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Merck
  • Identification of novel allosteric nonpeptidergic inhibitors of the human cytomegalovirus-encoded chemokine receptor US28.

Identification of novel allosteric nonpeptidergic inhibitors of the human cytomegalovirus-encoded chemokine receptor US28.

Bioorganic & medicinal chemistry (2009-12-25)
Henry F Vischer, Janneke W Hulshof, Saskia Hulscher, Silvina A Fratantoni, Mark H P Verheij, Jane Victorina, Martine J Smit, Iwan J P de Esch, Rob Leurs
ABSTRACT

Human cytomegalovirus (HCMV) is a widespread human pathogen, possessing onco-modulatory properties. Constitutive signaling of the HCMV-encoded chemokine receptor US28 and its ability to bind a broad spectrum of chemokines might facilitate HCMV-associated tumor progression. Novel nonpeptidergic chemotypes were identified as neutral antagonists or inverse agonists on US28, that allosterically inhibit chemokine binding to US28.