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Identification Of A Non Peptidic Rantes Antagonist

C Bright,T J Brown,P Cox,F Halley,P Lockey,I M McLay,U Moore,B Porter,R J Williams

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS（1998）

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Abstract
A series of phenothiazines demonstrating inhibition of RANTES binding to THP-1 cell membranes has been identified. The lead compound RP23618 (IC50=3 mu M) was found to inhibit specific binding of I-125-RANTES, but not I-125-MCP-1 to THP-1 cell membranes and furthermore to antagonise RANTES, but not MCP-1-induced chemotaxis of THP-1 cells. (C) 1998 Elsevier Science Ltd. All rights reserved.
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peptidic rantes antagonist
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