Browsing Research publications by Author "Groot, Pieter H. E."

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. ...

    • Identification of a truncated form of the CC chemokine CKβ-8 demonstrating greatly enhanced biological activity 

      MacPhee, Colin H.; Appelbaum, Edward R.; Johanson, Kyung; Moores, Kitty E.; Imburgia, Christina S.; Fornwald, Jim; Berkhout, Theo; Brawner, Mary; Groot, Pieter H. E.; O'Donnell, Kevin; O'Shannessy, Daniel; Scott, Gil; White, John R. (1998-12-01)
      A new CC chemokine, designated CKβ-8 or myeloid progenitor inhibitor factor-1, was recently identified in a large scale sequencing effort and was cloned from a human aortic endothelial library. CKβ-8 cDNA encodes a signal ...

    • 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 ...