title: Increasing the kinase specificity of k252a by protein surface recognition.
abstract: [reaction: see text] Here we describe a miniature protein (1) that presents the cAMP-dependent protein kinase (PKA) recognition epitope found within the heat-stable Protein Kinase Inhibitor protein (PKI) and a miniature protein conjugate (1-K252a) in which 1 is joined covalently to the high-affinity but nonselective kinase inhibitor K252a. Miniature protein 1 recognizes PKA with an affinity that rivals that of PKI and, in the context of 1-K252a, leads to a dramatic increase in kinase specificity.
authors.affiliation: Department of Chemistry and Department of Molecular, Cellular, and Developmental Biology, Yale University, New Haven, Connecticut 06520-8107, USA.
authors.forename: Tanya L
authors.initials: TL
authors.lastname: Schneider
authors.forename: Rebecca S
authors.initials: RS
authors.lastname: Mathew
authors.forename: Kevin P
authors.initials: KP
authors.lastname: Rice
authors.forename: Kazuhiko
authors.initials: K
authors.lastname: Tamaki
authors.forename: John L
authors.initials: JL
authors.lastname: Wood
authors.forename: Alanna
authors.initials: A
authors.lastname: Schepartz
mesh_terms: D002227:Carbazoles / Q000737:chemistry / Q000494:pharmacology*; D017868:Cyclic AMP-Dependent Protein Kinases / Q000037:antagonists & inhibitors / Q000378:metabolism*; D026121:Indole Alkaloids; D047908:Intracellular Signaling Peptides and Proteins; D015394:Molecular Structure; D013379:Substrate Specificity
chemical_list: D002227:Carbazoles; D026121:Indole Alkaloids; D047908:Intracellular Signaling Peptides and Proteins; C015482:protein kinase modulator; C049985:staurosporine aglycone; D017868:Cyclic AMP-Dependent Protein Kinases