2. Academic Validation
  3. Identification of death-associated protein kinases inhibitors using structure-based virtual screening

Identification of death-associated protein kinases inhibitors using structure-based virtual screening

  • J Med Chem. 2009 Nov 26;52(22):7323-7. doi: 10.1021/jm901191q.
Masako Okamoto 1,  Kiyoshi Takayama,  Tomoko Shimizu,  Kazuhiro Ishida,  Osamu Takahashi,  Toshio Furuya
Affiliations

Affiliation

  • 1 Drug Discovery Department, Research and Development Division, PharmaDesign, Inc., 2-19-8 Hatchobori, Chuo-ku, Tokyo 104-0032, Japan. okamoto@pharmadesign.co.jp
PMID: 19877644 DOI: 10.1021/jm901191q
Abstract

Death-associated protein kinases (DAPKs) function in the early stages of eukaryotic programmed cell death. DAPKs are now emerging as targets for drug discovery in novel therapeutic approaches for ischemic diseases in the brain, heart, kidney, and Other organs. Using a structure-based virtual screening approach, we discovered potent and selective DAPKs inhibitors. 6 was found to be the most potent inhibitor with Enzyme selectivity (IC(50) = 69 nM for DAPK1).

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-15513
    98.26%, DAPK Inhibitor