Abstract：
UNASSIGNED: PROteolysis-TArgeting Chimeras (PROTACs) allow the selective degradation of a protein of interest (POI) by the ubiquitin-proteasome system (UPS). With this unique mechanism of action, the research and development of PROTACs that target the Breakpoint Cluster Region Abelson (BCR-ABL) tyrosine kinase (TK) has been increasing dramatically, as they are promising molecules in the treatment of Chronic Myeloid Leukemia (CML), one of the main hematological malignancies, which results from an uncontrolled myeloproliferation due to the constitutive activation of BCR-ABL.
UNASSIGNED: This review summarizes the patents/applications published in the online databases like Espacenet or World Intellectual Property Organization regarding PROTACs that promote BCR-ABL degradation. Patents will be described mostly in terms of chemical structure, biochemical/pharmacological activities, and potential clinical applications.
UNASSIGNED: The recent discovery of the enormous potential of PROTACs led to the creation of new compounds capable of degrading BCR-ABL for the treatment of CML. Although still in reduced numbers, and in the pre-clinical phase of development, some compounds have already been shown to overcome some of the difficulties presented by conventional BCR-ABL inhibitors, such as the well-known imatinib. Therefore, it is very likely that some of the present PROTACs will enter future CML therapy in the coming years.
UNASSIGNED: This review summarizes the patents/applications published in the online databases like Espacenet or World Intellectual Property Organization regarding PROTACs that promote BCR-ABL degradation. Patents will be described mostly in terms of chemical structure, biochemical/pharmacological activities, and potential clinical applications.
UNASSIGNED: The recent discovery of the enormous potential of PROTACs led to the creation of new compounds capable of degrading BCR-ABL for the treatment of CML. Although still in reduced numbers, and in the pre-clinical phase of development, some compounds have already been shown to overcome some of the difficulties presented by conventional BCR-ABL inhibitors, such as the well-known imatinib. Therefore, it is very likely that some of the present PROTACs will enter future CML therapy in the coming years.
摘要：
■蛋白质溶解-调整嵌合体（PROTACs）允许泛素-蛋白酶体系统（UPS）选择性降解感兴趣的蛋白质（POI）。有了这种独特的作用机制，针对断点簇区Abelson(BCR-ABL)酪氨酸激酶(TK,因为它们是治疗慢性粒细胞白血病（CML）的有前途的分子，主要的血液恶性肿瘤之一，这是由于BCR-ABL的组成型激活导致的不受控制的骨髓增殖。
■本综述总结了在Espacenet或世界知识产权组织等在线数据库中发布的有关促进BCR-ABL降解的PROTACs的专利/申请。专利将主要在化学结构方面进行描述，生化/药理活性，和潜在的临床应用。
■最近对PROTACs巨大潜力的发现导致产生了能够降解BCR-ABL的新化合物，用于治疗CML。虽然数量仍然减少，在发展的临床前阶段，一些化合物已经被证明可以克服常规BCR-ABL抑制剂带来的一些困难，例如著名的伊马替尼。因此,目前的一些PROTACs很有可能在未来几年进入未来的CML治疗.
■本综述总结了在Espacenet或世界知识产权组织等在线数据库中发布的有关促进BCR-ABL降解的PROTACs的专利/申请。专利将主要在化学结构方面进行描述，生化/药理活性，和潜在的临床应用。
■最近对PROTACs巨大潜力的发现导致产生了能够降解BCR-ABL的新化合物，用于治疗CML。虽然数量仍然减少，在发展的临床前阶段，一些化合物已经被证明可以克服常规BCR-ABL抑制剂带来的一些困难，例如著名的伊马替尼。因此,目前的一些PROTACs很有可能在未来几年进入未来的CML治疗.
