The DOI matches its Crossref record; 47 of the 47 references it cites were found in a registry or an index.
Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1
Open accessAbstract
Chronic myelogenous leukemia (CML) arises from the constitutive activity of the BCR-ABL1 oncoprotein. Tyrosine kinase inhibitors (TKIs) that target the ATP-binding site have transformed CML into a chronic manageable disease. However, some patients develop drug resistance due to ATP-site mutations impeding drug binding. We describe the discovery of asciminib (ABL001), the first allosteric BCR-ABL1 inhibitor to reach the clinic. Asciminib binds to the myristate pocket of BCR-ABL1 and maintains activity against TKI-resistant ATP-site mutations. Although resistance can emerge due to myristate-site mutations, these are sensitive to ATP-competitive inhibitors so that combinations of asciminib with ATP-competitive TKIs suppress the emergence of resistance. Fragment-based screening using NMR and X-ray yielded ligands for the myristate pocket. An NMR-based conformational assay guided the transformation of these inactive ligands into ABL1 inhibitors. Further structure-based optimization for potency, physicochemical, pharmacokinetic, and drug-like properties, culminated in asciminib, which is currently undergoing clinical studies in CML patients.
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Metadata
- Authors
- Schoepfer, J., Jahnke, W., Berellini, G., Buonamici, S., Cotesta, S., Cowan-Jacob, S. W., Dodd, S., Drueckes, P., Fabbro, D., Gabriel, T., Groell, J.-M., Grotzfeld, R. M., Hassan, A. Q., Henry, C., Iyer, V., Jones, D., Lombardo, F., Loo, A., Manley, P. W., Pellé, X., Rummel, G., Salem, B., Warmuth, M., Wylie, A. A., Zoller, T., Marzinzik, A. L., & Furet, P.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2018-08-23
- Volume
- 61
- Issue
- 18
- Pages
- 8120-8135
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2888514087
- Cited by
- 454
- References
- 47
- FWCI
- 17.63
- Type
- journal article
- Language
- en
- Open access
- green
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- Schoepfer, J., Jahnke, W., Berellini, G., Buonamici, S., Cotesta, S., Cowan-Jacob, S. W., Dodd, S., Drueckes, P., Fabbro, D., Gabriel, T., Groell, J.-M., Grotzfeld, R. M., Hassan, A. Q., Henry, C., Iyer, V., Jones, D., Lombardo, F., Loo, A., Manley, P. W., . . . Furet, P. (2018). Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1. Journal of Medicinal Chemistry. https://doi.org/10.1021/acs.jmedchem.8b01040
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Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
