2. Academic Validation
  3. Identification of a non peptidic RANTES antagonist

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

Affiliation

  • 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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