AI Article Synopsis
- Aberrant B-cell activation is linked to various cancers and blood disorders, making them a target for treatment.
- BTK and PI3Kδ are important kinases involved in B-cell signaling, and their inhibitors have shown promise in treating specific lymphomas.
- The study introduces new compounds that effectively inhibit both BTK and PI3Kδ, potentially enhancing treatment responses and addressing resistance in B-cell diseases.
Article Abstract
The aberrant activation of B-cells has been implicated in several types of cancers and hematological disorders. BTK and PI3Kδ are kinases responsible for B-cell signal transduction, and inhibitors of these enzymes have demonstrated clinical benefit in certain types of lymphoma. Simultaneous inhibition of these pathways could result in more robust responses or overcome resistance as observed in single agent use. We report a series of novel compounds that have low nanomolar potency against both BTK and PI3Kδ as well as acceptable PK properties that could be useful in the development of treatments against B-cell related diseases.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5150666 | PMC |
| http://dx.doi.org/10.1021/acsmedchemlett.6b00356 | DOI Listing |
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