Identification of a non peptidic RANTES antagonist

DOI: 10.1016/S0960-894X(98)00094-8

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 771 - 774 (1998)

Update date:2022-07-30

Topics:

Authors:

Bright, Colin

Brown, Thomas J.

Cox, Paul

Halley, Frank

Lockey, Peter

McLay, Iain M.

Moore, Una

Porter, Barry

Williams, Robert J.

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Article abstract of DOI:10.1016/S0960-894X(98)00094-8

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

Full text of DOI:10.1016/S0960-894X(98)00094-8

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