chain
;IKK = inhibitor of NF-κB kinase
;MALT1 = mucosa-associated lymphoid tissue lymphoma translocation protein 1
;MAPK = mitogen-activated protein kinase
;mTOR = mammalian target of rapamycin
;NF-kB = nuclear factor kappa-light chain enhancer of activated B cells
;NFAT = nuclear factor of activated T cells
;PI3K = Phosphatidylinositol 3-kinase
;PIP = phosphatidylinositol
;PKC = protein kinase C
;PLC = phospholipase C
;SFK = SRC-family kinase
;SYK = spleen tyrosine kinase
;STE = homologs of the yeast STE7, STE11, and STE20 genes
;TK = tyrosine kinases
;TKL = tyrosine kinase-like
References
Document ID: 03435135-2ea5-4261-b52b-476f8c4a6afb
Last updated: 17-April-2023