J Drugs Dermatol. 2024 Aug 1;23(8):645-652. doi: 10.36849/JDD.8293.
Members of the Janus kinase (JAK) superfamily, comprising tyrosine kinase 2 (TYK2) and JAK1, JAK2, and JAK3, mediate signaling by cytokines (eg, interleukin [IL]-23) involved in psoriasis pathogenesis. Binding of IL-23 to its receptor activates TYK2 and JAK2, which trigger signal transducer and activator of transcription (STAT) translocation to the nucleus to regulate target gene transcription, including genes of proinflammatory mediators such as IL-17. Physiologically, TYK2 solely mediates immune function, whereas JAK1,2,3 mediate broad systemic and immune functions. Inhibition of individual JAK family members is being evaluated in many dermatologic indications, including psoriasis. Selective TYK2 inhibition is therefore expected to be associated with few adverse effects in patients with psoriasis. People with genetic mutations leading to loss of function of TYK2 are protected from the development of psoriasis without an increased risk of infections or malignancies. In contrast, treatments with JAK1,2,3 inhibitors are associated with various systemic effects. We review the unique allosteric mechanism of action of the selective TYK2 inhibitor, deucravacitinib, which binds to the TYK2 regulatory (pseudokinase) domain, and the mechanisms of action of JAK1,2,3 inhibitors, which bind to the adenosine 5'-triphosphate-binding active (catalytic) site in the kinase domains of JAK1,2,3. Deucravacitinib, which is approved for the treatment of moderate to severe plaque psoriasis in adults in the United States and several other countries, represents a novel, targeted systemic treatment approach with a favorable safety profile. J Drugs Dermatol. 2024;23(8):645-652. doi:10.36849/JDD.8293.
Janus 激酶(JAK)家族成员包括酪氨酸激酶 2(TYK2)和 JAK1、JAK2、JAK3,介导细胞因子(如白细胞介素[IL]-23)参与银屑病发病机制的信号转导。IL-23 与其受体结合激活 TYK2 和 JAK2,触发信号转导和转录激活因子(STAT)向核内易位,以调节包括促炎介质(如 IL-17)在内的靶基因转录。在生理上,TYK2 仅介导免疫功能,而 JAK1、2、3 则介导广泛的系统和免疫功能。目前正在许多皮肤科适应证中评估包括银屑病在内的个体 JAK 家族成员的抑制作用。因此,选择性 TYK2 抑制作用预计与银屑病患者的不良反应较少相关。导致 TYK2 功能丧失的遗传突变患者不会发生银屑病,且不会增加感染或恶性肿瘤的风险。相比之下,JAK1、2、3 抑制剂的治疗与各种全身效应相关。我们回顾了选择性 TYK2 抑制剂地舒单抗的独特变构作用机制,它与 TYK2 调节(假激酶)结构域结合,以及 JAK1、2、3 抑制剂的作用机制,它们与 JAK1、2、3 的腺苷 5'-三磷酸结合活性(催化)结构域结合。地舒单抗已在美国和其他几个国家获得批准用于治疗成人中度至重度斑块型银屑病,代表了一种具有良好安全性特征的新型靶向全身治疗方法。皮肤病药物杂志。2024;23(8):645-652。doi:10.36849/JDD.8293.