Identification of a non peptidic RANTES antagonist

  • Bioorg Med Chem Lett. 1998 Apr 7;8(7):771-4. doi: 10.1016/s0960-894x(98)00094-8.
C Bright  1 ,  T J Brown ,  P Cox ,  F Halley ,  P Lockey ,  I M McLay ,  U Moore ,  B Porter ,  R J Williams
Affiliations
  • 1. Rhône-Poulenc Rorer, Dagenham Research Centre, Dagenham, Essex, UK.
PMID: 9871539 DOI: 10.1016/s0960-894x(98)00094-8
Abstract

A series of phenothiazines demonstrating inhibition of RANTES binding to THP-1 cell membranes has been identified. The lead compound RP23618 (IC50 = 3 microM) was found to inhibit specific binding of 125I-RANTES, but not 125I-MCP-1 to THP-1 cell membranes and furthermore to antagonize RANTES, but not MCP-1-induced chemotaxis of THP-1 cells.

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