■据报道,PIM激酶(PIM-1,PIM-2和PIM-3)在控制细胞存活的信号级联中起关键作用,扩散,和差异化。这些激酶的过度表达导致血液恶性肿瘤,如弥漫性大B细胞淋巴瘤(DLBCL),多发性骨髓瘤,白血病,淋巴瘤和前列腺癌等.PIM激酶作为生物标志物和潜在的治疗靶标已显示出对精确癌症治疗的希望。选择性PIM-1、PIM-2和/或PIM-3同种型抑制剂已经在患有晚期癌症(包括复发性/难治性癌症)的患者中显示出显著结果。
■关于PIM激酶(PIM-1,PIM-2和PIM-3)在肿瘤发生中的综合文献综述,获得专利的PIM激酶抑制剂(2016年至今),和他们的药理学和结构见解已被强调。
■最近,PIM激酶即.作为治疗靶标的PIM-1、PIM-2和PIM-3(丝氨酸/苏氨酸蛋白激酶家族的成员)已经在肿瘤学特别是血液恶性肿瘤中引起了相当大的兴趣。专利的PIM激酶抑制剂由杂环(稠合)环结构(如吲哚)组成,吡啶,吡嗪,吡唑,吖嗪,哌嗪,噻唑,恶二唑,喹啉,三唑并吡啶,吡唑并吡啶,咪唑并吡啶嗪,恶二唑-硫酮,吡唑并嘧啶,三唑并吡啶嗪,咪唑并吡啶嗪,吡唑并喹唑啉和吡唑并吡啶等。在癌症化疗中显示出有希望的结果。
UNASSIGNED: PIM Kinases (PIM-1, PIM-2, and PIM-3) have been reported to play crucial role in signaling cascades that govern cell survival, proliferation, and differentiation. Over-expression of these kinases leads to hematological malignancies such as diffuse large B cell lymphomas (DLBCL), multiple myeloma, leukemia, lymphoma and prostate cancer etc. PIM kinases as biomarkers and potential therapeutic targets have shown promise toward precision cancer therapy. The selective PIM-1, PIM-2, and/or PIM-3 isoform inhibitors have shown significant results in patients with advanced stages of cancer including relapsed/refractory cancer.
UNASSIGNED: A comprehensive literature
review of PIM Kinases (PIM-1, PIM-2, and PIM-3) in oncogenesis, the patented PIM kinase inhibitors (2016-Present), and their pharmacological and structural insights have been highlighted.
UNASSIGNED: Recently, PIM kinases viz. PIM-1, PIM-2, and PIM-3 (members of the serine/threonine protein kinase family) as therapeutic targets have attracted considerable interest in oncology especially in hematological malignancies. The patented PIM kinase inhibitors comprised of heterocyclic (fused)ring structure(s) like indole, pyridine, pyrazine, pyrazole, pyridazine, piperazine, thiazole, oxadiazole, quinoline, triazolo-pyridine, pyrazolo-pyridine, imidazo-pyridazine, oxadiazole-thione, pyrazolo-pyrimidine, triazolo-pyridazine, imidazo-pyridazine, pyrazolo-quinazoline and pyrazolo-pyridine etc. showed promising results in cancer chemotherapy.