title: Direct and two-step bioorthogonal probes for Bruton's tyrosine kinase based on ibrutinib: a comparative study.
abstract: Ibrutinib is a covalent and irreversible inhibitor of Bruton's tyrosine kinase (BTK) and has been approved for the treatment of haematological malignancies, such as chronic lymphocytic leukaemia, mantle cell lymphoma and Waldenström's macroglobulinemia. The covalent and irreversible nature of its molecular mode of action allows identification and monitoring of its target in an activity-based protein profiling (ABPP) setting. Fluorescent and biotinylated ibrutinib derivatives have appeared in the literature in recent years to monitor BTK in vitro and in situ. The work described here complements this existing methodology and pertains a comparative study on the efficacy of direct and two-step bioorthogonal ABPP of BTK.
authors: Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, 2300 RA Leiden, The Netherlands. h.s.overkleeft@chem.leidenuniv.nl m.van.der.stelt@chem.leidenuniv.nl.
authors: Nora
authors: N
authors: Liu
authors: Sascha
authors: S
authors: Hoogendoorn
authors: Bas
authors: B
authors: van de Kar
authors: Allard
authors: A
authors: Kaptein
authors: Tjeerd
authors: T
authors: Barf
authors: Christoph
authors: C
authors: Driessen
authors: Dmitri V
authors: DV
authors: Filippov
authors: Gijsbert A
authors: GA
authors: van der Marel
authors: Mario
authors: M
authors: van der Stelt
authors: Herman S
authors: HS
authors: Overkleeft
mesh_terms: D000225:Adenine / Q000031:analogs & derivatives; D000077329:Agammaglobulinaemia Tyrosine Kinase; D019337:Hematologic Neoplasms / Q000188:drug therapy; D006801:Humans; D015335:Molecular Probes; D009426:Netherlands; D010880:Piperidines; D047428:Protein Kinase Inhibitors / Q000627:therapeutic use; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors / Q000378:metabolism*; D011720:Pyrazoles / Q000494:pharmacology*; D011743:Pyrimidines / Q000494:pharmacology*
chemical_list: D015335:Molecular Probes; D010880:Piperidines; D047428:Protein Kinase Inhibitors; D011720:Pyrazoles; D011743:Pyrimidines; C551803:ibrutinib; D011505:Protein-Tyrosine Kinases; D000077329:Agammaglobulinaemia Tyrosine Kinase; C000625949:BTK protein, human; D000225:Adenine