CXCR4 chemokine receptor antagonists: nickel(ii) complexes of configurationally restricted macrocycles
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چکیده
منابع مشابه
CXCR4 chemokine receptor antagonists: nickel(II) complexes of configurationally restricted macrocycles.
Tetraazamacrocyclic complexes of transition metals provide useful units for incorporating multiple coordination interactions into a single protein binding molecule. They can be designed with available sites for protein interactions via donor atom-containing amino acid side chains or labile ligands, such as H(2)O, allowing facile exchange. Three configurationally restricted nickel(II) cyclam com...
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A zinc(II) containing configurationally restricted analogue of bismacrocyclic cyclam-type CXCR4 chemokine receptor antagonists has been synthesized and shown to adopt only one configuration in solution. The single crystal X-ray structure reveals favorable binding to acetate via a bidentate chelation that can be related to the proposed interaction with aspartate on the receptor protein surface. ...
متن کاملBinding optimization through coordination chemistry: CXCR4 chemokine receptor antagonists from ultrarigid metal complexes.
A new copper(II) containing bis-macrocyclic CXCR4 chemokine receptor antagonist is shown to have improved binding properties to the receptor protein in comparison to the drug AMD3100 (Plerixafor, Mozobil). The interaction of the metallodrug has been optimized by using ultrarigid chelator units that offer an equatorial site for coordination to the amino acid side chains of the protein. Binding c...
متن کاملIdentification and profiling of CXCR3-CXCR4 chemokine receptor heteromer complexes.
BACKGROUND AND PURPOSE The C-X-C chemokine receptors 3 (CXCR3) and C-X-C chemokine receptors 4 (CXCR4) are involved in various autoimmune diseases and cancers. Small antagonists have previously been shown to cross-inhibit chemokine binding to CXCR4, CC chemokine receptors 2 (CCR2) and 5 (CCR5) heteromers. We investigated whether CXCR3 and CXCR4 can form heteromeric complexes and the binding cha...
متن کاملTitle: Synthesis of Thiophene Analogs as Potential Antagonists of Chemokine Receptor Type 4 (cxcr4)
Introduction: CXCR4 is a chemokine receptor involved in the progression of several disease pathways. Inhibition of CXCR4 with small molecules and peptides has been shown to: 1) reduce the inflammatory response in people suffering from autoimmune disorders such as Rheumatoid Arthritis, 2) in slowing the spread of cancer, and 3) in HIV-1 infection. We have designed a new series of thiophene compo...
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ژورنال
عنوان ژورنال: Dalton Transactions
سال: 2012
ISSN: 1477-9226,1477-9234
DOI: 10.1039/c2dt31137b