Targeting CXCR1/CXCR2 receptor antagonism in malignant melanoma.
Targeting CXCR1/CXCR2 receptor antagonism in malignant melanoma.
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DOI：
10.1517/14728221003652471
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发表时间：
2010-04
影响因子：
5.8
通讯作者：
Singh RK
中科院分区：
文献类型：
--
作者：
Sharma B;Singh S;Varney ML;Singh RK
恶性黑色素瘤的发病率在全世界都在增加，目前在男性中比任何其他癌症都增长得快，在女性中仅次于肺癌。目前的治疗策略集中在全身治疗，对生存率没有影响。因此，迫切需要开发新的靶向治疗剂。我们的目标是提供一个关于恶性黑色素瘤中靶向CXCR 1/2的概述，这些方法背后的原理和未来的前景。本文综述了CXCR 1/2受体在黑色素瘤进展和转移中的作用。我们描述了正在开发的阻断CXCR 1/2激活的方法，包括低分子量拮抗剂，修饰的趋化因子和针对配体和受体的抗体。趋化因子受体CXCR 1和CXCR 2及其配体在恶性黑色素瘤的发病机制中起重要作用。最近的报道表明，CXCR 1是组成性表达的所有黑色素瘤的情况下，无论阶段和级别，然而，CXCR 2的表达仅限于侵袭性黑色素瘤肿瘤。此外，CXCR 1/2表达和/或活性的调节已显示出调节恶性黑素瘤生长、血管生成和转移，表明CXCR 1/2靶向作为恶性黑素瘤的新治疗方法。
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 have shown no effect on survival. Therefore there is a pressing need for developing novel targeted therapeutics. Our goal is to provide an overview regarding targeting CXCR1/2 in malignant melanoma, the rationale behind these approaches and the future perspective. 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. 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.
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