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
Comment
. 2011 Nov 23;18(11):1352-3.
doi: 10.1016/j.chembiol.2011.11.001.

BCR-ABL1 kinase: hunting an elusive target with new weapons

Tomasz Skorski  1
Affiliations
Comment

BCR-ABL1 kinase: hunting an elusive target with new weapons

Tomasz Skorski. Chem Biol. .

Abstract

Tyrosine kinase inhibitors such as imatinib, dasatinib, and nilotinib interfere with ATP-binding pocket to inhibit BCR-ABL1 kinase. A recent report in Cell by Grebien et al. paves the way for a new approach to target BCR-ABL1 kinase by interfering with its SH2-kinase domain interface.

PubMed Disclaimer

Figures

Figure 1
Figure 1. Targeting the SH2-kinase domain interface in BCR-ABL1
Cartoon diagram of the SH2-kinase domain interface underlining the critical role of Ile164 (I164). The 7c12 monobody interferes with the I164 to inhibit BCR-ABL1 kinase activity.
See this image and copyright information in PMC

Comment on

References

    1. Daley GQ, Van Etten RA, Baltimore D. Science. 1990;247:824–830. - PubMed
    1. Druker BJ, Tamura S, Buchdunger E, Ohno S, Segal GM, Fanning S, Zimmermann J, Lydon NB. Nat Med. 1996;2:561–566. - PubMed
    1. Eide CA, Adrian LT, Tyner JW, Mac Partlin M, Anderson DJ, Wise SC, Smith BD, Petillo PA, Flynn DL, Deininger MW, et al. Cancer Res. 2011;71:3189–3195. - PMC - PubMed
    1. Grebien F, Hantschel O, Wojcik J, Kaupe I, Kovacic B, Wyrzucki AM, Gish GD, Cerny-Reiterer S, Koide A, Beug H, et al. Cell. 2011;147:306–319. - PMC - PubMed
    1. Koptyra M, Falinski R, Nowicki MO, Stoklosa T, Majsterek I, Nieborowska-Skorska M, Blasiak J, Skorski T. Blood. 2006;108:319–327. - PMC - PubMed