Heptapeptide mimic of ohmefentanyl binding in the discontinuous mu-opiod receptor
by Gawley, Robert E.; Dukh, Mykhaylo; Cardona, Claudia M.; Jannach, Stephan H.; Greathouse, Denise V.
Ohmefentanyl binds to the rat mu-opiod receptor via two dipeptide sequences (Trp-His and Asp-Tyr) that are separated by 170 residues. A turn-inducing tripeptide, Pro-Aib-Aib, holds the dipeptides in a conformation that binds the narcotic (K-b = 7.1 x 10(4) M-1) in THF. Binding is specific for ohmefentanyl over morphine and is accompanied by a conformational change in the heptapeptide host. Control experiments with a Gly-Gly-Gly tripeptide linking the dipeptides show no evidence of binding.
- Organic Letters
- Start Page
- 1523-7052; 1523-7060