title: DYRK1A kinase inhibitors with emphasis on cancer.
abstract: Various types of cancers (including gliomas, melanomas, and esophageal, pancreas and non-small-cell lung cancers) display intrinsic resistance to pro-apoptotic stimuli, such as conventional chemotherapy and radiotherapy, and/or the activation of a multidrug resistance phenotype, which are major barriers to effective treatment and lead to poor patient prognosis. The DYRK1A kinase is directly implicated in the resistance of cancer cells to pro-apoptotic stimuli and drives several pathways that enhance proliferation, migration, and the reduction of cell death, leading to very aggressive biological behavior in cancer cell populations. The DYRK1A kinase is also implicated in neurological diseases and in neoangiogenic processes. Thus, the DYRK1A kinase is of great interest for both cancer and neuroscience research. During the last decade, numerous compounds that inhibit DYRK1A have been synthesized. The present review discusses the available molecules known to interfere with DYRK1A activity and the implications of DYRK1A in cancer and other diseases and serves as a rational analysis for researchers who aim to improve the anti-DYRK1A activity of currently available compounds.
authors.affiliation: Laboratoire de Chimie Organique, Faculté des Sciences, Université Libre de Bruxelles (ULB), Brussels, Belgium.
authors.forename: A
authors.initials: A
authors.lastname: Ionescu
authors.forename: F
authors.initials: F
authors.lastname: Dufrasne
authors.forename: M
authors.initials: M
authors.lastname: Gelbcke
authors.forename: I
authors.initials: I
authors.lastname: Jabin
authors.forename: R
authors.initials: R
authors.lastname: Kiss
authors.forename: D
authors.initials: D
authors.lastname: Lamoral-Theys
mesh_terms: D000818:Animals; D006801:Humans; D009369:Neoplasms / Q000201:enzymology*; D047428:Protein Kinase Inhibitors / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism; D013329:Structure-Activity Relationship; D000097603:Dyrk Kinases
chemical_list: D047428:Protein Kinase Inhibitors; D017346:Protein Serine-Threonine Kinases; D011505:Protein-Tyrosine Kinases; D000097603:Dyrk Kinases