Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Case Reports
. 2014 Jun 12;370(24):2352-4.
doi: 10.1056/NEJMc1402716. Epub 2014 May 28.

Ibrutinib resistance in chronic lymphocytic leukemia

Richard R Furman  1 , Shuhua Cheng, Pin Lu, Menu Setty, Alexendar R Perez, Ailin Guo, Joelle Racchumi, Guozhou Xu, Hao Wu, Jiao Ma, Susanne M Steggerda, Morton Coleman, Christina Leslie, Y Lynn Wang
Affiliations
Case Reports

Ibrutinib resistance in chronic lymphocytic leukemia

Richard R Furman et al. N Engl J Med. .

Erratum in

  • N Engl J Med. 2014 Jun 26;370(26):2547. Perez, Alijandro R [corrected to Perez, Alexendar R]
No abstract available

PubMed Disclaimer

Figures

Figure 1
Figure 1. Effect of C481S Mutation of Bruton’s Tyrosine Kinase (BTK) on Ibrutinib Binding and the Ability of Ibrutinib to Inhibit BTK Phosphorylation
Panel A shows structural modeling of nonmutant and mutant BTK with ibrutinib. The red arrows indicate the covalent bond between ibrutinib (purple and blue) and BTK (green and yellow) before and after the mutation. Panel B shows the inhibition of nonmutant BTK or C481S BTK phosphorylation by ibrutinib in HEK 293 cells. The half-maximal inhibitory concentration (IC50) of ibrutinib for inhibition of BTK phosphorylation was analyzed and plotted with GraphPad Prism. GFP denotes green fluorescent protein.
See this image and copyright information in PMC

References

    1. Advani RH, Buggy JJ, Sharman JP, et al. Bruton tyrosine kinase inhibitor ibrutinib (PCI-32765) has significant activity in patients with relapsed/refractory B-cell malignancies. J Clin Oncol. 2013;31:88–94. - PMC - PubMed
    1. Byrd JC, Furman RR, Coutre SE, et al. Targeting BTK with ibrutinib in relapsed chronic lymphocytic leukemia. N Engl J Med. 2013;369:32–42. [Erratum, N Engl J Med 2014;370:786.] - PMC - PubMed
    1. Cheng S, Ma J, Guo A, et al. BTK inhibition targets in vivo CLL proliferation through its effects on B-cell receptor signaling activity. Leukemia. 2014;28:649–57. - PubMed
    1. Herman SE, Gordon AL, Hertlein E, et al. Bruton tyrosine kinase represents a promising therapeutic target for treatment of chronic lymphocytic leukemia and is effectively targeted by PCI-32765. Blood. 2011;117:6287–96. - PMC - PubMed
    1. Honigberg LA, Smith AM, Sirisawad M, et al. The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy. Proc Natl Acad Sci U S A. 2010;107:13075–80. - PMC - PubMed

MeSH terms