一种通过肽支架的组合修饰产生的高效且选择性的蛋白激酶Cα（PKCalpha）抑制剂。
A highly potent and selective PKCalpha inhibitor generated via combinatorial modification of a peptide scaffold.
作者信息
Lee Jung Hwan, Nandy Sandip K, Lawrence David S
机构信息
The Albert Einstein College of Medicine, Department of Biochemistry, 1300 Morris Park Ave., Bronx, New York 10461, USA.
出版信息
J Am Chem Soc. 2004 Mar 24;126(11):3394-5. doi: 10.1021/ja037300b.
A potent and highly selective inhibitor of protein kinase C alpha has been generated via the combinatorial modification of a consensus sequence peptide. The inhibitor displays a Ki of 800 pM versus variable peptide substrate and good selectivity versus other members of the PKC family, including PKCbeta (385-fold), PKCgamma (580-fold), PKCdelta (2730-fold), PKCepsilon (600-fold), PKCeta (1310-fold), PKCtheta (1210-fold), PKCiota (940-fold), and PKCzeta (640-fold). The parallel synthesis strategy employed is easily automated and straightforward to implement.
通过对共有序列肽进行组合修饰，生成了一种强效且高度选择性的蛋白激酶Cα抑制剂。该抑制剂对可变肽底物的抑制常数（Ki）为800皮摩尔，对蛋白激酶C（PKC）家族的其他成员具有良好的选择性，包括PKCβ（385倍）、PKCγ（580倍）、PKCδ（2730倍）、PKCε（600倍）、PKCη（1310倍）、PKCθ（1210倍）、PKCι（940倍）和PKCζ（640倍）。所采用的平行合成策略易于自动化且实施简单。
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