[HTML][HTML] Molecular interactions of cyclam and bicyclam non-peptide antagonists with the CXCR4 chemokine receptor
LO Gerlach, RT Skerlj, GJ Bridger… - Journal of Biological …, 2001 - ASBMB
The non-peptide CXCR4 receptor antagonist AMD3100, which is a potent blocker of human
immunodeficiency virus cell entry, is a symmetrical bicyclam composed of two identical 1, 4,
8, 11-tetraazacyclotetradecane (cyclam) moieties connected by a relatively rigid
phenylenebismethylene linker. Based on the known strong propensity of the cyclam moiety
to bind carboxylic acid groups, receptor mutagenesis identified Asp 171 and Asp 262,
located in transmembrane domain (TM) IV and TM-VI, respectively, at each end of the main …
immunodeficiency virus cell entry, is a symmetrical bicyclam composed of two identical 1, 4,
8, 11-tetraazacyclotetradecane (cyclam) moieties connected by a relatively rigid
phenylenebismethylene linker. Based on the known strong propensity of the cyclam moiety
to bind carboxylic acid groups, receptor mutagenesis identified Asp 171 and Asp 262,
located in transmembrane domain (TM) IV and TM-VI, respectively, at each end of the main …
