BI_2536--targeting the mitotic kinase Polo-like kinase 1 (Plk1).
Human Polo-like kinase 1 (Plk1) is an essential regulator of mitotic progression. Targeted inhibition of this kinase was effective in killing tumor cells in vitro and in vivo. The Plk1 inhibitor BI_2536 was well tolerated and showed antitumor activity in the first clinical trials enrolling patients with advanced solid tumors and refractory or relapsed acute myeloid leukemia.
Wäsch
R
R
Department of Hematology and Oncology, Freiburg University Medical Center, Hugstetterstrasse 55, 79106, Freiburg, Germany. ralph.waesch@uniklinik-freiburg.de
Hasskarl
J
J
Schnerch
D
D
Lübbert
M
M
D000818:Animals; D018797:Cell Cycle Proteins / Q000037:antagonists & inhibitors*; D002986:Clinical Trials as Topic; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy*; D047428:Protein Kinase Inhibitors / Q000627:therapeutic use*; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors*; D011518:Proto-Oncogene Proteins / Q000037:antagonists & inhibitors*; D011621:Pteridines / Q000494:pharmacology / Q000627:therapeutic use*; D000097869:Polo-Like Kinase 1
D018797:Cell Cycle Proteins; D047428:Protein Kinase Inhibitors; D017346:Protein Serine-Threonine Kinases; D011518:Proto-Oncogene Proteins; D011621:Pteridines; D000097869:Polo-Like Kinase 1; C518477:BI 2536