Tyrosine Kinases are enzymes that catalyse the phosphorylation of the tyrosine residues of their substrates and activate downstream pathways involved in cellular proliferation. Their overexpression/hyper-activity is implicated in numerous different cancerous cell lines. Small molecule Tyrosine Kinase Inhibitors (TKi’s), such as Imatinib, Erlotinib and Sunitinib have been developed as targeted anti-cancer therapeutics but, at the moment, their clinical usage is hindered due to acquired and innate resistance and/or dose limiting side effects. Recently, Metal-Tyrosine Kinase Inhibitor conjugates have become a promising field to overtake these drawbacks since the TKi’s show potential to improve selectivity and pharmacological properties of metal-based drugs, overcoming the resistance associated with current TKi’s. Metal-Tyrosine Kinase Inhibitor conjugates further find applications in several biological fields as dual-modal activity drugs, pro-drug systems and selective metal theragnostics. In this review, advancements over the past decade in the field of metal based-TKi conjugates are discussed and insights are provided to successfully develop metal – TKi conjugates. Four main TK targets are discussed here: EGFR (Epidermal Growth Factor Receptor), BCR-ABL (Breakpoint Cluster Region – Abelson Kinase), PDGFR (Platelet Derived Growth Factor Receptor) and VEGFR (Vascular Endothelial Growth Factor Receptor). Future perspectives and applications of this promising research area are also outlined.

酪氨酸激酶是催化其底物的酪氨酸残基磷酸化并激活参与细胞增殖的下游途径的酶。它们的过表达/高活性与许多不同的癌细胞系有关。小分子酪氨酸激酶抑制剂 (Tki)，如伊马替尼、厄洛替尼和舒尼替尼已被开发为靶向抗癌治疗药物，但目前，由于获得性和先天性耐药性和/或剂量限制性副作用，它们的临床应用受到阻碍。最近，金属-酪氨酸激酶抑制剂缀合物已成为克服这些缺点的有希望的领域，因为 Tki 显示出提高金属基药物的选择性和药理学特性的潜力，克服了与当前 Tki 相关的耐药性。Metal-Tyrosine Kinase Inhibitor conjugates 进一步发现在多个生物领域中作为双模式活性药物、前药系统和选择性金属治疗学的应用。在这篇综述中，我们讨论了过去十年在金属基 TKi 偶联物领域取得的进展，并为成功开发金属 TKi 偶联物提供了见解。这里讨论了四个主要的 TK 靶点：EGFR（表皮生长因子受体）、BCR-ABL（断点簇区域 - Abelson 激酶）、PDGFR（血小板衍生生长因子受体）和 VEGFR（血管内皮生长因子受体）。还概述了这一有前途的研究领域的未来前景和应用。讨论了过去十年在金属基 TKi 偶联物领域的进展，并提供了成功开发金属 TKi 偶联物的见解。这里讨论了四个主要的 TK 靶点：EGFR（表皮生长因子受体）、BCR-ABL（断点簇区域 - Abelson 激酶）、PDGFR（血小板衍生生长因子受体）和 VEGFR（血管内皮生长因子受体）。还概述了这一有前途的研究领域的未来前景和应用。讨论了过去十年在金属基 TKi 偶联物领域的进展，并提供了成功开发金属 TKi 偶联物的见解。这里讨论了四个主要的 TK 靶点：EGFR（表皮生长因子受体）、BCR-ABL（断点簇区域 - Abelson 激酶）、PDGFR（血小板衍生生长因子受体）和 VEGFR（血管内皮生长因子受体）。还概述了这一有前途的研究领域的未来前景和应用。PDGFR（血小板衍生生长因子受体）和 VEGFR（血管内皮生长因子受体）。还概述了这一有前途的研究领域的未来前景和应用。PDGFR（血小板衍生生长因子受体）和 VEGFR（血管内皮生长因子受体）。还概述了这一有前途的研究领域的未来前景和应用。