Interventional Radiology Unit with Integrated Section of Transational Medical Oncology National Cancer Research Centre, Cancer Institute"Giovanni Paolo II", Bari, Italy.
Crit Rev Oncol Hematol. 2013 Nov;88(2):293-308. doi: 10.1016/j.critrevonc.2013.05.009. Epub 2013 Jun 13.
Tyrosine kinase receptors (TKRs) play a key role in tumour cell proliferation and survival since they are involved in endothelial cell activation leading to tumour neoangiogenesis. In particular, vascular endothelial growth factor receptors (VEGFRs), platelet-derived growth factor receptor (PDGFR), stem cell factor receptor (c-KitR), and colony-stimulating factor 1 (CSF-1) are overexpressed or constitutively activated in human and pet malignancies. A variety of small molecule inhibitors targeting specific tyrosine kinases (known as tyrosine kinase inhibitors or TKIs) have recently been approved, or are under investigation, for the treatment of human cancer. TKI application in animal cancer is however relatively recent. This review aims to illustrate the major aspects of tyrosine kinase dysfunctions, with special regard to human and animal cancer of the mammary gland, providing an update on the background of the anti-angiogenic and anti-neoplastic properties of TKIs in human and veterinary cancer.
酪氨酸激酶受体（TKRs）在肿瘤细胞增殖和存活中发挥着关键作用，因为它们参与内皮细胞激活，导致肿瘤新生血管形成。特别是血管内皮生长因子受体（VEGFRs）、血小板衍生生长因子受体（PDGFR）、干细胞因子受体（c-KitR）和集落刺激因子 1（CSF-1）在人和宠物的恶性肿瘤中过度表达或持续激活。最近已经批准了针对特定酪氨酸激酶的多种小分子抑制剂（称为酪氨酸激酶抑制剂或 TKIs），用于治疗人类癌症。然而，TKI 在动物癌症中的应用相对较新。本文旨在阐述酪氨酸激酶功能障碍的主要方面，特别关注人类和动物乳腺肿瘤，提供人类和兽医肿瘤中 TKIs 的抗血管生成和抗肿瘤特性的最新背景。
