Small-Molecule Kinase Downregulators.
Sign Up to like & getrecommendations! Published in 2018 at "Cell chemical biology"
DOI: 10.1016/j.chembiol.2017.10.011
Abstract: New opportunities to advance small-molecule kinase ligands that downregulate their cognate target binding proteins are discussed. Rationally designed heterobifunctional kinase degraders are compared with ATP site ligands that were serendipitously found to cause kinase downregulation.… read more here.
Keywords: molecule kinase; kinase; kinase downregulators; small molecule ... See more keywords
Regulatory spine RS3 residue of protein kinases: a lipophilic bystander or a decisive element in the small-molecule kinase inhibitor binding?
Sign Up to like & getrecommendations! Published in 2022 at "Biochemical Society Transactions"
DOI: 10.1042/bst20210837
Abstract: In recent years, protein kinases have been one of the most pursued drug targets. These determined efforts have resulted in ever increasing numbers of small-molecule kinase inhibitors reaching to the market, offering novel treatment options… read more here.
Keywords: small molecule; molecule kinase; protein kinases; rs3 ... See more keywords
Therapeutic drug monitoring of small molecule kinase inhibitors in oncology in a real‐world cohort study: does age matter?
Sign Up to like & getrecommendations! Published in 2018 at "British Journal of Clinical Pharmacology"
DOI: 10.1111/bcp.13725
Abstract: Pharmacokinetics of small molecule kinase inhibitors (KIs) used in cancer treatment may alter with increasing age, but results are conflicting. This study aims to compare exposure to KIs between older and younger patients (≥70 and read more here.
Keywords: kinase inhibitors; small molecule; oncology; molecule kinase ... See more keywords