No single drug available today blocks both of these coreceptors, so Dennis C. Liotta and colleagues at Emory University wondered whether they could come up with one. They overlaid the structures of CCR5 and CXCR4 and found a structurally similar binding motif in both coreceptors. They then virtually screened small molecules and found some that should block both coreceptors. Anthony Prosser, a graduate student in Liotta’s lab, devised a synthesis of one such compound and made many analogs (example shown). The molecules not only inhibited HIV’s binding to both CCR5 and CXCR4, but they also blocked HIV reverse transcriptase, an enzyme that’s key to the virus’s ability to copy itself. Liotta noted that the compounds are still in early development, but if successful, they could lead to a low-cost HIV treatment. /articles/93/i13/Dual-Action-Inhibitor-Fighting-HIV.html 20150330 ACS Meeting News: Chemists create compounds capable of binding both coreceptors HIV uses to infect T cells Concentrates 93 13 /magazine/93/09313.html /departments/.html /collections/con.html Dual-Action Inhibitor For Fighting HIV Science & Technology Bethany Halford Structure of a small molecule that inhibits coreceptors CXCR4 and CCR5.
by Bethany Halford |
March 30, 2015