title: [Research progress on aurora kinase inhibitor MK-0457 in therapy for some hematological malignancies -- review].
abstract: Recent work indicates that an Aurora kinase inhibitor MK-0457 (VX-680), a small-molecule inhibitor of Aurora kinases A, B, C and BCR-ABL, FLT-3, JAK-2, can block the progression of cell growth cycle, causing apoptosis in a range of human tumors. MK-0457 has the activity against expressions of wild-type and mutated bcr-abl gene, including the T315I mutant, and can inhibit the activity of FLT-3, JAK-2 and their mutated types as well. Clinical applications suggest that the MK-0457 has therapeutic effect on the highly refractory CML and CML with poor prognosis, Ph(+) ALL with T315I mutant, relapse refractory AML and JAK-2 positive myeloproliferative diseases (MPD). The intensive preclinical studies and the on-going phase II clinical trials will open up a new vista of therapy for some hematological malignancies. This review focuses on the pharmacologic action of MK-0457 and its clinical trial as well as combined application.
authors: Department of Hematology, Zhongda Hospital, Southeast University Clinical Medical College, Nanjing, Jiangsu Province, China.
authors: Yi-Qiong
authors: YQ
authors: Liang
authors: Bao-An
authors: BA
authors: Chen
authors: Ya-Li
authors: YL
authors: Chen
mesh_terms: D064127:Aurora Kinases; D019337:Hematologic Neoplasms / Q000145:classification / Q000188:drug therapy*; D006801:Humans; D010879:Piperazines / Q000627:therapeutic use*; D047428:Protein Kinase Inhibitors / Q000627:therapeutic use*; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors*; D003521:Cyclopropanes; D011720:Pyrazoles; D011743:Pyrimidines
chemical_list: D064127:Aurora Kinases; D010879:Piperazines; D047428:Protein Kinase Inhibitors; D017346:Protein Serine-Threonine Kinases; C484810:tozasertib; D003521:Cyclopropanes; D011720:Pyrazoles; D011743:Pyrimidines