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Discovery of AZ0108, an orally bioavailable phthalazinone PARP inhibitor that blocks centrosome clustering

Academic Article
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  • Research
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Overview

authors

  • Johannes, J. W.
  • Almeida, L.
  • Daly, K.
  • Ferguson, A. D.
  • Grosskurth, S. E.
  • Guan, H.
  • Howard, T.
  • Ioannidis, S.
  • Kazmirski, S.
  • Lamb, M. L.
  • Larsen, Nicholas
  • Lyne, P. D.
  • Mikule, K.
  • Ogoe, C.
  • Peng, B.
  • Petteruti, P.
  • Read, J. A.
  • Su, N.
  • Sylvester, M.
  • Throner, S.
  • Wang, W.
  • Wang, X.
  • Wu, J.
  • Ye, Q.
  • Yu, Y.
  • Zheng, X.
  • Scott, D. A.

publication date

  • December 2015

journal

  • Bioorganic & Medicinal Chemistry Letters  Journal

subject areas

  • Administration, Oral
  • Animals
  • Binding Sites
  • Caco-2 Cells
  • Centrosome
  • Crystallography, X-Ray
  • Drug Evaluation, Preclinical
  • HeLa Cells
  • Humans
  • Microsomes
  • Molecular Conformation
  • Molecular Dynamics Simulation
  • Phthalazines
  • Poly(ADP-ribose) Polymerase Inhibitors
  • Protein Structure, Tertiary
  • Rats
  • Tankyrases
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Research

keywords

  • Cell cycle
  • Centrosome
  • Oncology
  • PARP
  • Tankyrase
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Identity

International Standard Serial Number (ISSN)

  • 0960-894X

Digital Object Identifier (DOI)

  • 10.1016/j.bmcl.2015.10.079

PubMed ID

  • 26546219
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Additional Document Info

start page

  • 5743

end page

  • 5747

volume

  • 25

issue

  • 24

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