In this phase of structure–affinity relationship study of VL-0395, a new anthranilic acid based CCK1 selective antagonist, we propose a series of unnatural aminoacidic derivatives. The result of this work is the identification of a new CCK ligand, which possesses an affinity (IC50 = 35 nm) one order of magnitude greater than the lead and, as a general rule, it points out how the hypothesized receptorial pocket which accommodates the Phe residue allows much more structural modification than that interacting with the N-terminal group.

Anthranilic Acid Based CCK1 Receptor Antagonists: Preliminary Investigation On Their Second “Touch point”

VARNAVAS, ANTONIOS;LASSIANI, LUCIA;
2005-01-01

Abstract

In this phase of structure–affinity relationship study of VL-0395, a new anthranilic acid based CCK1 selective antagonist, we propose a series of unnatural aminoacidic derivatives. The result of this work is the identification of a new CCK ligand, which possesses an affinity (IC50 = 35 nm) one order of magnitude greater than the lead and, as a general rule, it points out how the hypothesized receptorial pocket which accommodates the Phe residue allows much more structural modification than that interacting with the N-terminal group.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11368/1702836
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