靶向 CXCR1/CXCR2 受体拮抗作用治疗恶性黑色素瘤。
Targeting CXCR1/CXCR2 receptor antagonism in malignant melanoma.
机构信息
Department of Pathology and Microbiology, University of Nebraska Medical Center, 985900 Nebraska Medical Center, Omaha, NE 68198-5900, USA.
出版信息
Expert Opin Ther Targets. 2010 Apr;14(4):435-42. doi: 10.1517/14728221003652471.
IMPORTANCE OF THE FIELD
The incidence of malignant melanoma is increasing throughout the world and is currently rising faster than any other cancer in men and second only to lung cancer in women. Current strategies focused on systemic therapy for treatment of melanoma have shown no effect on survival. Therefore there is a pressing need for developing novel targeted therapeutics.
AREAS COVERED IN THIS REVIEW
Our goal is to provide an overview regarding targeting CXCR1/2 in malignant melanoma, the rationale behind these approaches and the future perspective.
WHAT THE READER WILL GAIN
This review illustrates our current understanding of CXCR1/2 receptor in melanoma progression and metastasis. We describe approaches that are being developed to block CXCR1/2 activation, including low-molecular-weight antagonists, modified chemokines and antibodies directed against ligands and receptors.
TAKE HOME MESSAGE
The chemokine receptors CXCR1 and CXCR2 and their ligands play an important role in the pathogenesis of malignant melanoma. Recent reports demonstrated that CXCR1 is constitutively expressed in all melanoma cases irrespective of stage and grade, however, CXCR2 expression was restricted to aggressive melanoma tumors,. Furthermore, modulation of CXCR1/2 expression and/or activity has been shown to regulate malignant melanoma growth, angiogenesis and metastasis, suggesting CXCR1/2 targeting as a novel therapeutic approach for malignant melanoma.
重要性领域
恶性黑色素瘤的发病率在全球范围内不断增加，目前其发病率的上升速度超过了其他任何癌症，在男性中仅次于肺癌，在女性中仅次于肺癌。目前针对黑色素瘤的治疗方法主要集中在全身治疗上，但对生存率没有影响。因此，迫切需要开发新的靶向治疗药物。
涵盖范围综述
我们的目标是提供关于在恶性黑色素瘤中靶向 CXCR1/2 的概述，以及这些方法背后的原理和未来展望。
读者将获得什么
这篇综述阐述了我们目前对黑色素瘤进展和转移中 CXCR1/2 受体的理解。我们描述了正在开发的阻止 CXCR1/2 激活的方法，包括小分子拮抗剂、修饰趋化因子和针对配体和受体的抗体。
重要信息
趋化因子受体 CXCR1 和 CXCR2 及其配体在恶性黑色素瘤的发病机制中起着重要作用。最近的报告表明，CXCR1 在所有黑色素瘤病例中均持续表达，无论分期和分级如何，但 CXCR2 表达仅限于侵袭性黑色素瘤肿瘤。此外，调节 CXCR1/2 的表达和/或活性已被证明可调节恶性黑色素瘤的生长、血管生成和转移，这表明靶向 CXCR1/2 是一种治疗恶性黑色素瘤的新方法。
Zotero 插件