Cancer Research, Abbott Laboratories, Department R47J, Building AP10, 100 Abbott Park Road, Abbott Park, IL 60064, USA.
Expert Opin Ther Pat. 2010 Jul;20(7):885-97. doi: 10.1517/13543776.2010.493559.
Platelet-derived growth factor receptor (PDGFR) is a compelling target for developing therapeutic agents to treat diseases associated with overactivated platelet-derived growth factor (PDGF) signaling and has proved to be particularly encouraging for cancer treatment. The efforts in this area have been greatly enhanced by the approval of tyrosine kinase inhibitors with PDGFR inhibitory activity such as imatinib, sunitinib and sorafenib.
This review surveys the small molecule PDGFR inhibitors reported in patent literature over the past 5 years (2005 - 2009).
The reader will gain an overview of the chemical scaffolds and the activity/selectivity of the newly discovered PDGFR inhibitors.
Targeting PDGFR kinase with small molecule inhibitors has remained a very active area. Many new and novel PDGFR inhibitors with different selectivity profiles are being discovered and evaluated. In cancer therapy, the identification of novel and potent PDGFR inhibitors with preferred kinase inhibitory profiles that deliver superior antitumor efficacy, yet have manageable side effects and toxicities, will continue to be the key for success. Additionally, interest in targeting PDGF signaling for intervention of various vascular diseases and fibrotic conditions is expected to continue to grow.
血小板衍生生长因子受体（PDGFR）是一个引人注目的目标，开发治疗药物，以治疗与过度激活血小板衍生生长因子（PDGF）信号相关的疾病，并已被证明对癌症治疗特别有希望。由于批准了具有 PDGFR 抑制活性的酪氨酸激酶抑制剂，如伊马替尼、舒尼替尼和索拉非尼，该领域的努力得到了极大的增强。
调查了过去 5 年（2005-2009 年）专利文献中报道的小分子 PDGFR 抑制剂。
读者将获得对新发现的 PDGFR 抑制剂的化学结构骨架和活性/选择性的概述。
用小分子抑制剂靶向 PDGFR 激酶仍然是一个非常活跃的领域。正在发现和评估许多具有不同选择性特征的新型和新型 PDGFR 抑制剂。在癌症治疗中，识别具有优选激酶抑制谱的新型和有效的 PDGFR 抑制剂，提供更好的抗肿瘤疗效，同时具有可管理的副作用和毒性，将继续是成功的关键。此外，预计针对 PDGF 信号转导以干预各种血管疾病和纤维化疾病的兴趣将继续增长。
