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Fig. 3 | Molecular Cancer

Fig. 3

From: Chronic myeloid leukemia: the paradigm of targeting oncogenic tyrosine kinase signaling and counteracting resistance for successful cancer therapy

Fig. 3

Stategies for BCR-ABL1 inhibition. Displayed are the SH2 domain (green) and the SH1 (kinase) domain (blue). The inhibitor is in yellow. a ATP-competitive inhibitors like imatinib, nilotinib, dasatinib etc. bind in the cleft between the N-lobe and the C-lobe, at the bottom of which lies the ATP-binding site. b One mode of allosteric inhibition is to use small molecules mimicking myristate binding to the hydrophobic pocket located in the C-lobe. This is the mode of action of asciminib. c Another mode of allosteric inhibition is to use proteins (‘monobodies’) directed against the SH2-kinase interface

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Molecular Cancer

ISSN: 1476-4598