Introduction: Signal transduction cascades drive cellular proliferation, apoptosis, immune, and survival pathways. Proteins have emerged as actionable drug targets because they are often dysregulated in cancer, due to underlying genetic mutations, or dysregulated signaling pathways. Cancer drug development relies on proteomic technologies to identify potential biomarkers, mechanisms-of-action, and to identify protein binding hot spots.

Areas covered: Brief summaries of proteomic technologies for drug discovery include mass spectrometry, reverse phase protein arrays, chemoproteomics, and fragment based screening. Protein-protein interface mapping is presented as a promising method for peptide therapeutic development. The topic of biosimilar therapeutics is presented as an opportunity to apply proteomic technologies to this new class of cancer drug.

Expert opinion: Proteomic technologies are indispensable for drug discovery. A suite of technologies including mass spectrometry, reverse phase protein arrays, and protein-protein interaction mapping provide complimentary information for drug development. These assays have matured into well controlled, robust technologies. Recent regulatory approval of biosimilar therapeutics provides another opportunity to decipher the molecular nuances of their unique mechanisms of action. The ability to identify previously hidden protein hot spots is expanding the gamut of potential drug targets. Proteomic profiling permits lead compound evaluation beyond the one drug, one target paradigm.

简介：信号转导级联驱动细胞增殖、凋亡、免疫和生存途径。蛋白质已成为可行的药物靶点，因为由于潜在的基因突变或信号通路失调，它们在癌症中常常失调。癌症药物开发依靠蛋白质组学技术来识别潜在的生物标志物、作用机制，并识别蛋白质结合热点。

涵盖领域：用于药物发现的蛋白质组学技术的简要概述包括质谱、反相蛋白质阵列、化学蛋白质组学和基于片段的筛选。蛋白质-蛋白质界面图谱被认为是肽治疗开发的一种有前途的方法。生物仿制药疗法主题是将蛋白质组学技术应用于此类新型癌症药物的机会。

专家观点：蛋白质组学技术对于药物发现是不可或缺的。包括质谱、反相蛋白质阵列和蛋白质-蛋白质相互作用图谱在内的一系列技术为药物开发提供了补充信息。这些检测方法已经成熟，成为控制良好、稳健的技术。最近对生物仿制药疗法的监管批准提供了另一个机会来破译其独特作用机制的分子细微差别。识别以前隐藏的蛋白质热点的能力正在扩大潜在药物靶标的范围。蛋白质组分析允许先导化合物评估超越一种药物、一种靶标范式。