[HTML][HTML] Progress with covalent small-molecule kinase inhibitors
Highlights•Summarized the diverse types of warheads across the human
kinome.•Highlighted facile covalent reactive functional groups which bind protein
kinases.•Distribution of covalent-involved amino acids beyond cysteine.•Design
perspectives and future strategies.•Discussed the challenges and opportunities for
designing covalent kinase inhibitors.With reduced risk of toxicity and high selectivity,
covalent small-molecule kinase inhibitors (CSKIs) have emerged rapidly. Through the lens …
kinome.•Highlighted facile covalent reactive functional groups which bind protein
kinases.•Distribution of covalent-involved amino acids beyond cysteine.•Design
perspectives and future strategies.•Discussed the challenges and opportunities for
designing covalent kinase inhibitors.With reduced risk of toxicity and high selectivity,
covalent small-molecule kinase inhibitors (CSKIs) have emerged rapidly. Through the lens …
Highlights
- Summarized the diverse types of warheads across the human kinome.
- Highlighted facile covalent reactive functional groups which bind protein kinases.
- Distribution of covalent-involved amino acids beyond cysteine.
- Design perspectives and future strategies.
- Discussed the challenges and opportunities for designing covalent kinase inhibitors.
With reduced risk of toxicity and high selectivity, covalent small-molecule kinase inhibitors (CSKIs) have emerged rapidly. Through the lens of structural system pharmacology, here we review this rapid progress by considering design strategies and the challenges and opportunities offered by current CSKIs.
Elsevier
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