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MARK inhibitors: Declaring a No-Go decision on a chemical series based on extensive DMPK experimentation.
Haidle AM, Childers KK, Zabierek AA, Katz JD, Jewell JP, Hou Y, Altman MD, Szewczak A, Chen D, Harsch A, Hayashi M, Warren L, Hutton M, Nuthall H, Stanton MG, Davies IW, Munoz B, Northrup A. Haidle AM, et al. Bioorg Med Chem Lett. 2017 Jan 1;27(1):109-113. doi: 10.1016/j.bmcl.2016.08.066. Epub 2016 Aug 25. Bioorg Med Chem Lett. 2017. PMID: 27894874
Attempts to optimize pharmacokinetic properties in a promising series of pyrrolopyrimidinone MARK inhibitors for the treatment of Alzheimer's disease are described. ...
Attempts to optimize pharmacokinetic properties in a promising series of pyrrolopyrimidinone MARK inhibitors for the treatment of Alz …
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.
Katz JD, Haidle A, Childers KK, Zabierek AA, Jewell JP, Hou Y, Altman MD, Szewczak A, Chen D, Harsch A, Hayashi M, Warren L, Hutton M, Nuthall H, Su HP, Munshi S, Stanton MG, Davies IW, Munoz B, Northrup A. Katz JD, et al. Bioorg Med Chem Lett. 2017 Jan 1;27(1):114-120. doi: 10.1016/j.bmcl.2016.08.068. Epub 2016 Oct 22. Bioorg Med Chem Lett. 2017. PMID: 27816515
Information gleaned from ligand co-crystal structures allowed for rapid refinements in both MARK potency and kinase selectivity. These efforts allowed for the identification of a compound with properties suitable for use as an in vitro tool compound for validation studies …
Information gleaned from ligand co-crystal structures allowed for rapid refinements in both MARK potency and kinase selectivity. Thes …
Optical High Content Nanoscopy of Epigenetic Marks Decodes Phenotypic Divergence in Stem Cells.
Kim JJ, Bennett NK, Devita MS, Chahar S, Viswanath S, Lee EA, Jung G, Shao PP, Childers EP, Liu S, Kulesa A, Garcia BA, Becker ML, Hwang NS, Madabhushi A, Verzi MP, Moghe PV. Kim JJ, et al. Sci Rep. 2017 Jan 4;7:39406. doi: 10.1038/srep39406. Sci Rep. 2017. PMID: 28051095 Free PMC article.
We propose the first such use of optical high content nanoscopy of histone epigenetic marks (epi-marks) in stem cells to classify emergent cell states. By combining nanoscopy with epi-mark textural image informatics, we developed a novel approach, termed EDICTS (Epi-mar …
We propose the first such use of optical high content nanoscopy of histone epigenetic marks (epi-marks) in stem cells to classify emergent c …