Pfizer Research and Development, Medicinal Chemistry, 559 Eastern Point Rd., Groton, CT 06340, USA.
Expert Opin Ther Pat. 2011 Jul;21(7):1045-69. doi: 10.1517/13543776.2011.577068. Epub 2011 May 9.
MAPK/extracellular signal-regulated kinase (MEK) inhibitors target the Ras/Raf/MEK/ERK signaling pathway, which is important in cell growth, differentiation and development. The pathway has been implicated in the progression of a variety of diseases, in particular cancer, as well as in immune and inflammatory diseases such as rheumatoid arthritis, organ transplant rejection, septic shock, asthma and viral infection.
A comprehensive review of the patent literature (2008 - 2010) covering MEK inhibitors and combinations thereof is provided in this paper.
The first MEK inhibitor was described in the literature in 1995, and several companies are still active in the research and development of MEK inhibitors for various disease states. The emerging role of MEK inhibitors in disease has prompted further investigations of this important target. The combination of MEK inhibitors with other agents/therapies in the treatment of diseases, particularly cancer, is a key development in the field.
MAPK/细胞外信号调节激酶（MEK）抑制剂针对 Ras/Raf/MEK/ERK 信号通路，该通路在细胞生长、分化和发育中起着重要作用。该通路与多种疾病的进展有关，特别是癌症，以及免疫和炎症性疾病，如类风湿性关节炎、器官移植排斥、感染性休克、哮喘和病毒感染。
本文对涵盖 MEK 抑制剂及其组合的专利文献（2008-2010 年）进行了全面回顾。
第一个 MEK 抑制剂于 1995 年在文献中描述，几家公司仍在积极研究 MEK 抑制剂，以治疗各种疾病状态。MEK 抑制剂在疾病中的新作用促使人们进一步研究这一重要靶点。在治疗疾病，特别是癌症方面，将 MEK 抑制剂与其他药物/疗法联合使用是该领域的一个关键发展。
