Thursday, October 10, 2013
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Crystal structure of Selzentry maraviroc-bound HIV-1
co-receptor CC chemokine receptor 5 (CCR5; CD195)
The crystal structure of
HIV-1 co-receptor CCR5 bound by the allosteric inhibitor Selzentry maraviroc
could help to guide design of therapies for HIV-1 infection. The crystal
structure of the complex was determined at
2.7 Å resolution and showed Selzentry bound at a site distinct from proposed
recognition sites for chemokines and HIV gp120. Crystal
structure-based modeling showed that different charge distributions and
steric hindrances in the co-receptor ligand-binding pocket could be major
determinants for HIV-1 co-receptor selectivity. Next steps include structural
studies of CCR5 and CXC chemokine receptor 4 (CXCR4; NPY3R) in complex with the
HIV envelope protein gp120 and CD4 to obtain more insight
into the process of viral infection.
Selzentry is marketed by Pfizer Inc. to treat
CytoDyn Inc.'s CCR5
inhibitor, PRO 140, is in Phase II
Tobira Therapeutics Inc.
has the dual CCR5 and CCR2 (CD192) antagonist cenicriviroc in Phase II
trials to treat HIV/AIDS. (see Seeing CCR5, page 11)
Published online Oct. 10, 2013
status not applicable
Tan, Q. et al. Science;
published online Sept. 12, 2013;
Contact: Beili Wu, Shanghai Institute of Materia Medica, Chinese
Academy of Sciences,
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