Pargellis C A, Campbell S J, Pav S, Graham E T, Pitner T P
Department of Biochemistry, Boehringer Ingelheim Pharmaceuticals Inc., Ridgefield, CT 06877, USA.
J Enzyme Inhib. 1997 Jan;11(3):151-69. doi: 10.3109/14756369709027647.
Peptide boronic acid dipeptide compounds were analyzed for their ability to inhibit recombinant human dipeptidylpeptidase IV (CD26, DPPIV). Rate constants for the peptide boronates are difficult to obtain because the active boronic acid dipeptide exists in equilibrium with a cyclic inactive species in aqueous solution. Rate constants were determined for the inhibition of DPPIV using several peptide boronates at different pH values. Val-boroPro forms the most tightly bound complex with DPPIV; the first order half life for dissociation of the inactive enzyme-inhibitor complex at 23 degrees C is approximately 27 days.
对肽硼酸二肽化合物抑制重组人二肽基肽酶IV（CD26，DPPIV）的能力进行了分析。肽硼酸盐的速率常数难以获得，因为活性硼酸二肽在水溶液中与环状非活性物种处于平衡状态。使用几种肽硼酸盐在不同pH值下测定了抑制DPPIV的速率常数。缬氨酸-硼代脯氨酸与DPPIV形成结合最紧密的复合物；在23℃下，非活性酶-抑制剂复合物解离的一级半衰期约为27天。
