Tomomura Mineko, Tomomura Akito
Mineko Tomomura, Meikai Pharmaco-Medical Laboratory, MPL and Division of Biochemistry, Department of Oral Biology and Tissue Engineering, Meikai University School of Dentistry, Sakado, Saitama 350-0283, Japan.
World J Biol Chem. 2015 Nov 26;6(4):358-65. doi: 10.4331/wjbc.v6.i4.358.
Caldecrin was originally isolated from the pancreas as a factor that reduced serum calcium levels. This secreted serine protease has chymotrypsin-like activity and is also known as chymotrypsin C; it belongs to the elastase family. Although intravenous administration of caldecrin decreases the serum calcium concentration even when its protease activity is blocked, this effect does require cleavage of caldecrin's pro-peptide by trypsin, converting it to the mature enzyme. Ectopic intramuscular expression of caldecrin prevented bone resorption in ovariectomized mice. Caldecrin inhibited parathyroid hormone-stimulated calcium release from fetal mouse long bone organ cultures. Furthermore, caldecrin suppressed the formation of osteoclasts from bone marrow cells by inhibiting the receptor activator of nuclear factor-κ B ligand (RANKL)-stimulated phospholipase Cγ-calcium oscillation-calcineurin-nuclear factor of activated T-cells, cytoplasmic 1 pathway. Caldecrin also suppressed the bone resorption activity of mature osteoclasts by preventing RANKL-stimulated Src activation, calcium entry, and actin ring formation. In vivo and in vitro studies have indicated that caldecrin is a unique multifunctional protease with anti-osteoclastogenic activities that are distinct from its protease activity. Caldecrin might be a potential therapeutic target for the treatment of osteolytic diseases such as osteoporosis and osteoarthritis. This mini-review describes caldecrin's historical background and its mechanisms of action.
钙降素最初是从胰腺中分离出来的一种可降低血清钙水平的因子。这种分泌型丝氨酸蛋白酶具有胰凝乳蛋白酶样活性,也被称为胰凝乳蛋白酶C;它属于弹性蛋白酶家族。尽管静脉注射钙降素即使在其蛋白酶活性被阻断时也会降低血清钙浓度,但这种作用确实需要胰蛋白酶切割钙降素的前肽,将其转化为成熟酶。钙降素在卵巢切除小鼠中的异位肌肉表达可预防骨吸收。钙降素抑制甲状旁腺激素刺激的胎鼠长骨器官培养物中的钙释放。此外,钙降素通过抑制核因子κB受体激活剂配体(RANKL)刺激的磷脂酶Cγ-钙振荡-钙调神经磷酸酶-活化T细胞核因子细胞质1途径,抑制骨髓细胞形成破骨细胞。钙降素还通过阻止RANKL刺激的Src激活、钙内流和肌动蛋白环形成,抑制成熟破骨细胞的骨吸收活性。体内和体外研究表明,钙降素是一种独特的多功能蛋白酶,具有与其蛋白酶活性不同的抗破骨细胞生成活性。钙降素可能是治疗骨质疏松症和骨关节炎等溶骨性疾病的潜在治疗靶点。这篇小型综述描述了钙降素的历史背景及其作用机制。