Department of Pharmacology, University of Valencia, Av. Vicent Andrés Estellés s/n, 46100 Burjasot, Valencia, Spain.
Biochem Pharmacol. 2010 Jul 1;80(1):13-21. doi: 10.1016/j.bcp.2010.02.017. Epub 2010 Mar 3.
Osteoarthritis (OA) is a chronic degenerative joint disorder characterized by destruction of the articular cartilage, subchondral bone alterations and synovitis. Current treatments are focused on symptomatic relief but they lack efficacy to control the progression of this disease which is a leading cause of disability. Therefore, the development of effective disease-modifying drugs is urgently needed. Different initiatives are in progress to define the molecular mechanisms involved in the initiation and progression of OA. These studies support the therapeutic potential of pathways relevant in joint metabolism such as Wnt/beta-catenin, discoidin domain receptor 2 or proteinase-activated receptor 2. The dysregulation in cartilage catabolism and subchondral bone remodeling could be improved by selective inhibitors of matrix metalloproteinases, aggrecanases and other proteases. Another approach would favor the activity of anabolic processes by using growth factors or regulatory molecules. Recent studies have also revealed the role of oxidative stress and synovitis in the progression of this disease, supporting the development of a number of inhibitory strategies. Novel targets in OA are represented by genes involved in OA pathophysiology discovered using gene network, epigenetic and microRNA approaches. Further insights into the molecular mechanisms involved in OA initiation and progression may lead to the development of new therapies able to control joint destruction and repair.
骨关节炎(OA)是一种慢性退行性关节疾病,其特征为关节软骨破坏、软骨下骨改变和滑膜炎。目前的治疗方法侧重于缓解症状,但缺乏控制疾病进展的疗效,而 OA 是导致残疾的主要原因之一。因此,迫切需要开发有效的疾病修饰药物。目前正在进行不同的研究计划,以确定参与 OA 起始和进展的分子机制。这些研究支持了与关节代谢相关的途径(如 Wnt/β-连环蛋白、盘状结构域受体 2 或蛋白酶激活受体 2)的治疗潜力。通过选择性抑制基质金属蛋白酶、聚集蛋白聚糖酶和其他蛋白酶,可以改善软骨分解代谢和软骨下骨重塑的失调。另一种方法是通过使用生长因子或调节分子来促进合成代谢过程的活性。最近的研究还揭示了氧化应激和滑膜炎在疾病进展中的作用,支持了许多抑制策略的发展。OA 的新靶点是使用基因网络、表观遗传学和 microRNA 方法发现的参与 OA 病理生理学的基因。对 OA 起始和进展中涉及的分子机制的进一步了解可能会导致开发出能够控制关节破坏和修复的新疗法。