[HTML][HTML] Structural basis for Chk1 inhibition by UCN-01
B Zhao, MJ Bower, PJ McDevitt, H Zhao… - Journal of Biological …, 2002 - ASBMB
Chk1 is a serine-threonine kinase that plays an important role in the DNA damage response,
including G 2/M cell cycle control. UCN-01 (7-hydroxystaurosporine), currently in clinical
trials, has recently been shown to be a potent Chk1 inhibitor that abrogates the G 2/M
checkpoint induced by DNA-damaging agents. To understand the structural basis of Chk1
inhibition by UCN-01, we determined the crystal structure of the Chk1 kinase domain in
complex with UCN-01. Chk1 structures with staurosporine and its analog SB-218078 were …
including G 2/M cell cycle control. UCN-01 (7-hydroxystaurosporine), currently in clinical
trials, has recently been shown to be a potent Chk1 inhibitor that abrogates the G 2/M
checkpoint induced by DNA-damaging agents. To understand the structural basis of Chk1
inhibition by UCN-01, we determined the crystal structure of the Chk1 kinase domain in
complex with UCN-01. Chk1 structures with staurosporine and its analog SB-218078 were …