Walker L A, Gailly P, Jensen P E, Somlyo A V, Somlyo A P
Department of Molecular Physiology and Biological Physics, University of Virginia, Health Sciences Center, Charlottesville 22906-0011, USA.
FASEB J. 1998 Jul;12(10):813-21. doi: 10.1096/fasebj.12.10.813.
The purpose of our study was to determine the mechanism through which phorbol esters and smooth muscle myosin phosphatase inhibitors can induce contraction of smooth muscle in the absence of Ca2+. Protein kinase C-epsilon (PKC-epsilon) was previously implicated in this process based largely on its supposed absence in the ferret portal vein, and a correlation was drawn between the presence of this isoform and the ability of smooth muscle to contract independently of Ca2+ and phosphorylation of the 20 kDa regulatory light chains of myosin (MLC20). We demonstrate here, with two antibodies, one to the NH2 terminus and the other to the COOH terminus of PKC-epsilon, that epsilon is present in both ferret portal vein and rabbit portal vein smooth muscle, neither of which exhibits phorbol ester-induced contraction in the absence of Ca2+. However, in the presence of clamped submaximal Ca2+, phorbol es ter increased MLC20 phosphorylation from 17.7+/-1.7% to 46.4+/-3.6% in ferret portal vein smooth muscle and evoked an increase in force. Prolonged (48 h) incubation of ferret portal vein with phorbol esters completely down-regulated PKC-epsilon, as shown by Western blots, and abolished the phorbol ester-evoked contraction at submaximal Ca2+, but not Ca2+-independent, contractions induced by the phosphatase inhibitor microcystin. Contractions induced by microcystin in Ca2+-free solution were associated with increased phosphorylation of myosin light chain kinase (MLCK). Activation of MLCK by autophosphorylation in the absence of Ca2+ occurs in vitro (1). We conclude that PKC-epsilon is neither necessary nor sufficient for Ca2+-independent regulation of myosin II in smooth muscle, but contractions induced by agents that inhibit smooth muscle myosin phosphatase in the absence of Ca2+ may be mediated by MLCK autophosphorylated or activated by another Ca2+-independent kinase.
我们研究的目的是确定佛波酯和平滑肌肌球蛋白磷酸酶抑制剂在无Ca2+情况下诱导平滑肌收缩的机制。蛋白激酶C-ε(PKC-ε)此前在很大程度上因其在雪貂门静脉中被认为不存在而与该过程有关,并且在这种同工型的存在与平滑肌独立于Ca2+收缩的能力以及肌球蛋白20 kDa调节轻链(MLC20)的磷酸化之间建立了相关性。我们在此用两种抗体进行了证明,一种针对PKC-ε的NH2末端,另一种针对其COOH末端,结果显示ε存在于雪貂门静脉和兔门静脉平滑肌中,而在无Ca2+的情况下,这两种平滑肌均未表现出佛波酯诱导的收缩。然而,在钳制的亚最大Ca2+存在时,佛波酯使雪貂门静脉平滑肌中的MLC20磷酸化从17.7±1.7%增加到46.4±3.6%,并引起力量增加。如蛋白质印迹所示,用佛波酯对雪貂门静脉进行长时间(48小时)孵育会使PKC-ε完全下调,并消除亚最大Ca2+时佛波酯诱发的收缩,但不会消除由磷酸酶抑制剂微囊藻毒素诱导的不依赖Ca2+的收缩。在无Ca2+溶液中微囊藻毒素诱导的收缩与肌球蛋白轻链激酶(MLCK)磷酸化增加有关。在体外,MLCK在无Ca2+情况下通过自身磷酸化被激活(1)。我们得出结论,PKC-ε对于平滑肌中肌球蛋白II的不依赖Ca2+调节既不是必需的也不是充分的,但在无Ca2+情况下由抑制平滑肌肌球蛋白磷酸酶的试剂诱导的收缩可能由被另一种不依赖Ca2+的激酶自身磷酸化或激活的MLCK介导。