Kinase Inhibitors of Marine Origin

Marine Pharmaceuticals: A New Wave of Anti-angiogenic Drugs

“…CDK-4 is a catalytic subunit whose presence is crucial for the succession of the cell cycle through the G1 phase [41]. Studies have also shown that fascaplysin does not inhibit any other tyrosine kinases and is a poor inhibitor of other types of CDK [42]. Philinopside A and Philinopside E Philinopsides A, B, E and F are triterpene glycosides isolated from the sea cucumber Pentacta quadrangularis, exhibiting significant cytotoxicity against various cancer cell lines.…”

Synthesis and Cytotoxicity of N12-Ethyl Substituted Indolocarbazole Derivatives

“…但 STA 的选择性差, 可作用于多种细 胞信号转导通路, 且毒性大 [18] , 限制了其作为抗肿瘤药 物的使用. 随后药物化学家对其进行结构改造, 多个衍 生物已经作为抗肿瘤药物进入了临床研究 [19] . 多靶点 的蛋白激酶抑制剂 PKC-412 [20] 可以有效抑制人白血病 细胞的增殖 [21] , 在临床 I 期研究中表现出了安全性和有 效性 [22] .…”

“…临床 II 期研究结果表明, PKC-412 对 FMS 样酪 氨酸激酶 3 (Flt-3)突变型和野生型的急性骨髓性白血病 受试者均有效 [23] . 目前正处于侵袭性全身性肥大细胞 增多症/肥大细胞白血病的临床 II 期和 Flt-3 突变的急性 骨髓性白血病的临床 III 期研究 [19,23] . Lestaurtinib [24] 对含 有野生型和突变型 Flt-3 的急性白血病细胞均有效 [25] , 并能诱导霍奇金淋巴瘤细胞凋亡 [26] .…”

Targeting Cellular Proapoptotic Agents from Marine Sources

“…Other kinase inhibitors of marine origin have been recently reviewed by Sandip B. Bharate, et al [96]. These marine derived kinase inhibitor include serine/ threonine kinase inhibitors, cyclin-dependent kinase inhibitors, glycogen synthase kinase-3 inhibitors, check-point kinase inhibitors, casein kinase inhibitors, mitogenactivated protein kinase inhibitors, and polo-like kinase inhibitors.…”