Schneider Tanya L, Mathew Rebecca S, Rice Kevin P, Tamaki Kazuhiko, Wood John L, Schepartz Alanna
Department of Chemistry and Department of Molecular, Cellular, and Developmental Biology, Yale University, New Haven, Connecticut 06520-8107, USA.
Org Lett. 2005 Apr 28;7(9):1695-8. doi: 10.1021/ol050179o.
[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.
[反应：见正文] 在此，我们描述了一种微型蛋白质（1），它呈现出在热稳定蛋白激酶抑制剂蛋白（PKI）中发现的环磷酸腺苷（cAMP）依赖性蛋白激酶（PKA）识别表位，以及一种微型蛋白质偶联物（1-K252a），其中1与高亲和力但非选择性的激酶抑制剂K252a共价连接。微型蛋白质1识别PKA的亲和力可与PKI相媲美，并且在1-K252a的情况下，会导致激酶特异性显著提高。
