title: Design and synthesis of AX4697, a bisindolylmaleimide exo-affinity probe that labels protein kinase C alpha and beta.
abstract: The synthesis and biochemical characterization of AX4697, a fluorescent, bisindolylmaleimide-derived probe for PKCalpha and beta, is described. AX4697 was able to quantify changes in PKC expression in drug-treated Jurkat cells and was shown to covalently label PKCalpha on C619, a residue that sits just outside the active site.
authors.affiliation: ActivX Biosciences, 11025 N. Torrey Pines Road, La Jolla, CA 92037, USA.
authors.forename: Yongsheng
authors.initials: Y
authors.lastname: Liu
authors.forename: Jiangyue
authors.initials: J
authors.lastname: Wu
authors.forename: Helge
authors.initials: H
authors.lastname: Weissig
authors.forename: Juan M
authors.initials: JM
authors.lastname: Betancort
authors.forename: Wen Zhi
authors.initials: WZ
authors.lastname: Gai
authors.forename: Phillip S
authors.initials: PS
authors.lastname: Leventhal
authors.forename: Matthew P
authors.initials: MP
authors.lastname: Patricelli
authors.forename: Babak
authors.initials: B
authors.lastname: Samii
authors.forename: Anna K
authors.initials: AK
authors.lastname: Szardenings
authors.forename: Kevin R
authors.initials: KR
authors.lastname: Shreder
authors.forename: John W
authors.initials: JW
authors.lastname: Kozarich
mesh_terms: D020134:Catalytic Domain; D015195:Drug Design; D005456:Fluorescent Dyes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D019169:Jurkat Cells; D008301:Maleimides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D011493:Protein Kinase C / Q000378:metabolism*; D064546:Protein Kinase C beta; D051571:Protein Kinase C-alpha / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: C533387:AX4697; D005456:Fluorescent Dyes; D007211:Indoles; D008301:Maleimides; D011493:Protein Kinase C; D064546:Protein Kinase C beta; D051571:Protein Kinase C-alpha; C088060:bisindolylmaleimide