Hospital Infantil Universitario Virgen del Rocío, Unidad de Cuidados Intensivos Pediátricos, Av. Manuel Siurot s/n, 41013 - Sevilla, Spain.
Expert Opin Ther Pat. 2012 Jul;22(7):735-46. doi: 10.1517/13543776.2012.697153. Epub 2012 Jun 15.
After binding to the neurokinin (NK-1) receptor, substance P (SP) induces tumor cell proliferation, the migration of tumor cells (invasion and metastasis) and angiogenesis. By contrast, NK-1 receptor antagonists inhibit tumor cell proliferation (tumor cells die by apoptosis), block the migratory activity of tumor cells and exert antiangiogenic properties.
This review offers a 12-year overview of the underlying mechanism of the action of the SP/NK-1 receptor system and NK-1 receptor antagonists in cancer, providing a new approach to the treatment of tumors.
Chemically diverse NK-1 receptor antagonists have been identified. The antitumor action of these compounds is independent of their chemical structures and such action is associated with their affinity for the NK-1 receptor and with the dose of the antagonist administered. The NK-1 receptor can be considered as a target in cancer treatment and NK-1 receptor antagonists could be considered as new antitumor drugs. The NK-1 receptor antagonist aprepitant is used in clinical practice and exerts an antitumor action against tumor cells in vitro. In the future, such antitumor action should be tested in human clinical trials.
与神经激肽（NK-1）受体结合后，P 物质（SP）可诱导肿瘤细胞增殖、肿瘤细胞迁移（侵袭和转移）和血管生成。相比之下，NK-1 受体拮抗剂可抑制肿瘤细胞增殖（肿瘤细胞通过细胞凋亡死亡）、阻断肿瘤细胞的迁移活性并发挥抗血管生成特性。
本文对 SP/NK-1 受体系统和 NK-1 受体拮抗剂在癌症中的作用机制进行了为期 12 年的综述，为肿瘤治疗提供了新方法。
已经鉴定出化学结构多样的 NK-1 受体拮抗剂。这些化合物的抗肿瘤作用与其化学结构无关，与 NK-1 受体的亲和力以及拮抗剂的给药剂量有关。NK-1 受体可被视为癌症治疗的靶点，NK-1 受体拮抗剂可被视为新型抗肿瘤药物。NK-1 受体拮抗剂阿瑞匹坦已在临床实践中应用，并在体外对肿瘤细胞发挥抗肿瘤作用。未来，应在人体临床试验中检验这种抗肿瘤作用。
