As part of an ongoing drug development effort aimed at selective opioid receptor ligands based on the pawhuskin natural products we have synthesized a small set of amide isosteres. These amides were centered on lead compounds which are selective antagonists for the delta and kappa opioid receptors. The amide isomers revealed here show dramatically different activity from the parent stilbene compounds. Three of the isomers synthesized showed antagonist activity for the opioid growth factor (OGF)/opioid growth factor receptor (OGFR) axis which is involved in cellular and organ growth control. This cellular signaling mechanism is targeted by "low-dose" naltrexone therapy which is being tested clinically for multiple sclerosis, Crohn's disease, cancer, and wound healing disorders. The compounds described here are the first selective small molecule ligands for the OGF/OGFR system and will serve as important leads and probes for further study.
Pharmacology, Toxicology and Pharmaceutical Science
3
8%
Biochemistry, Genetics and Molecular Biology
2
5%
Neuroscience
2
5%
Other
6
16%
Unknown
13
34%
Attention Score in Context
Attention Score in Context
This research output has an Altmetric Attention Score of 1. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 22 September 2018.
All research outputs
#26,486,740
of 31,836,582 outputs
Outputs from Bioorganic & Medicinal Chemistry
#8,040
of 8,798 outputs
Outputs of similar age
#276,580
of 348,695 outputs
Outputs of similar age from Bioorganic & Medicinal Chemistry
#82
of 102 outputs
Altmetric has tracked 31,836,582 research outputs across all sources so far. This one is in the 9th percentile – i.e., 9% of other outputs scored the same or lower than it.
So far Altmetric has tracked 8,798 research outputs from this source. They typically receive a little more attention than average, with a mean Attention Score of 5.5. This one is in the 5th percentile – i.e., 5% of its peers scored the same or lower than it.
Older research outputs will score higher simply because they've had more time to accumulate mentions. To account for age we can compare this Altmetric Attention Score to the 348,695 tracked outputs that were published within six weeks on either side of this one in any source. This one is in the 11th percentile – i.e., 11% of its contemporaries scored the same or lower than it.
We're also able to compare this research output to 102 others from the same source and published within six weeks on either side of this one. This one is in the 9th percentile – i.e., 9% of its contemporaries scored the same or lower than it.
