Paul W. Manley

Research interests

Publications

• Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1

  Journal of Medicinal Chemistry · 2018 · 10.1021/acs.jmedchem.8b01040

• Imaging the intracellular distribution of tyrosine kinase inhibitors in living cells with quantitative hyperspectral stimulated Raman scattering

  Nature Chemistry · 2014 · 10.1038/nchem.1961

• Targeting Bcr–Abl by combining allosteric with ATP-binding-site inhibitors

  Nature · 2010 · 10.1038/nature08675

• Extended kinase profile and properties of the protein kinase inhibitor nilotinib

  Biochimica et Biophysica Acta (BBA) - Proteins and Proteomics · 2009 · 10.1016/j.bbapap.2009.11.008

• Solution Conformations and Dynamics of ABL Kinase-Inhibitor Complexes Determined by NMR Substantiate the Different Binding Modes of Imatinib/Nilotinib and Dasatinib

  Journal of Biological Chemistry · 2008 · 10.1074/jbc.m801337200

• Inhibition of collagen-induced discoidin domain receptor 1 and 2 activation by imatinib, nilotinib and dasatinib

  European Journal of Pharmacology · 2008 · 10.1016/j.ejphar.2008.10.014

• Expansion of Bcr-Abl-Positive Leukemic Stem Cells Is Dependent on Hedgehog Pathway Activation

  Cancer Cell · 2008 · 10.1016/j.ccr.2008.08.003

• Evidence that Resistance to Nilotinib May Be Due to BCR-ABL, Pgp, or Src Kinase Overexpression

  Cancer Research · 2008 · 10.1158/0008-5472.can-08-1008

• Second generation inhibitors of BCR-ABL for the treatment of imatinib-resistant chronic myeloid leukaemia

  Nature reviews. Cancer · 2007 · https://doi.org/10.1038/nrc2126

• Most CML patients who have a suboptimal response to imatinib have low OCT-1 activity: higher doses of imatinib may overcome the negative impact of low OCT-1 activity

  Blood · 2007 · 10.1182/blood-2007-06-093617

• Allosteric inhibitors of Bcr-abl–dependent cell proliferation

  Nature Chemical Biology · 2006 · 10.1038/nchembio760

• Structural biology contributions to the discovery of drugs to treat chronic myelogenous leukaemia

  Acta Crystallographica Section D Biological Crystallography · 2006 · 10.1107/s0907444906047287

• AMN107 (nilotinib): a novel and selective inhibitor of BCR-ABL

  British Journal of Cancer · 2006 · 10.1038/sj.bjc.6603170

• Nilotinib in Imatinib-Resistant CML and Philadelphia Chromosome–Positive ALL

  New England Journal of Medicine · 2006 · https://doi.org/10.1056/nejmoa055104

• OCT-1–mediated influx is a key determinant of the intracellular uptake of imatinib but not nilotinib (AMN107): reduced OCT-1 activity is the cause of low in vitro sensitivity to imatinib

  Blood · 2006 · 10.1182/blood-2005-11-4687

• In vitro Activity of Bcr-Abl Inhibitors AMN107 and BMS-354825 against Clinically Relevant Imatinib-Resistant Abl Kinase Domain Mutants

  Cancer Research · 2005 · https://doi.org/10.1158/0008-5472.can-05-0259

• AMN107, a Novel Aminopyrimidine Inhibitor of Bcr-Abl, Has In vitro Activity against Imatinib-Resistant Chronic Myeloid Leukemia

  Clinical Cancer Research · 2005 · 10.1158/1078-0432.ccr-04-2601

• The Crystal Structure of a c-Src Complex in an Active Conformation Suggests Possible Steps in c-Src Activation

  Structure · 2005 · 10.1016/j.str.2005.03.012

• PKC412 inhibits in vitro growth of neoplastic human mast cells expressing the D816V-mutated variant of KIT: comparison with AMN107, imatinib, and cladribine (2CdA) and evaluation of cooperative drug effects

  Blood · 2005 · 10.1182/blood-2005-07-3022

• Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl

  Cancer Cell · 2005 · https://doi.org/10.1016/j.ccr.2005.01.007

• PKC412 overcomes resistance to imatinib in a murine model of FIP1L1-PDGFRα-induced myeloproliferative disease

  Cancer Cell · 2003 · 10.1016/s1535-6108(03)00108-9

• Imatinib: a selective tyrosine kinase inhibitor

  European Journal of Cancer · 2002 · 10.1016/s0959-8049(02)80599-8

• Inhibition of mutant FLT3 receptors in leukemia cells by the small molecule tyrosine kinase inhibitor PKC412

  Cancer Cell · 2002 · 10.1016/s1535-6108(02)00069-7

• Tyrosine kinase inhibitors: From rational design to clinical trials

  Medicinal Research Reviews · 2001 · 10.1002/med.1022

• New Anilinophthalazines as Potent and Orally Well Absorbed Inhibitors of the VEGF Receptor Tyrosine Kinases Useful as Antagonists of Tumor-Driven Angiogenesis

  Journal of Medicinal Chemistry · 2000 · 10.1021/jm9909443

Current projects

No projects listed.