Mari Ikuta

Summary

Affiliation: Merck Research Laboratories
Country: USA

Publications

  1. pmc Crystal structures of the N-terminal kinase domain of human RSK1 bound to three different ligands: Implications for the design of RSK1 specific inhibitors
    Mari Ikuta
    Department of Structural Biology, Merck Research Laboratories, West Point, Pennsylvania 19486, USA
    Protein Sci 16:2626-35. 2007
  2. doi request reprint Pyridyl aminothiazoles as potent inhibitors of Chk1 with slow dissociation rates
    Vadim Y Dudkin
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
    Bioorg Med Chem Lett 22:2609-12. 2012
  3. ncbi request reprint Synthesis and evaluation of substituted benzoisoquinolinones as potent inhibitors of Chk1 kinase
    Robert M Garbaccio
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
    Bioorg Med Chem Lett 17:6280-5. 2007
  4. ncbi request reprint Optimization of a pyrazoloquinolinone class of Chk1 kinase inhibitors
    Edward J Brnardic
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
    Bioorg Med Chem Lett 17:5989-94. 2007
  5. ncbi request reprint 3-(Indol-2-yl)indazoles as Chek1 kinase inhibitors: Optimization of potency and selectivity via substitution at C6
    Mark E Fraley
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
    Bioorg Med Chem Lett 16:6049-53. 2006
  6. ncbi request reprint Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure
    Nobuhiko Kawanishi
    Department of Medicinal Chemistry, Banyu Tsukuba Research Institute in collaboration with Merck Research Laboratories, Okubo 3, Tsukuba 300 2611, Ibaraki, Japan
    Bioorg Med Chem Lett 16:5122-6. 2006
  7. ncbi request reprint Development of 6-substituted indolylquinolinones as potent Chek1 kinase inhibitors
    Shaei Huang
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
    Bioorg Med Chem Lett 16:5907-12. 2006

Collaborators

Detail Information

Publications7

  1. pmc Crystal structures of the N-terminal kinase domain of human RSK1 bound to three different ligands: Implications for the design of RSK1 specific inhibitors
    Mari Ikuta
    Department of Structural Biology, Merck Research Laboratories, West Point, Pennsylvania 19486, USA
    Protein Sci 16:2626-35. 2007
    ..Structures of RSK1 ligand complexes offer insights into the design of novel anticancer agents and into the regulation of the catalytic activity of RSKs...
  2. doi request reprint Pyridyl aminothiazoles as potent inhibitors of Chk1 with slow dissociation rates
    Vadim Y Dudkin
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
    Bioorg Med Chem Lett 22:2609-12. 2012
    ....
  3. ncbi request reprint Synthesis and evaluation of substituted benzoisoquinolinones as potent inhibitors of Chk1 kinase
    Robert M Garbaccio
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
    Bioorg Med Chem Lett 17:6280-5. 2007
    ..Further SAR was explored at the solvent front and near to the H1 pocket and resulted in the discovery of low MW, sub-nanomolar inhibitors of Chk1...
  4. ncbi request reprint Optimization of a pyrazoloquinolinone class of Chk1 kinase inhibitors
    Edward J Brnardic
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
    Bioorg Med Chem Lett 17:5989-94. 2007
    ..1 nm)...
  5. ncbi request reprint 3-(Indol-2-yl)indazoles as Chek1 kinase inhibitors: Optimization of potency and selectivity via substitution at C6
    Mark E Fraley
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
    Bioorg Med Chem Lett 16:6049-53. 2006
    ..30nM) that was shown by X-ray crystallography to displace one of three highly conserved water molecules in the HI region of the ATP-binding cleft...
  6. ncbi request reprint Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure
    Nobuhiko Kawanishi
    Department of Medicinal Chemistry, Banyu Tsukuba Research Institute in collaboration with Merck Research Laboratories, Okubo 3, Tsukuba 300 2611, Ibaraki, Japan
    Bioorg Med Chem Lett 16:5122-6. 2006
    ..Biol.Chem.2001, 276, 27548], led to the discovery of potent CDK1,2,4,6 inhibitor that were suitable for iv administration for in vivo study...
  7. ncbi request reprint Development of 6-substituted indolylquinolinones as potent Chek1 kinase inhibitors
    Shaei Huang
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
    Bioorg Med Chem Lett 16:5907-12. 2006
    ..Minimization of these parameters (basic amines, PSA) resulted in Chek1 inhibitors with improved cell potency, and preliminary pharmacokinetic data are presented for several of these compounds...