Now showing items 1-4 of 4

    • CCR2B receptor antagonists : Conversion of a weak HTS hit to a potent lead compound 

      Forbes, Ian T.; Cooper, David G.; Dodds, Emma K.; Hickey, Deirdre M. B.; Ife, Robert J.; Meeson, Malcolm; Stockley, Martin; Berkhout, Theo; Gohil, Jayneeta; Groot, Pieter H. E.; Moores, Kitty E. (2000-08-21)
      A weak HTS hit at the CCR2B receptor has been converted into a potent antagonist by array SAR studies. Selectivity over the closely related CCR5 receptor is also achieved. (C) 2000 Elsevier Science Ltd. All rights reserved.
    • Conformationally restricted indolopiperidine derivatives as potent CCR2B receptor antagonists 

      Witherington, Jason; Bordas, Vincent; Cooper, Dave G.; Forbes, Ian T.; Gribble, Andrew D.; Ife, Robert J.; Berkhout, Theo; Gohil, Jayneeta; Groot, Pieter H. E. (2001-08-20)
      The preparation and biological evaluation of a series of indolopiperidine CCR2B receptor antagonists possessing a conformationally restricted C-5 linker chain in combination with a restricted piperidine ring are described. ...
    • The role of fractalkine in the recruitment of monocytes to the endothelium 

      Chapman, Gayle A.; Moores, Kitty E.; Gohil, Jayneeta; Berkhout, Theo; Patel, Lisa; Green, Paula; MacPhee, Colin H.; Stewart, Brian R. (2000-03-31)
      Recombinant fractalkine possesses both chemoattractive and adhesive properties in vitro. Previous studies have demonstrated an upregulation of this molecule on the membranes of activated human endothelial cells and ...
    • Selective binding of the truncated form of the chemokine CKβ8 (25-99) to CC chemokine receptor 1 (CCR1) 

      Berkhout, Theo; Gohil, Jayneeta; Gonzalez, Pilar; Nicols, Charlotte L.; Moores, Kitty E.; MacPhee, Colin H.; White, John R.; Groot, Pieter H. E. (2000-03-01)
      Human CC chemokine receptor 1 (CCR1) has been proposed as a receptor for CKβ8. To obtain conclusive evidence, binding-displacement studies of 125I-CKβ8 (25-99) were performed on membranes of Chinese hamster ovary cells ...