Gulledgea B M, Aggena J B, Huangb H-B, Nairnc A C, Chamberlin A R
Department of Chemistry, University of California, Irvine, Irvine, CA 92697, USA.
Curr Med Chem. 2002 Nov;9(22):1991-2003. doi: 10.2174/0929867023368845.
The serine/threonine phosphatases are inhibited by a variety of natural toxins, including the microcystins and nodularins. Progress in understanding the details of the biosynthetic origin and the binding of these compounds is discussed, as is the progress made in synthesizing the members of these families. Additionally, the work by several groups to either synthesize simplified analogues that are still potent, or introduce selectivity for PP1 over PP2A are discussed. Finally, the properties of a series of five new truncated analogues are examined.
丝氨酸/苏氨酸磷酸酶受到多种天然毒素的抑制,包括微囊藻毒素和节球藻毒素。本文讨论了在理解这些化合物的生物合成起源细节及其结合方面所取得的进展,以及在合成这些家族成员方面所取得的进展。此外,还讨论了几个研究小组的工作,这些工作包括合成仍然有效的简化类似物,或引入对PP1比对PP2A的选择性。最后,研究了一系列五个新的截短类似物的性质。